Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10210629 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 2 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 None
107810 1646 25 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 604 12 4 6 3.4 CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C 7647976
998 1646 25 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 604 12 4 6 3.4 CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C 7647976
CHEMBL352396 1646 25 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 604 12 4 6 3.4 CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C 7647976
3951 388 82 None 47 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
4337 388 82 None 47 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
6918493 388 82 None 47 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
CHEMBL1111 388 82 None 47 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
DB06403 388 82 None 47 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
3539 4062 78 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 6 1 9 2.7 COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1 15956965
9910224 4062 78 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 6 1 9 2.7 COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1 15956965
CHEMBL1628688 4062 78 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 6 1 9 2.7 COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1 15956965
DB06629 4062 78 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 6 1 9 2.7 COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1 15956965
10070 445 41 None 109 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
25099191 445 41 None 109 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
CHEMBL2165326 445 41 None 109 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
DB15059 445 41 None 109 2 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
1000 3434 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 614 14 2 9 6.1 CCCCn1ncc(c1c1ccc(cc1OCc1ccccc1C(=O)O)OC)/C=C(/C(=O)O)\Cc1cc2OCOc2cc1OC 9694916
5311425 3434 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 614 14 2 9 6.1 CCCCn1ncc(c1c1ccc(cc1OCc1ccccc1C(=O)O)OC)/C=C(/C(=O)O)\Cc1cc2OCOc2cc1OC 9694916
CHEMBL1628624 3434 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 614 14 2 9 6.1 CCCCn1ncc(c1c1ccc(cc1OCc1ccccc1C(=O)O)OC)/C=C(/C(=O)O)\Cc1cc2OCOc2cc1OC 9694916
16004692 2411 85 None 107 2 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
4809 2411 85 None 107 2 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
7352 2411 85 None 107 2 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
CHEMBL2103873 2411 85 None 107 2 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
DB08932 2411 85 None 107 2 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
131845706 3403 6 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
71308726 3403 6 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
995 3403 6 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
CHEMBL1222310 3403 6 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
CHEMBL4524099 3403 6 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
101598716 1526 26 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
16133807 1526 26 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
16212950 1526 26 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
989 1526 26 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
CHEMBL3775234 1526 26 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
16133808 1527 0 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
16219332 1527 0 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
56947103 1527 0 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
990 1527 0 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
CHEMBL3774897 1527 0 None - 1 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7647976
108002 3425 14 None -1 2 Rat 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588
3528 3425 14 None -1 2 Rat 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588
CHEMBL8823 3425 14 None -1 2 Rat 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
CHEMBL2370066 208022 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL315841 209437 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
CHEMBL2370067 208023 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](N)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@H](C=O)Cc1c[nH]c2ccccc12)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL407269 210894 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL313344 209356 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL387200 210651 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL86703 214102 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C 10.1021/jm00070a001
10985050 9407 0 None - 0 Pig 11.4 pIC50 = 11.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 629 11 1 10 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(Br)cn1 10.1021/jm0102304
CHEMBL112144 9407 0 None - 0 Pig 11.4 pIC50 = 11.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 629 11 1 10 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(Br)cn1 10.1021/jm0102304
44284437 99509 0 None - 0 Human 11.0 pIC50 = 11.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL286621 99509 0 None - 0 Human 11.0 pIC50 = 11.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1 10.1016/j.bmcl.2004.01.008
44284405 99879 0 None - 0 Human 11.0 pIC50 = 11.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL289634 99879 0 None - 0 Human 11.0 pIC50 = 11.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
44284287 160688 0 None - 0 Human 11.0 pIC50 = 11.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL411925 160688 0 None - 0 Human 11.0 pIC50 = 11.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
11017304 113628 0 None - 0 Pig 10.9 pIC50 = 10.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 579 11 1 9 5.8 CCc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)cc1 10.1021/jm0102304
CHEMBL332922 113628 0 None - 0 Pig 10.9 pIC50 = 10.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 579 11 1 9 5.8 CCc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)cc1 10.1021/jm0102304
44284288 99660 0 None - 0 Human 10.9 pIC50 = 10.9 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287683 99660 0 None - 0 Human 10.9 pIC50 = 10.9 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1 10.1016/j.bmcl.2004.01.008
44284292 167538 0 None - 0 Human 10.9 pIC50 = 10.9 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 518 8 3 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)(C)O)c1 10.1016/j.bmcl.2004.01.008
CHEMBL432856 167538 0 None - 0 Human 10.9 pIC50 = 10.9 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 518 8 3 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)(C)O)c1 10.1016/j.bmcl.2004.01.008
9852318 9508 5 None - 2 Rat 10.8 pIC50 = 10.8 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL112624 9508 5 None - 2 Rat 10.8 pIC50 = 10.8 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL1627022 9508 5 None - 2 Rat 10.8 pIC50 = 10.8 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
11082446 9803 0 None - 0 Pig 10.8 pIC50 = 10.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 581 12 1 11 4.6 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2Oc2cccc(OC)c2)nc1 10.1021/jm0102304
CHEMBL114380 9803 0 None - 0 Pig 10.8 pIC50 = 10.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 581 12 1 11 4.6 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2Oc2cccc(OC)c2)nc1 10.1021/jm0102304
10897569 10030 0 None - 0 Pig 10.7 pIC50 = 10.7 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 645 11 1 10 5.7 COc1ccccc1Sc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(Br)cn1 10.1021/jm0102304
CHEMBL115724 10030 0 None - 0 Pig 10.7 pIC50 = 10.7 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 645 11 1 10 5.7 COc1ccccc1Sc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(Br)cn1 10.1021/jm0102304
10227760 100505 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 481 6 2 7 4.9 CC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL294291 100505 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 481 6 2 7 4.9 CC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
10163017 199087 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 482 6 3 8 4.6 C/C(=N\O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL60058 199087 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 482 6 3 8 4.6 C/C(=N\O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
44284236 121796 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 504 9 3 7 4.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCCO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL35984 121796 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 504 9 3 7 4.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCCO)c1 10.1016/j.bmcl.2004.01.008
72548703 161007 0 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysisDisplacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161007 0 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysisDisplacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
101598716 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
16133807 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
16212950 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
989 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
CHEMBL3775234 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
101598716 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
16133807 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
16212950 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
989 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
CHEMBL3775234 1526 26 None - 0 Human 10.6 pIC50 = 10.6 Binding
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
44284288 99660 0 None - 0 Human 10.6 pIC50 = 10.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287683 99660 0 None - 0 Human 10.6 pIC50 = 10.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1 10.1016/j.bmcl.2004.01.008
44284405 99879 0 None - 0 Human 10.6 pIC50 = 10.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL289634 99879 0 None - 0 Human 10.6 pIC50 = 10.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
9873636 173242 0 None - 0 Rat 10.6 pIC50 = 10.6 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 607 10 1 10 6.4 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cc3ccccc3s2)nc1 10.1016/j.bmcl.2016.06.014
CHEMBL4538570 173242 0 None - 0 Rat 10.6 pIC50 = 10.6 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 607 10 1 10 6.4 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cc3ccccc3s2)nc1 10.1016/j.bmcl.2016.06.014
44381151 59062 0 None - 0 Pig 10.6 pIC50 = 10.6 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 671 13 1 10 6.3 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1016/s0960-894x(01)00682-5
CHEMBL170908 59062 0 None - 0 Pig 10.6 pIC50 = 10.6 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 671 13 1 10 6.3 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1016/s0960-894x(01)00682-5
44284266 136396 0 None - 0 Human 10.6 pIC50 = 10.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 531 8 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CN(C)C(C)=O)c1 10.1016/j.bmcl.2004.01.008
CHEMBL37427 136396 0 None - 0 Human 10.6 pIC50 = 10.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 531 8 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CN(C)C(C)=O)c1 10.1016/j.bmcl.2004.01.008
11039156 9960 0 None - 0 Pig 10.6 pIC50 = 10.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 581 11 1 10 5.2 COc1cccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)c1 10.1021/jm0102304
CHEMBL115333 9960 0 None - 0 Pig 10.6 pIC50 = 10.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 581 11 1 10 5.2 COc1cccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)c1 10.1021/jm0102304
10206855 100422 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 493 7 2 7 5.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CC2)c1 10.1021/jm030528p
CHEMBL293830 100422 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 493 7 2 7 5.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CC2)c1 10.1021/jm030528p
10185556 102170 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 503 6 2 8 3.8 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(C)(=O)=O)c1 10.1021/jm030528p
CHEMBL304460 102170 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 503 6 2 8 3.8 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(C)(=O)=O)c1 10.1021/jm030528p
10228523 199535 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 495 7 2 7 5.3 CCC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL60367 199535 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 495 7 2 7 5.3 CCC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
44284238 99652 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 490 8 3 7 4.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287622 99652 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 490 8 3 7 4.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCO)c1 10.1016/j.bmcl.2004.01.008
10152810 14602 1 None - 0 Rat 10.5 pIC50 = 10.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F 10.1016/s0960-894x(98)00301-1
CHEMBL1206706 14602 1 None - 0 Rat 10.5 pIC50 = 10.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F 10.1016/s0960-894x(98)00301-1
CHEMBL298725 14602 1 None - 0 Rat 10.5 pIC50 = 10.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F 10.1016/s0960-894x(98)00301-1
159594 518 38 None 1 3 Human 10.5 pIC50 = 10.5 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm970101g
3487 518 38 None 1 3 Human 10.5 pIC50 = 10.5 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm970101g
CHEMBL9194 518 38 None 1 3 Human 10.5 pIC50 = 10.5 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm970101g
DB06199 518 38 None 1 3 Human 10.5 pIC50 = 10.5 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm970101g
10962637 9969 0 None - 0 Rat 10.5 pIC50 = 10.5 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 549 10 2 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1 10.1021/jm000538f
CHEMBL115372 9969 0 None - 0 Rat 10.5 pIC50 = 10.5 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 549 10 2 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1 10.1021/jm000538f
CHEMBL1627023 9969 0 None - 0 Rat 10.5 pIC50 = 10.5 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 549 10 2 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1 10.1021/jm000538f
159594 518 38 None 1 3 Human 10.5 pIC50 = 10.5 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990171i
3487 518 38 None 1 3 Human 10.5 pIC50 = 10.5 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990171i
CHEMBL9194 518 38 None 1 3 Human 10.5 pIC50 = 10.5 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990171i
DB06199 518 38 None 1 3 Human 10.5 pIC50 = 10.5 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990171i
11767155 11621 0 None - 0 Pig 10.4 pIC50 = 10.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 596 10 1 9 5.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccccn3)cn2)cc1 10.1021/jm0102304
CHEMBL1181545 11621 0 None - 0 Pig 10.4 pIC50 = 10.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 596 10 1 9 5.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccccn3)cn2)cc1 10.1021/jm0102304
CHEMBL177173 11621 0 None - 0 Pig 10.4 pIC50 = 10.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 596 10 1 9 5.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccccn3)cn2)cc1 10.1021/jm0102304
44284041 99826 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL289216 99826 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1 10.1016/j.bmcl.2004.01.008
9938571 9491 0 None - 1 Rat 10.4 pIC50 = 10.4 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptorAbility to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptor
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL112531 9491 0 None - 1 Rat 10.4 pIC50 = 10.4 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptorAbility to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptor
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL369489 9491 0 None - 1 Rat 10.4 pIC50 = 10.4 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptorAbility to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptor
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
9938571 9491 0 None - 1 Rat 10.4 pIC50 = 10.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL112531 9491 0 None - 1 Rat 10.4 pIC50 = 10.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL369489 9491 0 None - 1 Rat 10.4 pIC50 = 10.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
10187997 109471 0 None - 0 Rat 10.4 pIC50 = 10.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm031041j
CHEMBL323464 109471 0 None - 0 Rat 10.4 pIC50 = 10.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm031041j
11828009 9783 0 None - 0 Pig 10.4 pIC50 = 10.4 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 581 11 2 10 4.7 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(CO)cc2)nc1 10.1021/jm000538f
CHEMBL114298 9783 0 None - 0 Pig 10.4 pIC50 = 10.4 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 581 11 2 10 4.7 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(CO)cc2)nc1 10.1021/jm000538f
11966523 109868 0 None - 0 Pig 10.4 pIC50 = 10.4 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 613 10 2 9 4.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(CO)cc2)cc1 10.1021/jm000538f
CHEMBL324184 109868 0 None - 0 Pig 10.4 pIC50 = 10.4 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 613 10 2 9 4.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(CO)cc2)cc1 10.1021/jm000538f
9934302 72284 1 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 467 6 2 7 4.6 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL19950 72284 1 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 467 6 2 7 4.6 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
11752337 161666 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 496 7 2 8 4.7 CO/N=C(\C)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL416324 161666 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 496 7 2 8 4.7 CO/N=C(\C)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
23445355 199208 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 469 6 2 8 3.8 COC(=O)c1cc(C)ccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL60149 199208 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 469 6 2 8 3.8 COC(=O)c1cc(C)ccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
9934302 72284 1 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 467 6 2 7 4.6 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm000349x
CHEMBL19950 72284 1 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 467 6 2 7 4.6 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm000349x
44284115 99719 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL288247 99719 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1 10.1016/j.bmcl.2004.01.008
44381125 58962 0 None - 0 Pig 10.4 pIC50 = 10.4 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 674 10 1 9 6.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(-c3ccccn3)nc2OCCOc2ncc(Br)cn2)cc1 10.1016/s0960-894x(01)00682-5
CHEMBL170493 58962 0 None - 0 Pig 10.4 pIC50 = 10.4 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 674 10 1 9 6.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(-c3ccccn3)nc2OCCOc2ncc(Br)cn2)cc1 10.1016/s0960-894x(01)00682-5
10187997 109471 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL323464 109471 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
44284287 160688 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL411925 160688 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
44284481 211967 0 None -4 5 Human 10.3 pIC50 = 10.3 Binding
Inhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/np900287e
CHEMBL437472 211967 0 None -4 5 Human 10.3 pIC50 = 10.3 Binding
Inhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/np900287e
44284328 127006 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 476 7 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC)c1 10.1016/j.bmcl.2004.01.008
CHEMBL36627 127006 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 476 7 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC)c1 10.1016/j.bmcl.2004.01.008
44284437 99509 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL286621 99509 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1 10.1016/j.bmcl.2004.01.008
44386450 62054 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 606 15 1 10 5.1 COC(=O)CCCCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OC)c1OC 10.1021/jm031041j
CHEMBL177973 62054 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 606 15 1 10 5.1 COC(=O)CCCCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OC)c1OC 10.1021/jm031041j
44284481 211967 0 None -4 5 Human 10.3 pIC50 = 10.3 Binding
Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.ejmech.2013.01.044
CHEMBL437472 211967 0 None -4 5 Human 10.3 pIC50 = 10.3 Binding
Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.ejmech.2013.01.044
10143256 100095 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 531 7 2 8 4.6 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(=O)(=O)C(C)C)c1 10.1021/jm030528p
CHEMBL291592 100095 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 531 7 2 8 4.6 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(=O)(=O)C(C)C)c1 10.1021/jm030528p
10183338 201089 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 464 5 2 7 4.5 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C#N)c1C 10.1021/jm030528p
CHEMBL62159 201089 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 464 5 2 7 4.5 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C#N)c1C 10.1021/jm030528p
10722385 100020 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 606 13 1 11 4.6 COC(=O)CCCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
CHEMBL291058 100020 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 606 13 1 11 4.6 COC(=O)CCCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
11006709 9848 0 None - 0 Pig 10.3 pIC50 = 10.3 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membraneIn vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane
ChEMBL 629 11 1 10 5.4 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1016/s0960-894x(01)00682-5
CHEMBL114700 9848 0 None - 0 Pig 10.3 pIC50 = 10.3 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membraneIn vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane
ChEMBL 629 11 1 10 5.4 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1016/s0960-894x(01)00682-5
11006709 9848 0 None - 0 Pig 10.3 pIC50 = 10.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 629 11 1 10 5.4 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm0102304
CHEMBL114700 9848 0 None - 0 Pig 10.3 pIC50 = 10.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 629 11 1 10 5.4 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm0102304
10651488 162815 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
CHEMBL419367 162815 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
159594 518 38 None 1 3 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/acs.jmedchem.5b01781
3487 518 38 None 1 3 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/acs.jmedchem.5b01781
CHEMBL9194 518 38 None 1 3 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/acs.jmedchem.5b01781
DB06199 518 38 None 1 3 Human 10.3 pIC50 = 10.3 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/acs.jmedchem.5b01781
44284041 99826 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL289216 99826 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1 10.1016/j.bmcl.2004.01.008
11734600 9900 0 None - 0 Pig 10.2 pIC50 = 10.2 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 585 11 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)c1 10.1021/jm0102304
CHEMBL114964 9900 0 None - 0 Pig 10.2 pIC50 = 10.2 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 585 11 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)c1 10.1021/jm0102304
44284115 99719 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL288247 99719 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1 10.1016/j.bmcl.2004.01.008
10119327 201059 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 531 8 2 8 4.6 CCCS(=O)(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL62019 201059 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 531 8 2 8 4.6 CCCS(=O)(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
10206155 201079 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 481 7 2 7 5.0 CCC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL62112 201079 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 481 7 2 7 5.0 CCC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
10344914 99662 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 476 7 3 7 4.1 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287711 99662 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 476 7 3 7 4.1 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CO)c1 10.1016/j.bmcl.2004.01.008
44284391 138758 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 9 3 7 5.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCC(C)(C)O)c1 10.1016/j.bmcl.2004.01.008
CHEMBL37920 138758 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 532 9 3 7 5.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCC(C)(C)O)c1 10.1016/j.bmcl.2004.01.008
10119177 116949 0 None - 0 Rat 10.2 pIC50 = 10.2 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 528 12 1 6 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm010237l
CHEMBL339904 116949 0 None - 0 Rat 10.2 pIC50 = 10.2 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 528 12 1 6 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm010237l
10603409 110102 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL325581 110102 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
10228588 101375 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 496 6 2 7 4.1 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)C)c1 10.1021/jm030528p
CHEMBL300577 101375 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 496 6 2 7 4.1 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)C)c1 10.1021/jm030528p
10210629 8661 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL109644 8661 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
9916235 9248 1 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL111277 9248 1 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
159594 518 38 None 1 3 Human 10.1 pIC50 = 10.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990170q
3487 518 38 None 1 3 Human 10.1 pIC50 = 10.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990170q
CHEMBL9194 518 38 None 1 3 Human 10.1 pIC50 = 10.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990170q
DB06199 518 38 None 1 3 Human 10.1 pIC50 = 10.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990170q
9916235 9248 1 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm990170q
CHEMBL111277 9248 1 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm990170q
10278217 101287 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 492 6 2 8 5.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ncco2)c1 10.1021/jm030528p
CHEMBL299921 101287 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 492 6 2 8 5.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ncco2)c1 10.1021/jm030528p
9911482 167499 15 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 447 6 2 7 4.2 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm030528p
CHEMBL432521 167499 15 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 447 6 2 7 4.2 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm030528p
10114414 197134 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 444 5 2 7 4.2 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C#N)c1C 10.1021/jm030528p
CHEMBL58359 197134 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 444 5 2 7 4.2 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C#N)c1C 10.1021/jm030528p
11766844 109280 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 553 9 1 8 5.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1 10.1021/jm0102304
CHEMBL176272 109280 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 553 9 1 8 5.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1 10.1021/jm0102304
CHEMBL323243 109280 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 553 9 1 8 5.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1 10.1021/jm0102304
159594 518 38 None -1 3 Rat 10.1 pIC50 = 10.1 Binding
Inhibitory activity against human Endothelin A receptorInhibitory activity against human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
3487 518 38 None -1 3 Rat 10.1 pIC50 = 10.1 Binding
Inhibitory activity against human Endothelin A receptorInhibitory activity against human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
CHEMBL9194 518 38 None -1 3 Rat 10.1 pIC50 = 10.1 Binding
Inhibitory activity against human Endothelin A receptorInhibitory activity against human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
DB06199 518 38 None -1 3 Rat 10.1 pIC50 = 10.1 Binding
Inhibitory activity against human Endothelin A receptorInhibitory activity against human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
10115469 100358 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 459 5 2 6 5.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(Cl)c1 10.1021/jm030528p
CHEMBL293398 100358 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 459 5 2 6 5.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(Cl)c1 10.1021/jm030528p
10627272 202349 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 592 12 1 11 4.2 COC(=O)CCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
CHEMBL69986 202349 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 592 12 1 11 4.2 COC(=O)CCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
10603409 110102 0 None - 0 Rat 10.0 pIC50 = 10.0 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL325581 110102 0 None - 0 Rat 10.0 pIC50 = 10.0 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
10187997 109471 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL323464 109471 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
21041278 171201 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 554 12 2 9 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4467748 171201 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 554 12 2 9 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
10165963 102363 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 545 8 2 9 3.6 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)CS(C)(=O)=O)c1 10.1021/jm030528p
CHEMBL305602 102363 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 545 8 2 9 3.6 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)CS(C)(=O)=O)c1 10.1021/jm030528p
10366278 171887 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 446 6 2 6 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL448165 171887 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 446 6 2 6 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
10624511 71379 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 478 6 2 7 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2noc(C)c2Cl)c(C)c1CC#N 10.1021/jm000349x
CHEMBL19661 71379 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 478 6 2 7 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2noc(C)c2Cl)c(C)c1CC#N 10.1021/jm000349x
10210629 8661 0 None - 0 Rat 10.0 pIC50 = 10.0 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL109644 8661 0 None - 0 Rat 10.0 pIC50 = 10.0 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
11827657 19169 1 None - 0 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 540 13 1 7 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1 10.1021/jm010237l
CHEMBL129220 19169 1 None - 0 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 540 13 1 7 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1 10.1021/jm010237l
44284481 211967 0 None -4 5 Human 10.0 pIC50 = 10.0 Binding
Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmc.2013.03.016
CHEMBL437472 211967 0 None -4 5 Human 10.0 pIC50 = 10.0 Binding
Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmc.2013.03.016
44302615 198730 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 497 7 2 8 4.6 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)OC(C)C)c1 10.1021/jm030528p
CHEMBL59819 198730 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 497 7 2 8 4.6 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)OC(C)C)c1 10.1021/jm030528p
25211074 18284 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1272244 18284 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
11016761 108523 0 None - 0 Pig 10.0 pIC50 = 10.0 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 519 9 1 8 4.8 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)cc1 10.1021/jm0102304
CHEMBL321242 108523 0 None - 0 Pig 10.0 pIC50 = 10.0 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 519 9 1 8 4.8 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)cc1 10.1021/jm0102304
44284329 99933 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 504 8 2 7 5.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)C)c1 10.1016/j.bmcl.2004.01.008
CHEMBL290181 99933 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 504 8 2 7 5.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)C)c1 10.1016/j.bmcl.2004.01.008
9914310 204907 3 None 1995 2 Human 10.0 pIC50 = 10.0 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8923 204907 3 None 1995 2 Human 10.0 pIC50 = 10.0 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
10768977 61504 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 548 13 1 8 5.6 CCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OCC)c1OCC 10.1021/jm031041j
CHEMBL177378 61504 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 548 13 1 8 5.6 CCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OCC)c1OCC 10.1021/jm031041j
44352079 116028 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 494 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1 10.1021/jm010237l
CHEMBL336272 116028 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 494 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1 10.1021/jm010237l
10674176 162138 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 548 11 1 9 5.0 CCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OCC)c1OCC 10.1021/jm9606507
CHEMBL417067 162138 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 548 11 1 9 5.0 CCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OCC)c1OCC 10.1021/jm9606507
44334146 167426 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 446 7 2 6 4.6 CCCNc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL432012 167426 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 446 7 2 6 4.6 CCCNc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
10163744 98248 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 495 7 2 7 5.2 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C(C)C)c1 10.1021/jm000349x
CHEMBL277706 98248 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 495 7 2 7 5.2 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C(C)C)c1 10.1021/jm000349x
9916235 9248 1 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL111277 9248 1 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
11465535 199376 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 468 6 3 7 3.5 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1 10.1021/jm030528p
CHEMBL60276 199376 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 468 6 3 7 3.5 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1 10.1021/jm030528p
10277399 66517 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 478 6 2 7 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1CC#N 10.1021/jm000349x
CHEMBL18626 66517 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 478 6 2 7 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1CC#N 10.1021/jm000349x
10139080 72207 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 454 6 2 7 4.6 Cc1cc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O 10.1021/jm000349x
CHEMBL19921 72207 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 454 6 2 7 4.6 Cc1cc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O 10.1021/jm000349x
10717923 98227 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm030528p
CHEMBL277595 98227 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm030528p
9810351 57760 0 None - 0 Pig 9.8 pIC50 = 9.8 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 705 14 2 12 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCO)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
CHEMBL167314 57760 0 None - 0 Pig 9.8 pIC50 = 9.8 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 705 14 2 12 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCO)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
44284481 211967 0 None -3 5 Pig 9.8 pIC50 = 9.8 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00077a013
CHEMBL437472 211967 0 None -3 5 Pig 9.8 pIC50 = 9.8 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00077a013
9936145 18822 1 None - 1 Human 9.8 pIC50 = 9.8 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
CHEMBL128818 18822 1 None - 1 Human 9.8 pIC50 = 9.8 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
44284481 211967 0 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of radiolabeled endothelin-1 from human endothelin ETA receptorDisplacement of radiolabeled endothelin-1 from human endothelin ETA receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm8007618
CHEMBL437472 211967 0 None -4 5 Human 9.8 pIC50 = 9.8 Binding
Displacement of radiolabeled endothelin-1 from human endothelin ETA receptorDisplacement of radiolabeled endothelin-1 from human endothelin ETA receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm8007618
11731472 9406 0 None - 0 Pig 9.8 pIC50 = 9.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 571 10 1 10 5.6 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)s2)nc1 10.1021/jm0102304
CHEMBL112141 9406 0 None - 0 Pig 9.8 pIC50 = 9.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 571 10 1 10 5.6 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)s2)nc1 10.1021/jm0102304
11050163 11624 0 None - 0 Pig 9.8 pIC50 = 9.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 583 10 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL1181553 11624 0 None - 0 Pig 9.8 pIC50 = 9.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 583 10 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL177924 11624 0 None - 0 Pig 9.8 pIC50 = 9.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 583 10 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
44351968 117564 0 None - 0 Rat 9.8 pIC50 = 9.8 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 508 12 1 5 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
CHEMBL340575 117564 0 None - 0 Rat 9.8 pIC50 = 9.8 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 508 12 1 5 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
10717923 98227 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm000349x
CHEMBL277595 98227 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm000349x
10623757 98461 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 458 6 2 7 4.4 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1CC#N 10.1021/jm000349x
CHEMBL279471 98461 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 458 6 2 7 4.4 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1CC#N 10.1021/jm000349x
9806559 9046 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O 10.1021/jm980217s
CHEMBL110053 9046 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O 10.1021/jm980217s
9936145 18822 1 None - 1 Human 9.7 pIC50 = 9.7 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
CHEMBL128818 18822 1 None - 1 Human 9.7 pIC50 = 9.7 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
CHEMBL1790959 207155 0 None - 0 Pig 9.7 pIC50 = 9.7 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
9825494 200914 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm031041j
CHEMBL61211 200914 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm031041j
9825494 200914 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL61211 200914 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
9825494 200914 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 minsDisplacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 mins
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/acs.jmedchem.5b01781
CHEMBL61211 200914 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 minsDisplacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 mins
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/acs.jmedchem.5b01781
9868637 98618 1 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 455 5 3 7 4.4 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O 10.1021/jm000349x
CHEMBL280659 98618 1 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 455 5 3 7 4.4 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O 10.1021/jm000349x
CHEMBL1790963 207158 0 None - 0 Pig 9.7 pIC50 = 9.7 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
11757759 173864 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 570 13 2 10 2.8 COCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4553625 173864 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 570 13 2 10 2.8 COCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
18931096 58424 0 None - 0 Pig 9.7 pIC50 = 9.7 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 689 14 2 12 4.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(OCCO)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
CHEMBL168604 58424 0 None - 0 Pig 9.7 pIC50 = 9.7 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 689 14 2 12 4.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(OCCO)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
44284481 211967 0 None -4 5 Human 9.7 pIC50 = 9.7 Binding
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
CHEMBL437472 211967 0 None -4 5 Human 9.7 pIC50 = 9.7 Binding
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
10722371 101745 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 605 11 1 11 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN3CCOCC3)c2)cc1 10.1021/jm980504w
CHEMBL302974 101745 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 605 11 1 11 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN3CCOCC3)c2)cc1 10.1021/jm980504w
10578853 103104 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 564 10 1 11 3.4 COC(=O)COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
CHEMBL308646 103104 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 564 10 1 11 3.4 COC(=O)COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
44334128 4325 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 443 7 1 5 4.9 C=CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL101424 4325 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 443 7 1 5 4.9 C=CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
9939238 202419 0 None - 1 Human 9.7 pIC50 = 9.7 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 637 12 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70385 202419 0 None - 1 Human 9.7 pIC50 = 9.7 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 637 12 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44284481 211967 0 None -4 5 Human 9.7 pIC50 = 9.7 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00400-9
CHEMBL437472 211967 0 None -4 5 Human 9.7 pIC50 = 9.7 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00400-9
CHEMBL1790960 207156 0 None - 0 Pig 9.7 pIC50 = 9.7 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00077a013
10120499 109255 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 564 12 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CC(C)C 10.1021/jm970101g
CHEMBL323055 109255 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 564 12 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CC(C)C 10.1021/jm970101g
11113541 201568 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 476 7 1 7 5.2 COc1ccc(OC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL64632 201568 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 476 7 1 7 5.2 COc1ccc(OC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
10299555 100551 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 481 6 2 7 4.9 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL294563 100551 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 481 6 2 7 4.9 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
10321290 4553 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 445 7 1 5 5.1 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL102969 4553 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 445 7 1 5 5.1 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
10651488 162815 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
CHEMBL419367 162815 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
44284381 127974 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 462 6 3 7 4.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(O)c1 10.1016/j.bmcl.2004.01.008
CHEMBL36671 127974 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 462 6 3 7 4.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(O)c1 10.1016/j.bmcl.2004.01.008
10648937 205565 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9334 205565 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44284481 211967 0 None -4 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2013.01.025
CHEMBL437472 211967 0 None -4 5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2013.01.025
123883 14460 1 None - 0 Human 9.6 pIC50 = 9.6 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm970101g
CHEMBL1205177 14460 1 None - 0 Human 9.6 pIC50 = 9.6 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm970101g
CHEMBL61425 14460 1 None - 0 Human 9.6 pIC50 = 9.6 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm970101g
123883 14460 1 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030528p
CHEMBL1205177 14460 1 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030528p
CHEMBL61425 14460 1 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030528p
11006532 12122 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 601 10 1 9 6.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1 10.1021/jm0102304
CHEMBL1184515 12122 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 601 10 1 9 6.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1 10.1021/jm0102304
CHEMBL367445 12122 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 601 10 1 9 6.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1 10.1021/jm0102304
9894460 204972 6 None 24 3 Human 9.6 pIC50 = 9.6 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm970101g
CHEMBL313871 204972 6 None 24 3 Human 9.6 pIC50 = 9.6 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm970101g
CHEMBL8978 204972 6 None 24 3 Human 9.6 pIC50 = 9.6 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm970101g
22004774 100329 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 442 8 1 6 5.7 CCCCSC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL293192 100329 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 442 8 1 6 5.7 CCCCSC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL2304284 207733 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation counting
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/np900287e
44387242 119884 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 502 15 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(C)C 10.1021/jm031041j
CHEMBL353560 119884 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 502 15 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(C)C 10.1021/jm031041j
11093237 10294 0 None - 0 Pig 9.5 pIC50 = 9.5 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 601 10 1 9 6.4 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc3ccccc3c2)nc1 10.1021/jm0102304
CHEMBL116281 10294 0 None - 0 Pig 9.5 pIC50 = 9.5 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 601 10 1 9 6.4 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc3ccccc3c2)nc1 10.1021/jm0102304
10769526 102214 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 578 12 2 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCC(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL304762 102214 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 578 12 2 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCC(=O)O)c2)cc1 10.1021/jm980504w
9870959 8814 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
CHEMBL109778 8814 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
44339655 9003 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL109926 9003 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
10278777 167558 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL432974 167558 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
9870830 204977 34 None 66 2 Human 9.5 pIC50 = 9.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL8981 204977 34 None 66 2 Human 9.5 pIC50 = 9.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
9939238 202419 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 637 12 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL70385 202419 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 637 12 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
21041284 170360 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 568 13 2 9 3.9 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4455360 170360 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 568 13 2 9 3.9 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
58688006 170540 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 524 13 2 9 3.8 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4458005 170540 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 524 13 2 9 3.8 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
21041264 81585 1 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 600 12 2 8 4.0 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2165339 81585 1 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 600 12 2 8 4.0 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
10311570 14446 0 None - 1 Rat 9.5 pIC50 = 9.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 520 10 1 9 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205068 14446 0 None - 1 Rat 9.5 pIC50 = 9.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 520 10 1 9 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL48907 14446 0 None - 1 Rat 9.5 pIC50 = 9.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 520 10 1 9 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
10555424 202329 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 592 13 2 10 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCCC(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL69832 202329 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 592 13 2 10 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCCC(=O)O)c2)cc1 10.1021/jm980504w
9870830 204977 34 None 66 2 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm980504w
CHEMBL8981 204977 34 None 66 2 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm980504w
9871348 202320 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 520 8 1 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4nsnc4c3)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(97)10151-2
CHEMBL69741 202320 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 520 8 1 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4nsnc4c3)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(97)10151-2
9809919 202694 0 None - 2 Human 9.5 pIC50 = 9.5 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL72037 202694 0 None - 2 Human 9.5 pIC50 = 9.5 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44284481 211967 0 None -4 5 Human 9.5 pIC50 = 9.5 Binding
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00400-9
CHEMBL437472 211967 0 None -4 5 Human 9.5 pIC50 = 9.5 Binding
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00400-9
159594 518 38 None -1 3 Rat 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm031041j
3487 518 38 None -1 3 Rat 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm031041j
CHEMBL9194 518 38 None -1 3 Rat 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm031041j
DB06199 518 38 None -1 3 Rat 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm031041j
159594 518 38 None 1 3 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm030528p
3487 518 38 None 1 3 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm030528p
CHEMBL9194 518 38 None 1 3 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm030528p
DB06199 518 38 None 1 3 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm030528p
159594 518 38 None -1 3 Rat 9.5 pIC50 = 9.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
3487 518 38 None -1 3 Rat 9.5 pIC50 = 9.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
CHEMBL9194 518 38 None -1 3 Rat 9.5 pIC50 = 9.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
DB06199 518 38 None -1 3 Rat 9.5 pIC50 = 9.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
11144344 201314 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 424 8 1 5 5.8 CCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63267 201314 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 424 8 1 5 5.8 CCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44334150 4451 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 445 6 1 5 5.0 COc1ccc([C@@H]2c3nc(CC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL102314 4451 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 445 6 1 5 5.0 COc1ccc([C@@H]2c3nc(CC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
9852318 9508 5 None - 2 Rat 9.5 pIC50 = 9.5 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL112624 9508 5 None - 2 Rat 9.5 pIC50 = 9.5 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL1627022 9508 5 None - 2 Rat 9.5 pIC50 = 9.5 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
11102201 201523 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 438 9 1 6 5.1 C=CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL64447 201523 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 438 9 1 6 5.1 C=CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44266903 14402 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL10862 14402 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL1204672 14402 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
9960931 107522 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 635 12 1 12 4.1 CCOC(=O)CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
CHEMBL319452 107522 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 635 12 1 12 4.1 CCOC(=O)CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
159594 518 38 None -1 3 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity against Endothelin A receptor in MMQ cells in ratBinding affinity against Endothelin A receptor in MMQ cells in rat
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
3487 518 38 None -1 3 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity against Endothelin A receptor in MMQ cells in ratBinding affinity against Endothelin A receptor in MMQ cells in rat
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
CHEMBL9194 518 38 None -1 3 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity against Endothelin A receptor in MMQ cells in ratBinding affinity against Endothelin A receptor in MMQ cells in rat
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
DB06199 518 38 None -1 3 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity against Endothelin A receptor in MMQ cells in ratBinding affinity against Endothelin A receptor in MMQ cells in rat
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
9914310 204907 3 None - 2 Rat 9.4 pIC50 = 9.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8923 204907 3 None - 2 Rat 9.4 pIC50 = 9.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
9870830 204977 34 None 66 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL8981 204977 34 None 66 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/S0960-894X(97)00002-4
11017436 9841 0 None - 0 Pig 9.4 pIC50 = 9.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 597 12 1 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(SC)cn1 10.1021/jm0102304
CHEMBL114660 9841 0 None - 0 Pig 9.4 pIC50 = 9.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 597 12 1 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(SC)cn1 10.1021/jm0102304
44333913 5017 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 431 6 1 5 4.8 CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL105591 5017 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 431 6 1 5 4.8 CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
9870959 8814 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
CHEMBL109778 8814 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
9809526 14675 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 614 12 2 11 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL1207463 14675 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 614 12 2 11 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL408055 14675 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 614 12 2 11 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1 10.1021/jm980504w
44284481 211967 0 None -4 5 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human ETA receptorInhibition of human ETA receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm701575k
CHEMBL437472 211967 0 None -4 5 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human ETA receptorInhibition of human ETA receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm701575k
10208674 101370 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 529 7 2 7 5.6 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)c2ccccc2)c1 10.1021/jm030528p
CHEMBL300547 101370 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 529 7 2 7 5.6 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)c2ccccc2)c1 10.1021/jm030528p
10603409 110102 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL325581 110102 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
9852318 9508 5 None 2691 2 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/acs.jmedchem.5b01781
CHEMBL112624 9508 5 None 2691 2 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/acs.jmedchem.5b01781
CHEMBL1627022 9508 5 None 2691 2 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/acs.jmedchem.5b01781
44332735 172123 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 649 13 1 12 4.5 CCOC(=O)CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
CHEMBL450337 172123 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 649 13 1 12 4.5 CCOC(=O)CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
159594 518 38 None -1 3 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm960077r
3487 518 38 None -1 3 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm960077r
CHEMBL9194 518 38 None -1 3 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm960077r
DB06199 518 38 None -1 3 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm960077r
9852318 9508 5 None 2691 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL112624 9508 5 None 2691 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL1627022 9508 5 None 2691 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
71462245 81240 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 588 13 2 10 3.6 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cc(OC)ccc1Cl 10.1021/jm3009103
CHEMBL2163692 81240 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 588 13 2 10 3.6 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cc(OC)ccc1Cl 10.1021/jm3009103
44386169 130854 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 690 12 2 14 3.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
CHEMBL368996 130854 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 690 12 2 14 3.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
11122784 162360 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 8 1 6 4.9 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL417413 162360 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 8 1 6 4.9 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44339655 9003 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL109926 9003 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
44284196 100044 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 504 9 2 7 5.4 CCCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL291247 100044 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 504 9 2 7 5.4 CCCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
10364227 201102 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm031041j
CHEMBL62264 201102 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm031041j
10364227 201102 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL62264 201102 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
9806559 9046 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O 10.1021/jm980217s
CHEMBL110053 9046 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O 10.1021/jm980217s
11827880 10115 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 565 10 1 9 5.5 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
CHEMBL116046 10115 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 565 10 1 9 5.5 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
CHEMBL177979 10115 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 565 10 1 9 5.5 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
CHEMBL1790962 207157 0 None - 1 Pig 9.4 pIC50 = 9.4 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
10303555 162817 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 574 15 1 7 4.9 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL419383 162817 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 574 15 1 7 4.9 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
10578320 96848 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 538 12 1 6 5.2 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CCC(C)C)CCC(C)C)cc1 10.1021/jm9505369
CHEMBL269141 96848 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 538 12 1 6 5.2 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CCC(C)C)CCC(C)C)cc1 10.1021/jm9505369
10182624 99079 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 453 6 2 6 4.9 CCc1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm000349x
CHEMBL283582 99079 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 453 6 2 6 4.9 CCc1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm000349x
9870830 204977 34 None - 2 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(97)10151-2
CHEMBL8981 204977 34 None - 2 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(97)10151-2
9825494 200914 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity at human Endothelin A receptorBinding affinity at human Endothelin A receptor
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL61211 200914 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity at human Endothelin A receptorBinding affinity at human Endothelin A receptor
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
44380648 119992 0 None - 0 Pig 9.4 pIC50 = 9.4 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 727 12 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCN(C)CC2)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
CHEMBL354528 119992 0 None - 0 Pig 9.4 pIC50 = 9.4 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 727 12 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCN(C)CC2)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
10210629 8661 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL109644 8661 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10167052 109138 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 578 13 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCC(C)C 10.1021/jm970101g
CHEMBL322297 109138 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 578 13 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCC(C)C 10.1021/jm970101g
44265870 205827 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 524 12 1 6 5.1 CCCCN(CCCC)C(=O)C(C)N1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9488 205827 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 524 12 1 6 5.1 CCCCN(CCCC)C(=O)C(C)N1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
10391487 9555 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL112832 9555 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
10983045 201208 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 440 9 1 6 5.3 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL62762 201208 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 440 9 1 6 5.3 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
11050177 10147 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 585 10 1 9 6.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1 10.1021/jm0102304
CHEMBL116108 10147 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 585 10 1 9 6.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1 10.1021/jm0102304
CHEMBL175501 10147 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 585 10 1 9 6.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1 10.1021/jm0102304
9915028 9306 12 None 28183 2 Human 9.3 pIC50 = 9.3 Binding
Inhibitory activity against human endothelin A receptorInhibitory activity against human endothelin A receptor
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm010237l
CHEMBL111612 9306 12 None 28183 2 Human 9.3 pIC50 = 9.3 Binding
Inhibitory activity against human endothelin A receptorInhibitory activity against human endothelin A receptor
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm010237l
CHEMBL4761843 9306 12 None 28183 2 Human 9.3 pIC50 = 9.3 Binding
Inhibitory activity against human endothelin A receptorInhibitory activity against human endothelin A receptor
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm010237l
10391487 9555 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm031041j
CHEMBL112832 9555 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm031041j
10840068 60023 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL174573 60023 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm031041j
44387124 130356 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 524 13 1 6 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](CC(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm031041j
CHEMBL368558 130356 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 524 13 1 6 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](CC(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm031041j
10530409 5615 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 536 9 1 10 3.9 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL10781 5615 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 536 9 1 10 3.9 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
10815823 9689 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 520 8 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C 10.1021/jm9606507
CHEMBL11369 9689 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 520 8 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C 10.1021/jm9606507
15411009 106693 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 691 14 1 12 5.6 CCOC(=O)C(CC(C)C)NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
CHEMBL316523 106693 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 691 14 1 12 5.6 CCOC(=O)C(CC(C)C)NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
10391487 9555 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL112832 9555 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
16004692 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
4809 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
7352 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
CHEMBL2103873 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
DB08932 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
157574 77971 9 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 517 4 1 5 5.0 CCc1cc(C2=C(C(=O)O)N(c3ccccc3C(F)(F)F)S(=O)(=O)c3ccccc32)cc2c1OCO2 10.1016/j.bmcl.2016.06.014
CHEMBL2110610 77971 9 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 517 4 1 5 5.0 CCc1cc(C2=C(C(=O)O)N(c3ccccc3C(F)(F)F)S(=O)(=O)c3ccccc32)cc2c1OCO2 10.1016/j.bmcl.2016.06.014
21041283 172566 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 552 13 2 9 3.2 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4521348 172566 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 552 13 2 9 3.2 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
155544917 172832 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 540 13 2 10 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL4528516 172832 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 540 13 2 10 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1 10.1016/j.bmcl.2016.06.014
16004692 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
4809 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
7352 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
CHEMBL2103873 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
DB08932 2411 85 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
44279554 98854 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 512 11 2 7 3.8 COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL282187 98854 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 512 11 2 7 3.8 COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
11754394 108128 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 468 8 2 6 3.8 CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL32066 108128 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 468 8 2 6 3.8 CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
9933950 201129 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL62395 201129 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
10553384 109167 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1 10.1021/jm980217s
CHEMBL322537 109167 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1 10.1021/jm980217s
44333721 167219 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 447 7 1 6 4.3 CCOCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL430506 167219 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 447 7 1 6 4.3 CCOCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
9916235 9248 1 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL111277 9248 1 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10994374 201716 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 7 1 6 5.4 COc1ccc(CC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL65619 201716 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 7 1 6 5.4 COc1ccc(CC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
10651146 108364 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 596 12 1 8 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL321035 108364 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 596 12 1 8 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(OC)cc1 10.1021/jm970101g
10982740 201683 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 422 5 1 5 5.4 CC(C)Oc1ccc2c(c1)C(C1CCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL65353 201683 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 422 5 1 5 5.4 CC(C)Oc1ccc2c(c1)C(C1CCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10187997 109471 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL323464 109471 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10651488 162815 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
CHEMBL419367 162815 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
9915510 84717 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
CHEMBL22513 84717 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
9915510 84717 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1007/s00044-004-0021-y
CHEMBL22513 84717 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1007/s00044-004-0021-y
44334097 109567 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 447 7 2 6 3.7 COc1ccc([C@@H]2c3nc(CCCO)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL323561 109567 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 447 7 2 6 3.7 COc1ccc([C@@H]2c3nc(CCCO)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
10719598 205252 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9139 205252 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
9915028 9306 12 None - 2 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL111612 9306 12 None - 2 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL4761843 9306 12 None - 2 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
10886132 9701 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 549 10 1 9 4.8 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
CHEMBL113757 9701 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 549 10 1 9 4.8 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
CHEMBL368796 9701 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 549 10 1 9 4.8 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
10744973 205535 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 538 14 1 6 5.5 CCCCCN(CCCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9313 205535 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 538 14 1 6 5.5 CCCCCN(CCCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10209779 162867 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 560 14 1 7 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL419749 162867 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 560 14 1 7 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
11015826 201828 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 450 6 1 5 6.1 CC(C)Oc1ccc2c(c1)C(CC1CCCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL66426 201828 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 450 6 1 5 6.1 CC(C)Oc1ccc2c(c1)C(CC1CCCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
9915028 9306 12 None 28183 2 Human 9.2 pIC50 = 9.2 Binding
Affinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRAAffinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRA
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC nan
CHEMBL111612 9306 12 None 28183 2 Human 9.2 pIC50 = 9.2 Binding
Affinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRAAffinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRA
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC nan
CHEMBL4761843 9306 12 None 28183 2 Human 9.2 pIC50 = 9.2 Binding
Affinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRAAffinity On-target Cellular interaction (Endothelin-1-evoked phosphatidylinositol hydrolysis in MMQ cells) EUB0000348aPTSA EDNRA
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC nan
10346184 9091 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL110366 9091 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
15411005 4677 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 677 13 1 12 5.2 CCOC(=O)C(NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1)C(C)C 10.1016/S0960-894X(97)00002-4
CHEMBL103846 4677 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 677 13 1 12 5.2 CCOC(=O)C(NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1)C(C)C 10.1016/S0960-894X(97)00002-4
10346184 9091 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL110366 9091 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL2373291 208619 0 None - 1 Pig 9.2 pIC50 = 9.2 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
10579303 9325 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 590 16 1 8 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCOC)cc1 10.1021/jm970101g
CHEMBL111712 9325 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 590 16 1 8 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCOC)cc1 10.1021/jm970101g
11015645 201488 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 438 9 1 5 6.1 CCCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL64282 201488 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 438 9 1 5 6.1 CCCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10938122 162444 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 396 5 1 5 4.8 CC(C)Oc1ccc2c(c1)C(C(C)C)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL417555 162444 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 396 5 1 5 4.8 CC(C)Oc1ccc2c(c1)C(C(C)C)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10503921 100993 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1noc(C)c1Cl)OCO2 10.1021/jm9700068
CHEMBL297783 100993 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1noc(C)c1Cl)OCO2 10.1021/jm9700068
10717923 98227 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL277595 98227 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00132-7
44279141 106527 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 498 10 3 7 3.2 COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(=O)NCCO)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL31544 106527 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 498 10 3 7 3.2 COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(=O)NCCO)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
10552883 109503 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 484 13 1 5 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C1CC1 10.1021/jm980217s
CHEMBL323485 109503 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 484 13 1 5 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C1CC1 10.1021/jm980217s
10974047 9411 0 None - 0 Pig 9.2 pIC50 = 9.2 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 601 11 1 10 4.3 COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1OC 10.1021/jm0102304
CHEMBL112162 9411 0 None - 0 Pig 9.2 pIC50 = 9.2 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 601 11 1 10 4.3 COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1OC 10.1021/jm0102304
10745942 9206 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 588 13 1 8 4.3 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc2c(c1)OCCO2 10.1021/jm970101g
CHEMBL111010 9206 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 588 13 1 8 4.3 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc2c(c1)OCCO2 10.1021/jm970101g
11080933 201712 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 454 10 1 6 5.7 CCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL65599 201712 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 454 10 1 6 5.7 CCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10166223 201014 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 552 7 2 7 5.5 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)CC(C)(C)C)c1 10.1021/jm030528p
CHEMBL61711 201014 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 552 7 2 7 5.5 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)CC(C)(C)C)c1 10.1021/jm030528p
10076527 14431 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 485 7 2 6 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3ccccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1204990 14431 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 485 7 2 6 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3ccccc31)OCO2 10.1016/j.bmcl.2010.08.074
10720982 127282 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1 10.1021/jm031041j
CHEMBL121647 127282 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1 10.1021/jm031041j
CHEMBL366441 127282 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1 10.1021/jm031041j
71462320 81578 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL2165332 81578 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
10720982 127282 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1 10.1021/jm990171i
CHEMBL121647 127282 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1 10.1021/jm990171i
CHEMBL366441 127282 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1 10.1021/jm990171i
10649266 9526 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL112685 9526 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
11505449 170908 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 616 12 3 9 2.6 O=C(O)CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4463633 170908 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 616 12 3 9 2.6 O=C(O)CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
58688005 174378 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 540 11 2 9 3.1 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4565926 174378 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 540 11 2 9 3.1 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
71462320 81578 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL2165332 81578 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
10746431 101823 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 619 12 1 11 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN3CCOCC3)c2)cc1 10.1021/jm980504w
CHEMBL303484 101823 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 619 12 1 11 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN3CCOCC3)c2)cc1 10.1021/jm980504w
9809919 202694 0 None - 2 Human 9.2 pIC50 = 9.2 Binding
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL72037 202694 0 None - 2 Human 9.2 pIC50 = 9.2 Binding
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL2373292 208620 0 None - 1 Pig 9.2 pIC50 = 9.2 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
9870959 8814 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
CHEMBL109778 8814 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
10916597 201615 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL64832 201615 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44284184 139457 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 490 8 2 7 5.0 CCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL38000 139457 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 490 8 2 7 5.0 CCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL427748 211614 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
11827489 116472 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 524 12 1 4 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1 10.1021/jm010237l
CHEMBL338754 116472 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 524 12 1 4 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1 10.1021/jm010237l
10984671 9367 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 571 10 1 9 4.3 COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1 10.1021/jm0102304
CHEMBL111934 9367 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 571 10 1 9 4.3 COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1 10.1021/jm0102304
10648006 161105 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 468 6 1 6 4.7 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1021/jm9700068
CHEMBL413093 161105 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 468 6 1 6 4.7 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1021/jm9700068
10648135 9237 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 472 13 1 5 4.7 C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm031041j
CHEMBL111218 9237 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 472 13 1 5 4.7 C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm031041j
10209320 9180 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 546 12 1 7 4.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC(C)C 10.1021/jm970101g
CHEMBL110899 9180 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 546 12 1 7 4.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC(C)C 10.1021/jm970101g
11038320 18670 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 492 11 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1 10.1021/jm010237l
CHEMBL128240 18670 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 492 11 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1 10.1021/jm010237l
44340049 109829 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 500 13 1 5 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL323951 109829 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 500 13 1 5 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
10552413 110166 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 472 13 1 5 4.7 C/C=C\CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL325935 110166 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 472 13 1 5 4.7 C/C=C\CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
44266851 14401 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 550 11 1 9 4.7 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C 10.1021/jm9606507
CHEMBL10847 14401 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 550 11 1 9 4.7 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C 10.1021/jm9606507
CHEMBL1204671 14401 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 550 11 1 9 4.7 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C 10.1021/jm9606507
44279316 106849 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 518 8 2 6 4.0 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL31763 106849 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 518 8 2 6 4.0 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
137649592 156856 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 567 10 2 9 4.6 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4078537 156856 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 567 10 2 9 4.6 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
15411003 108220 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 589 11 1 10 4.8 C=CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
CHEMBL320839 108220 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 589 11 1 10 4.8 C=CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
10673644 9674 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113611 9674 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
177236 1293 39 None 2 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/s0960-894x(01)00660-6
3508 1293 39 None 2 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/s0960-894x(01)00660-6
CHEMBL23261 1293 39 None 2 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/s0960-894x(01)00660-6
DB04883 1293 39 None 2 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/s0960-894x(01)00660-6
71462322 81584 6 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 572 10 2 8 3.2 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2165338 81584 6 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 572 10 2 8 3.2 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
44284199 99635 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 552 9 2 7 6.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCc2ccccc2)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287517 99635 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 552 9 2 7 6.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCc2ccccc2)c1 10.1016/j.bmcl.2004.01.008
10993320 201282 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 412 6 1 6 4.6 CC(C)OC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63067 201282 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 412 6 1 6 4.6 CC(C)OC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10097589 204548 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCC(C(=O)O)CC1 10.1016/s0960-894x(00)00513-8
CHEMBL86965 204548 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCC(C(=O)O)CC1 10.1016/s0960-894x(00)00513-8
10792319 205494 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 530 10 1 6 5.1 CCCCN(C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm9505369
CHEMBL9283 205494 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 530 10 1 6 5.1 CCCCN(C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm9505369
10648937 205565 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9334 205565 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10673644 9674 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL113611 9674 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
10814655 205856 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 482 10 1 6 3.9 CCCCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9502 205856 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 482 10 1 6 3.9 CCCCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44339714 110807 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 500 14 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC/C=C(/C)CC 10.1021/jm980217s
CHEMBL326685 110807 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 500 14 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC/C=C(/C)CC 10.1021/jm980217s
10984617 9898 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 565 11 1 10 4.9 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(C)cn2)c1 10.1021/jm0102304
CHEMBL114933 9898 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 565 11 1 10 4.9 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(C)cn2)c1 10.1021/jm0102304
44284183 139032 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 518 9 2 7 5.7 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCC(C)C)c1 10.1016/j.bmcl.2004.01.008
CHEMBL37973 139032 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL 518 9 2 7 5.7 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCC(C)C)c1 10.1016/j.bmcl.2004.01.008
11027946 18710 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 540 12 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1 10.1021/jm010237l
CHEMBL128479 18710 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 540 12 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1 10.1021/jm010237l
11006213 168692 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 557 10 1 10 5.3 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cccs2)nc1 10.1021/jm0102304
CHEMBL441277 168692 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 557 10 1 10 5.3 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cccs2)nc1 10.1021/jm0102304
10602743 7063 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 550 9 1 10 4.2 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C 10.1021/jm9606507
CHEMBL10854 7063 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 550 9 1 10 4.2 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C 10.1021/jm9606507
10983992 19246 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
CHEMBL129740 19246 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
44333598 108690 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 447 7 1 6 4.6 CCCOc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL321520 108690 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 447 7 1 6 4.6 CCCOc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
11037806 201127 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 456 10 2 7 4.3 CC(C)Oc1ccc2c(c1)C(OCCCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL62376 201127 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 456 10 2 7 4.3 CC(C)Oc1ccc2c(c1)C(OCCCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10788494 170046 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9700068
CHEMBL445101 170046 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9700068
10768294 14404 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 520 10 1 8 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C 10.1021/jm9606507
CHEMBL10922 14404 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 520 10 1 8 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C 10.1021/jm9606507
CHEMBL1204674 14404 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 520 10 1 8 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C 10.1021/jm9606507
10625694 11326 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 516 9 2 6 4.5 CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL1180344 11326 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 516 9 2 6 4.5 CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL123107 11326 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 516 9 2 6 4.5 CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
9868379 100303 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1 10.1021/jm010382z
CHEMBL293012 100303 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1 10.1021/jm010382z
44332842 109220 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 703 11 1 10 7.5 COc1ccc(C2(OC(=O)N[C@@H](C)c3cccc4ccccc34)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL322920 109220 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 703 11 1 10 7.5 COc1ccc(C2(OC(=O)N[C@@H](C)c3cccc4ccccc34)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/S0960-894X(97)00002-4
44314904 102659 0 None - 0 Pig 9.0 pIC50 = 9 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 585 12 5 5 3.6 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL307936 102659 0 None - 0 Pig 9.0 pIC50 = 9 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 585 12 5 5 3.6 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
10649321 110444 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL326191 110444 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
3951 388 82 None -1 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
4337 388 82 None -1 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
6918493 388 82 None -1 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
CHEMBL1111 388 82 None -1 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
DB06403 388 82 None -1 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
9868379 100303 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1 10.1016/j.bmcl.2016.06.014
CHEMBL293012 100303 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1 10.1016/j.bmcl.2016.06.014
155519384 169839 0 None - 1 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 674 12 1 13 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL4448273 169839 0 None - 1 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 674 12 1 13 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1 10.1016/j.bmcl.2016.06.014
155551580 173411 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 526 12 2 10 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL4542394 173411 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 526 12 2 10 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1 10.1016/j.bmcl.2016.06.014
10146305 173689 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 656 14 2 13 4.2 COc1ccccc1Oc1c(NS(=O)(=O)CCc2cccs2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL4549357 173689 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 656 14 2 13 4.2 COc1ccccc1Oc1c(NS(=O)(=O)CCc2cccs2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
44439102 89854 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.2 CN(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1ccno1)C(=O)CC(C)(C)C 10.1016/j.bmcl.2006.10.009
CHEMBL238539 89854 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.2 CN(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1ccno1)C(=O)CC(C)(C)C 10.1016/j.bmcl.2006.10.009
71460621 81575 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 602 13 2 10 3.7 COc1cccc(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm3009103
CHEMBL2165329 81575 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 602 13 2 10 3.7 COc1cccc(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm3009103
44295173 14449 0 None - 0 Rat 9.0 pIC50 = 9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 554 10 1 9 5.3 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl 10.1016/s0960-894x(98)00301-1
CHEMBL1205090 14449 0 None - 0 Rat 9.0 pIC50 = 9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 554 10 1 9 5.3 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl 10.1016/s0960-894x(98)00301-1
CHEMBL51234 14449 0 None - 0 Rat 9.0 pIC50 = 9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 554 10 1 9 5.3 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl 10.1016/s0960-894x(98)00301-1
44279398 99414 0 None - 0 Human 9.0 pIC50 = 9 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 454 8 2 6 3.6 COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL285976 99414 0 None - 0 Human 9.0 pIC50 = 9 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 454 8 2 6 3.6 COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
44279294 99421 0 None - 0 Human 9.0 pIC50 = 9 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 546 8 1 6 4.6 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(=O)N(C)C)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL286014 99421 0 None - 0 Human 9.0 pIC50 = 9 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 546 8 1 6 4.6 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(=O)N(C)C)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
10897248 9403 0 None - 0 Pig 9.0 pIC50 = 9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 591 9 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc4ccccc4c3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL112134 9403 0 None - 0 Pig 9.0 pIC50 = 9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 591 9 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc4ccccc4c3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
11136124 10257 0 None - 0 Pig 9.0 pIC50 = 9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 667 9 1 8 4.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(I)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL116220 10257 0 None - 0 Pig 9.0 pIC50 = 9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 667 9 1 8 4.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(I)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
10211781 129206 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
CHEMBL367453 129206 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
10146640 205810 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 689 12 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
CHEMBL94786 205810 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 689 12 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
10555191 202086 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 577 12 1 10 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN(C)C)c2)cc1 10.1021/jm980504w
CHEMBL68269 202086 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 577 12 1 10 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN(C)C)c2)cc1 10.1021/jm980504w
CHEMBL1790519 207140 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N(C)[C@@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC 10.1021/jm970161m
44311346 102675 0 None - 1 Human 9.0 pIC50 = 9 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 681 13 2 13 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCSCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL308088 102675 0 None - 1 Human 9.0 pIC50 = 9 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 681 13 2 13 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCSCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44340049 109829 0 None - 0 Human 9.0 pIC50 = 9 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 500 13 1 5 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL323951 109829 0 None - 0 Human 9.0 pIC50 = 9 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 500 13 1 5 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
44339662 9744 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 527 13 1 7 4.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1nc(C)c(C)o1 10.1021/jm980217s
CHEMBL114074 9744 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 527 13 1 7 4.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1nc(C)c(C)o1 10.1021/jm980217s
44351961 18633 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 522 13 1 5 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCC)cc1 10.1021/jm010237l
CHEMBL128061 18633 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 522 13 1 5 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCC)cc1 10.1021/jm010237l
10553384 109167 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1 10.1021/jm980217s
CHEMBL322537 109167 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1 10.1021/jm980217s
9909467 203790 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 409 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80782 203790 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 409 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Br 10.1016/0960-894X(96)00441-6
9827093 172842 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 494 9 2 7 5.1 CCCc1nc(SC2CCC(CC(=O)O)CC2)c(C(=O)O)n1Cc1cc2c(cc1Cl)OCO2 10.1016/j.bmcl.2016.06.014
CHEMBL4528664 172842 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 494 9 2 7 5.1 CCCc1nc(SC2CCC(CC(=O)O)CC2)c(C(=O)O)n1Cc1cc2c(cc1Cl)OCO2 10.1016/j.bmcl.2016.06.014
10347080 84789 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
CHEMBL22562 84789 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
10347080 84789 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1007/s00044-004-0021-y
CHEMBL22562 84789 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1007/s00044-004-0021-y
71449713 81242 21 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 585 11 1 8 4.5 CCCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2163694 81242 21 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 585 11 1 8 4.5 CCCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
71458719 81252 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 647 15 1 13 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(SC)cn1 10.1021/jm3009103
CHEMBL2163704 81252 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 647 15 1 13 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(SC)cn1 10.1021/jm3009103
17885918 105480 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccsc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL313044 105480 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccsc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
9846994 105496 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL313153 105496 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
44380976 165063 0 None - 0 Pig 9.0 pIC50 = 9.0 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 639 10 1 8 6.7 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(C(C)C)nc2OCCOc2ncc(Br)cn2)cc1 10.1016/s0960-894x(01)00682-5
CHEMBL424358 165063 0 None - 0 Pig 9.0 pIC50 = 9.0 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 639 10 1 8 6.7 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(C(C)C)nc2OCCOc2ncc(Br)cn2)cc1 10.1016/s0960-894x(01)00682-5
10505755 14400 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 506 10 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL10832 14400 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 506 10 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL1204670 14400 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 506 10 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
9870830 204977 34 None 66 2 Human 9.0 pIC50 = 9.0 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL8981 204977 34 None 66 2 Human 9.0 pIC50 = 9.0 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
10142669 9338 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 518 11 1 7 3.3 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC 10.1021/jm970101g
CHEMBL111769 9338 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 518 11 1 7 3.3 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC 10.1021/jm970101g
137637038 155388 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 581 11 2 9 5.0 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4061110 155388 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 581 11 2 9 5.0 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
10649321 110444 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL326191 110444 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
10576427 5283 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 473 6 2 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(NC(C)=O)cc2)cc1 10.1021/jm9606507
CHEMBL10697 5283 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 473 6 2 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(NC(C)=O)cc2)cc1 10.1021/jm9606507
21041324 81238 2 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 542 11 2 8 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1021/jm3009103
CHEMBL2163690 81238 2 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 542 11 2 8 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1021/jm3009103
11093167 9943 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 593 11 1 9 6.3 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C(C)C)cc2)nc1 10.1021/jm0102304
CHEMBL115230 9943 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 593 11 1 9 6.3 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C(C)C)cc2)nc1 10.1021/jm0102304
11813644 109875 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccncn2)c1 10.1021/jm0102304
CHEMBL324246 109875 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccncn2)c1 10.1021/jm0102304
CHEMBL414165 211357 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory effect against Human ET-A receptorInhibitory effect against Human ET-A receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](c2cccs2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10719598 205252 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9139 205252 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44279296 110128 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 532 8 2 6 4.3 CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL32572 110128 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 532 8 2 6 4.3 CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
10206812 197944 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 492 6 2 8 5.0 Cc1cc(-c2ncco2)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL59288 197944 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 492 6 2 8 5.0 Cc1cc(-c2ncco2)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
11102609 167994 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 462 6 1 6 5.2 COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm031041j
CHEMBL435773 167994 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 462 6 1 6 5.2 COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm031041j
10603546 109945 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 592 15 1 7 5.0 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCC)c(F)c1 10.1021/jm970101g
CHEMBL324639 109945 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 592 15 1 7 5.0 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCC)c(F)c1 10.1021/jm970101g
11102609 167994 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 462 6 1 6 5.2 COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm010382z
CHEMBL435773 167994 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 462 6 1 6 5.2 COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm010382z
10576910 108039 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 486 13 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C(C)C 10.1021/jm980217s
CHEMBL320124 108039 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 486 13 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C(C)C 10.1021/jm980217s
10278777 167558 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL432974 167558 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
10767586 9662 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 496 13 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113529 9662 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 496 13 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
58688008 174720 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 496 11 2 9 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4573273 174720 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 496 11 2 9 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
23670447 2968 2 None - 2 Rat 8.9 pIC50 = 8.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1016/s0960-894x(98)00301-1
999 2968 2 None - 2 Rat 8.9 pIC50 = 8.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1016/s0960-894x(98)00301-1
CHEMBL1204799 2968 2 None - 2 Rat 8.9 pIC50 = 8.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1016/s0960-894x(98)00301-1
CHEMBL25438 2968 2 None - 2 Rat 8.9 pIC50 = 8.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1016/s0960-894x(98)00301-1
44320480 105465 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 442 6 1 6 5.4 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccco2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL312979 105465 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 442 6 1 6 5.4 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccco2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
17885920 204705 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCC(C(=O)O)C1 10.1016/s0960-894x(00)00513-8
CHEMBL88011 204705 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCC(C(=O)O)C1 10.1016/s0960-894x(00)00513-8
44291775 100685 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 506 6 1 10 4.1 CC#N.Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm9700068
CHEMBL295557 100685 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 506 6 1 10 4.1 CC#N.Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm9700068
10280278 100363 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 535 7 2 7 6.1 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CCCCC2)c1 10.1021/jm030528p
CHEMBL293421 100363 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 535 7 2 7 6.1 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CCCCC2)c1 10.1021/jm030528p
11071347 117290 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 516 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1 10.1021/jm010237l
CHEMBL340190 117290 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 516 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1 10.1021/jm010237l
10745564 6133 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 566 11 1 7 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccccc1 10.1021/jm970101g
CHEMBL108142 6133 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 566 11 1 7 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccccc1 10.1021/jm970101g
11125029 9929 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 627 11 2 9 4.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C(=O)O)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL115147 9929 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 627 11 2 9 4.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C(=O)O)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
15453177 203800 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80857 203800 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
10790757 96752 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL268480 96752 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2)cc1 10.1021/jm9606507
10554273 9305 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 532 13 1 7 4.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C1OCCO1 10.1021/jm980217s
CHEMBL111611 9305 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 532 13 1 7 4.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C1OCCO1 10.1021/jm980217s
8260 527 46 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
9912992 527 46 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
CHEMBL3989834 527 46 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
18630945 170415 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 507 9 1 9 4.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL4456288 170415 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 507 9 1 9 4.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OC 10.1016/j.bmcl.2016.06.014
155542285 172498 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 522 14 2 11 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1cccc(OC)c1 10.1016/j.bmcl.2016.06.014
CHEMBL4519822 172498 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 522 14 2 11 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1cccc(OC)c1 10.1016/j.bmcl.2016.06.014
11477084 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
216235 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
3548 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
3950 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
CHEMBL282724 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
DB06268 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
22467234 84915 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 534 7 1 8 4.1 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(C)=O)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261599 84915 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 534 7 1 8 4.1 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(C)=O)ccc12 10.1007/s00044-004-0021-y
21041372 81274 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 687 14 2 12 3.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(N2CCOCC2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163725 81274 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 687 14 2 12 3.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(N2CCOCC2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
21041370 81576 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 636 13 2 10 4.4 COc1ccc(Cl)c(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm3009103
CHEMBL2165330 81576 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 636 13 2 10 4.4 COc1ccc(Cl)c(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm3009103
21979593 81579 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 590 11 2 8 4.3 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1021/jm3009103
CHEMBL2165333 81579 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 590 11 2 8 4.3 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1021/jm3009103
44295177 14597 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 534 10 1 9 5.0 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C 10.1016/s0960-894x(98)00301-1
CHEMBL1206680 14597 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 534 10 1 9 5.0 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C 10.1016/s0960-894x(98)00301-1
CHEMBL295483 14597 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 534 10 1 9 5.0 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C 10.1016/s0960-894x(98)00301-1
104865 697 94 None -1 4 Rat 8.9 pIC50 = 8.9 Binding
In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
3494 697 94 None -1 4 Rat 8.9 pIC50 = 8.9 Binding
In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
392 697 94 None -1 4 Rat 8.9 pIC50 = 8.9 Binding
In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
CHEMBL957 697 94 None -1 4 Rat 8.9 pIC50 = 8.9 Binding
In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
DB00559 697 94 None -1 4 Rat 8.9 pIC50 = 8.9 Binding
In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
10952199 9913 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 609 9 1 8 5.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL115017 9913 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 609 9 1 8 5.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
11477084 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
216235 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
3548 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
3950 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
CHEMBL282724 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
DB06268 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
11477084 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
216235 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
3548 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
3950 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
CHEMBL282724 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
DB06268 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
11477084 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm000349x
216235 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm000349x
3548 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm000349x
3950 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm000349x
CHEMBL282724 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm000349x
DB06268 3540 46 None 1 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm000349x
42630655 18208 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271586 18208 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
11409462 197001 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 501 6 2 6 6.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ccccc2)c1 10.1021/jm030528p
CHEMBL58058 197001 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 501 6 2 6 6.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ccccc2)c1 10.1021/jm030528p
10505771 162792 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL419211 162792 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
11026025 201187 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 412 7 1 6 4.6 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL62669 201187 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 412 7 1 6 4.6 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10649122 9632 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 502 12 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113400 9632 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 502 12 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10505771 162792 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL419211 162792 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
21041297 169029 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 510 12 2 9 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4436531 169029 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 510 12 2 9 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
71453357 81256 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 707 12 1 12 5.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163708 81256 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 707 12 1 12 5.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
159594 518 38 None -1 3 Rat 8.8 pIC50 = 8.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1016/s0960-894x(98)00301-1
3487 518 38 None -1 3 Rat 8.8 pIC50 = 8.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1016/s0960-894x(98)00301-1
CHEMBL9194 518 38 None -1 3 Rat 8.8 pIC50 = 8.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1016/s0960-894x(98)00301-1
DB06199 518 38 None -1 3 Rat 8.8 pIC50 = 8.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1016/s0960-894x(98)00301-1
44279303 106599 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 576 11 2 7 4.3 COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL31592 106599 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 576 11 2 7 4.3 COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
10302092 110836 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 532 12 1 7 3.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC 10.1021/jm970101g
CHEMBL326861 110836 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 532 12 1 7 3.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC 10.1021/jm970101g
10768903 12013 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 544 11 2 6 5.3 CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL1184133 12013 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 544 11 2 6 5.3 CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL334076 12013 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 544 11 2 6 5.3 CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
11733231 201147 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)c1 10.1021/jm010382z
CHEMBL62465 201147 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)c1 10.1021/jm010382z
9872534 175439 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 521 11 2 10 3.5 COc1ccccc1Oc1c(NS(=O)(=O)/C=C/c2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4590018 175439 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 521 11 2 10 3.5 COc1ccccc1Oc1c(NS(=O)(=O)/C=C/c2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1016/j.bmcl.2016.06.014
44439103 91505 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 859 27 2 14 5.3 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL241460 91505 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 859 27 2 14 5.3 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
67952994 81580 11 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 634 11 2 8 4.4 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2165334 81580 11 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 634 11 2 8 4.4 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
19689505 58591 0 None - 0 Pig 8.8 pIC50 = 8.8 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 639 11 1 8 6.5 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(-c2ccc(C)cc2)c(OCCOc2ncc(Br)cn2)n1 10.1016/s0960-894x(01)00682-5
CHEMBL168904 58591 0 None - 0 Pig 8.8 pIC50 = 8.8 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 639 11 1 8 6.5 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(-c2ccc(C)cc2)c(OCCOc2ncc(Br)cn2)n1 10.1016/s0960-894x(01)00682-5
44334065 167248 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 429 5 1 5 4.7 COc1ccc([C@@H]2c3nc(C4CC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL430695 167248 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 429 5 1 5 4.7 COc1ccc([C@@H]2c3nc(C4CC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
10719367 97765 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)cc(OC)c2)cc1 10.1021/jm9606507
CHEMBL274359 97765 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)cc(OC)c2)cc1 10.1021/jm9606507
12286 933 30 None 1348 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
6433095 933 30 None 1348 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL109648 933 30 None 1348 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
DB06677 933 30 None 1348 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
22467237 84905 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 549 8 3 8 2.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(CC(=O)O)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1007/s00044-004-0021-y
CHEMBL2261357 84905 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 549 8 3 8 2.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(CC(=O)O)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1007/s00044-004-0021-y
71455063 81269 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 646 15 2 12 3.8 CCCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163720 81269 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 646 15 2 12 3.8 CCCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
21041267 81583 10 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 558 9 2 8 2.8 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2165337 81583 10 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 558 9 2 8 2.8 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
10813261 60091 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 8 1 6 4.4 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL175129 60091 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 8 1 6 4.4 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
9955200 9227 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL11115 9227 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
10601668 97981 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)cc2OC)cc1 10.1021/jm9606507
CHEMBL275701 97981 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)cc2OC)cc1 10.1021/jm9606507
10973523 201164 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 537 7 1 8 4.2 COc1ccc(C2=C(C(=O)NS(C)(=O)=O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL62578 201164 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 537 7 1 8 4.2 COc1ccc(C2=C(C(=O)NS(C)(=O)=O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
11122785 201277 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 8 1 6 4.6 COCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63057 201277 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 8 1 6 4.6 COCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10649546 108114 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 516 13 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCCO1 10.1021/jm980217s
CHEMBL320569 108114 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 516 13 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCCO1 10.1021/jm980217s
CHEMBL2304015 207716 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
10029171 98297 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 505 6 2 7 3.0 Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL278109 98297 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 505 6 2 7 3.0 Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
11800804 161275 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 550 10 4 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL414605 161275 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 550 10 4 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
42630655 18208 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271586 18208 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
10504475 205214 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 468 8 1 6 3.4 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)C)cc1 10.1021/jm9505369
CHEMBL9119 205214 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 468 8 1 6 3.4 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)C)cc1 10.1021/jm9505369
71456863 81264 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL2163716 81264 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
10971938 201278 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 424 7 1 5 5.6 CC(C)CCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63058 201278 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 424 7 1 5 5.6 CC(C)CCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44315008 102345 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 665 13 5 5 4.7 CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL305524 102345 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 665 13 5 5 4.7 CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
71453356 81239 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 554 13 2 10 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cccc(OC)c1 10.1021/jm3009103
CHEMBL2163691 81239 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 554 13 2 10 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cccc(OC)c1 10.1021/jm3009103
71456863 81264 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163716 81264 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
11827768 9767 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)c1 10.1021/jm0102304
CHEMBL114201 9767 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)c1 10.1021/jm0102304
44387543 60223 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 759 9 1 9 8.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(Cl)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1.O=C1C2=C(CCCC2)c2ccccc21 10.1021/jm0102304
CHEMBL175931 60223 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 759 9 1 9 8.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(Cl)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1.O=C1C2=C(CCCC2)c2ccccc21 10.1021/jm0102304
44334129 108054 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 459 8 1 5 5.5 CCCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL320208 108054 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 459 8 1 5 5.5 CCCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
10507467 8400 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 580 12 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)Cc1ccccc1 10.1021/jm970101g
CHEMBL109408 8400 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 580 12 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)Cc1ccccc1 10.1021/jm970101g
10118046 9330 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 504 10 1 7 2.9 CCCS(=O)(=O)N(C)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL111728 9330 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 504 10 1 7 2.9 CCCS(=O)(=O)N(C)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
10597575 6803 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 408 5 1 6 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCC2)cc1 10.1021/jm9606507
CHEMBL10843 6803 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 408 5 1 6 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCC2)cc1 10.1021/jm9606507
10671928 7180 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 467 5 1 7 4.4 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2nccc3ccccc23)cc1 10.1021/jm9606507
CHEMBL10860 7180 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 467 5 1 7 4.4 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2nccc3ccccc23)cc1 10.1021/jm9606507
10791988 8482 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 516 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCOCC1 10.1021/jm980217s
CHEMBL109474 8482 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 516 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCOCC1 10.1021/jm980217s
10792934 163350 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 10 2 6 5.6 CCc1cc(CC)c(NC(=O)CN2C[C@H](c3ccc4c(c3)OCO4)[C@@H](C(=O)O)[C@@H]2c2ccc(OC)cc2)c(CC)c1 10.1021/jm990170q
CHEMBL420729 163350 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 10 2 6 5.6 CCc1cc(CC)c(NC(=O)CN2C[C@H](c3ccc4c(c3)OCO4)[C@@H](C(=O)O)[C@@H]2c2ccc(OC)cc2)c(CC)c1 10.1021/jm990170q
9939960 174992 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 704 13 2 11 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)cc(C(=O)N2CCN(C)CC2)cc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL4579445 174992 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 704 13 2 11 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)cc(C(=O)N2CCN(C)CC2)cc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
127035070 135936 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 647 11 2 7 7.3 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3735931 135936 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 647 11 2 7 7.3 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
127036865 136886 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 584 10 3 7 5.7 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3753406 136886 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 584 10 3 7 5.7 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
9875246 119790 0 None - 0 Pig 8.0 pIC50 = 8 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 733 15 2 12 6.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCC(=O)O)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
CHEMBL352775 119790 0 None - 0 Pig 8.0 pIC50 = 8 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 733 15 2 12 6.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCC(=O)O)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
10696210 99074 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 9 3.7 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
CHEMBL283535 99074 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 9 3.7 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
44291884 172319 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 9 3.7 CC(=O)c1c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)ccc2c1OCO2 10.1021/jm9700068
CHEMBL45160 172319 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 9 3.7 CC(=O)c1c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)ccc2c1OCO2 10.1021/jm9700068
10671037 130909 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL273660 130909 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL369085 130909 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
10673756 201760 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 529 9 1 8 4.3 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN3CCCC3)c2)cc1 10.1021/jm980504w
CHEMBL65939 201760 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 529 9 1 8 4.3 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN3CCCC3)c2)cc1 10.1021/jm980504w
10475644 201433 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 392 5 1 6 3.2 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
CHEMBL6412 201433 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 392 5 1 6 3.2 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
10696210 99074 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 483 6 2 9 3.7 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm000349x
CHEMBL283535 99074 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 483 6 2 9 3.7 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm000349x
71456862 81257 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 651 12 1 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163709 81257 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 651 12 1 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
44291583 100907 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 500 8 3 9 2.9 COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1 10.1021/jm9608366
CHEMBL297215 100907 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 500 8 3 9 2.9 COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1 10.1021/jm9608366
44278215 99084 0 None - 0 Human 7.0 pIC50 = 7 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 491 5 1 9 4.7 O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3 10.1016/0960-894X(96)00232-6
CHEMBL283598 99084 0 None - 0 Human 7.0 pIC50 = 7 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 491 5 1 9 4.7 O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3 10.1016/0960-894X(96)00232-6
10841576 11323 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 620 11 2 6 6.3 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC 10.1021/jm990171i
CHEMBL1180336 11323 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 620 11 2 6 6.3 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC 10.1021/jm990171i
CHEMBL122673 11323 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 620 11 2 6 6.3 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC 10.1021/jm990171i
CHEMBL94907 214127 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
CHEMBL2304010 207711 0 None - 0 Pig 7.0 pIC50 = 7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
10792316 167906 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 530 8 2 6 5.3 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C(C)C)cc1 10.1021/jm990170q
CHEMBL435185 167906 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 530 8 2 6 5.3 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C(C)C)cc1 10.1021/jm990170q
18738890 98677 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 548 7 1 8 4.5 COC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1016/s0960-894x(01)00660-6
CHEMBL281121 98677 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 548 7 1 8 4.5 COC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1016/s0960-894x(01)00660-6
23445498 204963 0 None - 0 Human 7.0 pIC50 = 7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 426 4 1 5 4.9 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(96)00496-9
CHEMBL89688 204963 0 None - 0 Human 7.0 pIC50 = 7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 426 4 1 5 4.9 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(96)00496-9
10265127 96375 2 None - 0 Rat 6.0 pIC50 = 6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C 10.1021/jm00008a013
CHEMBL26522 96375 2 None - 0 Rat 6.0 pIC50 = 6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C 10.1021/jm00008a013
CHEMBL315047 209430 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
44327659 109321 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 937 26 9 8 4.6 CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1 10.1021/jm00015a003
CHEMBL323331 109321 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 937 26 9 8 4.6 CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1 10.1021/jm00015a003
CHEMBL318020 209453 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
44316685 203329 1 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 266 3 1 4 2.4 Cc1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL77090 203329 1 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 266 3 1 4 2.4 Cc1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
10022291 111523 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 374 9 1 3 5.1 O=C(O)CCC(C(=O)c1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
CHEMBL328964 111523 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 374 9 1 3 5.1 O=C(O)CCC(C(=O)c1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
12060119 109889 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 441 7 2 6 3.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL324304 109889 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 441 7 2 6 3.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)cc1 10.1016/j.bmcl.2016.06.014
4568158 110906 1 None - 0 Rat 6.0 pIC50 = 6 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 400 8 2 4 4.9 O=C(O)c1cc(-c2ccc(OCc3ccccc3)cc2OCc2ccccc2)[nH]n1 10.1021/jm9707131
CHEMBL327247 110906 1 None - 0 Rat 6.0 pIC50 = 6 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 400 8 2 4 4.9 O=C(O)c1cc(-c2ccc(OCc3ccccc3)cc2OCc2ccccc2)[nH]n1 10.1021/jm9707131
CHEMBL315047 209430 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
10568280 201405 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 328 4 1 5 2.5 CN(C)c1cccc2c(S(=O)(=O)Nc3cnccn3)cccc12 10.1021/jm9604585
CHEMBL6399 201405 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 328 4 1 5 2.5 CN(C)c1cccc2c(S(=O)(=O)Nc3cnccn3)cccc12 10.1021/jm9604585
10553319 60727 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 496 11 5 4 3.8 CCN(CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C)[nH]1 10.1021/jm950592+
CHEMBL176430 60727 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 496 11 5 4 3.8 CCN(CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C)[nH]1 10.1021/jm950592+
10006086 120536 0 None - 0 Pig 5.0 pIC50 = 5 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 498 9 2 5 4.6 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL356916 120536 0 None - 0 Pig 5.0 pIC50 = 5 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 498 9 2 5 4.6 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
10381122 98727 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C 10.1021/jm00008a013
CHEMBL281427 98727 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C 10.1021/jm00008a013
44327466 95991 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 966 25 9 8 5.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(C)(C)C)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL262229 95991 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 966 25 9 8 5.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(C)(C)C)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
18617385 203491 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL78601 203491 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1C 10.1016/0960-894X(96)00441-6
127029201 136721 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 644 12 3 9 5.7 CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3751994 136721 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 644 12 3 9 5.7 CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
3080568 178257 30 None - 0 Rat 5.0 pIC50 = 5 Binding
Displacement of endothelin-1 from ETA receptor in rat A10 cellsDisplacement of endothelin-1 from ETA receptor in rat A10 cells
ChEMBL 348 5 3 7 2.7 COC(=O)c1cc(O)cc(OC)c1Oc1cc(C)cc(O)c1C(=O)O 10.1021/np0102758
CHEMBL469424 178257 30 None - 0 Rat 5.0 pIC50 = 5 Binding
Displacement of endothelin-1 from ETA receptor in rat A10 cellsDisplacement of endothelin-1 from ETA receptor in rat A10 cells
ChEMBL 348 5 3 7 2.7 COC(=O)c1cc(O)cc(OC)c1Oc1cc(C)cc(O)c1C(=O)O 10.1021/np0102758
9846065 170342 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 439 7 2 6 3.6 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4455096 170342 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 439 7 2 6 3.6 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
44276947 106355 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 430 5 1 3 5.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)c(Cl)c3)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144803 106355 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 430 5 1 3 5.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)c(Cl)c3)c2=O)c1 10.1016/s0960-894x(00)00232-8
44276907 106359 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 376 4 1 4 3.6 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1 10.1016/s0960-894x(00)00232-8
CHEMBL3144845 106359 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 376 4 1 4 3.6 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1 10.1016/s0960-894x(00)00232-8
10381122 98727 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C 10.1021/jm00004a012
CHEMBL281427 98727 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C 10.1021/jm00004a012
3765218 201721 1 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 419 4 1 4 4.2 Cc1nc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)ccc1Br 10.1021/jm9604585
CHEMBL6566 201721 1 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 419 4 1 4 4.2 Cc1nc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)ccc1Br 10.1021/jm9604585
44266649 97646 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 391 3 1 4 5.4 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1-c1ccccc1 10.1016/0960-894X(96)00170-9
CHEMBL273488 97646 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 391 3 1 4 5.4 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1-c1ccccc1 10.1016/0960-894X(96)00170-9
23445421 59600 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 454 6 1 5 5.0 Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL173189 59600 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 454 6 1 5 5.0 Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
10832763 167864 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 366 4 2 6 2.3 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Br 10.1016/S0960-894X(97)00367-3
CHEMBL434983 167864 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 366 4 2 6 2.3 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Br 10.1016/S0960-894X(97)00367-3
137649809 156833 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 583 10 2 7 5.9 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4078297 156833 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 583 10 2 7 5.9 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10527774 183096 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL48031 183096 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
22998456 59467 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
CHEMBL172666 59467 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
9874379 60110 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 653 14 2 10 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL175268 60110 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 653 14 2 10 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
10718385 205074 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 450 7 1 6 2.4 C#CCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9040 205074 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 450 7 1 6 2.4 C#CCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
23445593 59904 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 440 6 1 5 4.7 Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
CHEMBL174086 59904 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 440 6 1 5 4.7 Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
10805820 202013 54 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 322 4 2 6 2.2 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Cl 10.1016/S0960-894X(97)00367-3
CHEMBL67664 202013 54 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 322 4 2 6 2.2 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Cl 10.1016/S0960-894X(97)00367-3
10812400 97914 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 427 9 1 6 3.7 CCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL275306 97914 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 427 9 1 6 3.7 CCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44265853 204666 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 4 1 6 2.7 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)N2CCOCC2)cc1 10.1021/jm9505369
CHEMBL8776 204666 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 4 1 6 2.7 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)N2CCOCC2)cc1 10.1021/jm9505369
10854399 201302 37 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 336 4 1 7 2.3 COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1016/S0960-894X(97)00367-3
CHEMBL63169 201302 37 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 336 4 1 7 2.3 COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1016/S0960-894X(97)00367-3
10647020 60951 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1OC 10.1021/jm031041j
CHEMBL176696 60951 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1OC 10.1021/jm031041j
10647021 6881 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1OC 10.1021/jm9606507
CHEMBL10846 6881 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1OC 10.1021/jm9606507
10552548 98057 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2OC)cc1 10.1021/jm9606507
CHEMBL276252 98057 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2OC)cc1 10.1021/jm9606507
9934580 162368 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 474 6 1 8 3.6 COC(=O)c1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL417428 162368 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 474 6 1 8 3.6 COC(=O)c1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
127035757 135969 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 591 10 1 8 6.2 CCCCc1nn(-c2ccccc2Cl)c(=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3736242 135969 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 591 10 1 8 6.2 CCCCc1nn(-c2ccccc2Cl)c(=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
76308472 84916 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 517 6 1 8 3.7 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C#N)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261600 84916 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 517 6 1 8 3.7 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C#N)ccc12 10.1007/s00044-004-0021-y
44320338 106478 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 490 7 2 6 5.0 O=C(O)c1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc1 10.1016/s0960-894x(00)00513-8
CHEMBL315087 106478 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 490 7 2 6 5.0 O=C(O)c1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc1 10.1016/s0960-894x(00)00513-8
44385162 61037 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 533 10 2 10 3.3 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176963 61037 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 533 10 2 10 3.3 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10697633 60000 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL174448 60000 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
10697633 60000 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL174448 60000 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
10551548 127283 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 450 7 1 5 5.0 COc1ccc(C(=O)/C(Cc2ccc(Cl)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL366442 127283 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 450 7 1 5 5.0 COc1ccc(C(=O)/C(Cc2ccc(Cl)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
11732966 201472 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 444 5 1 5 5.6 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1 10.1021/jm031041j
CHEMBL64244 201472 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 444 5 1 5 5.6 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1 10.1021/jm031041j
CHEMBL302776 209160 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00089a028
22616262 203818 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 366 3 1 4 3.7 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80980 203818 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 366 3 1 4 3.7 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1Br 10.1016/0960-894X(96)00441-6
18617351 103619 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL309397 103619 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1Br 10.1016/0960-894X(96)00441-6
10433234 203726 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 436 5 1 4 4.3 CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80342 203726 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 436 5 1 4 4.3 CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
11744509 5343 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 450 5 1 6 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1 10.1021/jm9606507
CHEMBL10733 5343 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 450 5 1 6 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1 10.1021/jm9606507
11732966 201472 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 444 5 1 5 5.6 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL64244 201472 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 444 5 1 5 5.6 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1 10.1021/jm010382z
54587165 59975 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 675 15 5 4 5.9 CCCCCC[C@@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL1744023 59975 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 675 15 5 4 5.9 CCCCCC[C@@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44293932 162584 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL417903 162584 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
15304942 163867 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 394 9 1 4 5.5 Cc1ccccc1C(CCC(=O)O)C(=O)c1cccc(OCc2ccsc2)c1 10.1021/jm9707131
CHEMBL421365 163867 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 394 9 1 4 5.5 Cc1ccccc1C(CCC(=O)O)C(=O)c1cccc(OCc2ccsc2)c1 10.1021/jm9707131
44213279 106352 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 456 6 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144737 106352 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 456 6 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
10554748 59744 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 552 10 6 6 3.3 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(O)CC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL173826 59744 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 552 10 6 6 3.3 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(O)CC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL335143 209790 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44382975 119814 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 596 11 4 7 3.7 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCc1nc(C(=O)O)cs1 10.1016/0960-894X(95)00144-I
CHEMBL352929 119814 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 596 11 4 7 3.7 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCc1nc(C(=O)O)cs1 10.1016/0960-894X(95)00144-I
10440821 205794 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 918 24 9 8 4.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c(C)c(C)c(C)c(C)c1C)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL94689 205794 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 918 24 9 8 4.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c(C)c(C)c(C)c(C)c1C)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10620470 111018 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 391 7 1 5 4.8 COc1cccc(/C(=C\c2cc(OCc3ccsc3)ccc2C#N)C(=O)O)c1 10.1021/jm970847e
CHEMBL327861 111018 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 391 7 1 5 4.8 COc1cccc(/C(=C\c2cc(OCc3ccsc3)ccc2C#N)C(=O)O)c1 10.1021/jm970847e
44293915 191937 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 507 9 1 8 4.4 CCOc1ccc2c(c1)[C@H](c1cc(OC)c(OC)c(OC)c1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL52110 191937 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 507 9 1 8 4.4 CCOc1ccc2c(c1)[C@H](c1cc(OC)c(OC)c(OC)c1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
44291495 11114 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl 10.1021/jm9700068
CHEMBL1178832 11114 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl 10.1021/jm9700068
CHEMBL45351 11114 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl 10.1021/jm9700068
44266565 97769 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 417 5 1 6 4.7 COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OC)cc23)cc1 10.1016/0960-894X(96)00170-9
CHEMBL274370 97769 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 417 5 1 6 4.7 COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OC)cc23)cc1 10.1016/0960-894X(96)00170-9
44311225 202991 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 581 11 1 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1ccoc1 10.1016/S0960-894X(97)00400-9
CHEMBL74118 202991 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 581 11 1 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1ccoc1 10.1016/S0960-894X(97)00400-9
13044638 85397 15 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 206 2 1 3 2.4 COc1cccc2oc(C(=O)O)c(C)c12 10.1007/s00044-013-0542-3
CHEMBL2296888 85397 15 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 206 2 1 3 2.4 COc1cccc2oc(C(=O)O)c(C)c12 10.1007/s00044-013-0542-3
CHEMBL269428 209032 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10769177 112400 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.2 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCOC)cc1 10.1021/jm990170q
CHEMBL331066 112400 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.2 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCOC)cc1 10.1021/jm990170q
127026338 136866 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 616 11 3 7 5.9 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3F)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3753277 136866 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 616 11 3 7 5.9 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3F)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
120533 101146 9 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 379 3 2 5 2.0 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1I 10.1016/s0960-894x(00)00366-8
CHEMBL298976 101146 9 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 379 3 2 5 2.0 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1I 10.1016/s0960-894x(00)00366-8
10674532 168012 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 567 10 4 5 5.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)s1 10.1021/jm950591h
CHEMBL435894 168012 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 567 10 4 5 5.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)s1 10.1021/jm950591h
10452089 4482 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 375 3 0 5 4.1 COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2 10.1016/S0960-894X(96)00551-3
CHEMBL102494 4482 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 375 3 0 5 4.1 COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2 10.1016/S0960-894X(96)00551-3
10095637 49682 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 457 9 1 5 5.8 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccccc1 10.1016/0960-894X(95)00186-W
CHEMBL15689 49682 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 457 9 1 5 5.8 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccccc1 10.1016/0960-894X(95)00186-W
19385674 98124 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br 10.1016/0960-894X(95)00186-W
CHEMBL276819 98124 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br 10.1016/0960-894X(95)00186-W
19385674 98124 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br 10.1021/jm058225d
CHEMBL276819 98124 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br 10.1021/jm058225d
44266538 5376 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 371 4 1 4 4.8 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccccc1 10.1016/0960-894X(96)00170-9
CHEMBL10750 5376 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 371 4 1 4 4.8 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccccc1 10.1016/0960-894X(96)00170-9
11798999 205841 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 482 7 1 6 3.8 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)(C)C)cc1 10.1021/jm9505369
CHEMBL9495 205841 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 482 7 1 6 3.8 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)(C)C)cc1 10.1021/jm9505369
71460536 81260 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 589 11 1 12 3.1 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163712 81260 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 589 11 1 12 3.1 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
10669120 205702 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1[C@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
CHEMBL94141 205702 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1[C@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
23445366 105689 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 482 7 1 5 6.2 Cc1cc(CCC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL313801 105689 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 482 7 1 5 6.2 Cc1cc(CCC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
52949197 18225 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 555 10 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271746 18225 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 555 10 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
10694591 9121 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 444 6 1 6 4.6 CC(C)Oc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL11064 9121 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 444 6 1 6 4.6 CC(C)Oc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
18184194 130027 0 None - 2 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 712 15 2 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL368107 130027 0 None - 2 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 712 15 2 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
9998577 97638 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 5 1 5 3.6 CCc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00008a013
CHEMBL27344 97638 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 5 1 5 3.6 CCc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00008a013
CHEMBL327350 209534 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
18184228 61009 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 604 13 2 9 4.6 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL176749 61009 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 604 13 2 9 4.6 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
10342643 5073 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
CHEMBL10588 5073 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
10791694 97735 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2OC)cc1 10.1021/jm9606507
CHEMBL274175 97735 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2OC)cc1 10.1021/jm9606507
11058202 201126 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 388 4 1 5 4.4 CC(C)Oc1ccc2c(c1)C(Cl)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL62374 201126 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 388 4 1 5 4.4 CC(C)Oc1ccc2c(c1)C(Cl)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
11799636 108764 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 502 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCO1 10.1021/jm980217s
CHEMBL321831 108764 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 502 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCO1 10.1021/jm980217s
10626646 16254 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.8 CCCc1cccc(CCC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL123305 16254 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.8 CCCc1cccc(CCC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
10224745 112180 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 432 5 2 6 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1016/j.bmcl.2016.06.014
CHEMBL330425 112180 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 432 5 2 6 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1016/j.bmcl.2016.06.014
44459272 90795 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 491 6 2 7 2.6 Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL24015 90795 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 491 6 2 7 2.6 Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
22010352 117110 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 404 10 1 4 5.5 CC(=O)c1ccc(OCc2ccccc2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400984 117110 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 404 10 1 4 5.5 CC(=O)c1ccc(OCc2ccccc2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
10693270 59739 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL172144 59739 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL173792 59739 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
44295257 14444 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 538 10 1 9 4.8 COc1cc(F)ccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1 10.1016/s0960-894x(98)00301-1
CHEMBL1205063 14444 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 538 10 1 9 4.8 COc1cc(F)ccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1 10.1016/s0960-894x(98)00301-1
CHEMBL48458 14444 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 538 10 1 9 4.8 COc1cc(F)ccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1 10.1016/s0960-894x(98)00301-1
9915095 101047 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 535 8 2 8 3.4 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(C(=O)C(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL298212 101047 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 535 8 2 8 3.4 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(C(=O)C(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10864618 112810 0 None - 0 Pig 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 556 11 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2nccs2)c1 10.1021/jm0102304
CHEMBL331580 112810 0 None - 0 Pig 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 556 11 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2nccs2)c1 10.1021/jm0102304
10599879 100793 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL296326 100793 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
10233400 128150 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccncc1 10.1016/s0960-894x(02)01084-3
CHEMBL366885 128150 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccncc1 10.1016/s0960-894x(02)01084-3
10304227 129473 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 603 10 2 13 4.2 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL367686 129473 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 603 10 2 13 4.2 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10745668 202663 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 572 10 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCN(C)CC3)c2)cc1 10.1021/jm980504w
CHEMBL71787 202663 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 572 10 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCN(C)CC3)c2)cc1 10.1021/jm980504w
CHEMBL137659 206994 0 None - 0 Pig 7.9 pIC50 = 7.9 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O 10.1021/jm00021a021
44302513 102232 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 553 9 3 9 5.1 CCCc1c(O)c(C(C)=O)cc(C(C)=O)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
CHEMBL304860 102232 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 553 9 3 9 5.1 CCCc1c(O)c(C(C)=O)cc(C(C)=O)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm030528p
10623465 202043 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of specific binding of [125-I] ET-1 to human Endothelin A receptorInhibition of specific binding of [125-I] ET-1 to human Endothelin A receptor
ChEMBL 450 6 1 6 3.7 CCN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12 10.1021/jm9604585
CHEMBL6785 202043 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of specific binding of [125-I] ET-1 to human Endothelin A receptorInhibition of specific binding of [125-I] ET-1 to human Endothelin A receptor
ChEMBL 450 6 1 6 3.7 CCN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12 10.1021/jm9604585
18617303 105302 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1cccc(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
CHEMBL312685 105302 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1cccc(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
15453179 203760 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80538 203760 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Br 10.1016/0960-894X(96)00441-6
44293866 101138 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 461 8 1 6 4.8 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL298922 101138 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 461 8 1 6 4.8 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL292901 209132 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00349-X
10627333 60049 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 595 11 4 8 4.2 COC(=O)C1(NC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc2cn(C)c3ccccc23)c2nc(C(=O)O)c(C)o2)CCCCC1 10.1021/jm950592+
CHEMBL174818 60049 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 595 11 4 8 4.2 COC(=O)C1(NC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc2cn(C)c3ccccc23)c2nc(C(=O)O)c(C)o2)CCCCC1 10.1021/jm950592+
CHEMBL335416 209791 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CCCC[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O 10.1021/jm00021a021
10961510 201138 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 458 7 1 4 6.6 COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm031041j
CHEMBL62425 201138 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 458 7 1 4 6.6 COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm031041j
44371449 49098 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c(OC)c1 10.1016/s0960-894x(99)00040-2
CHEMBL156404 49098 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c(OC)c1 10.1016/s0960-894x(99)00040-2
44371460 49250 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 469 5 1 7 4.9 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
CHEMBL156539 49250 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 469 5 1 7 4.9 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
10961510 201138 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 458 7 1 4 6.6 COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL62425 201138 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 458 7 1 4 6.6 COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
11733232 201167 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 7 1 6 5.2 CCCOc1cccc2c1C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL62586 201167 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 7 1 6 5.2 CCCOc1cccc2c1C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL412460 211234 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
23445317 100067 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 456 5 1 7 4.1 Cc1cccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(97)00367-3
CHEMBL291404 100067 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 456 5 1 7 4.1 Cc1cccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(97)00367-3
23445507 59433 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
CHEMBL172538 59433 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
44298956 193997 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 489 9 1 7 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1OC)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL55666 193997 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 489 9 1 7 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1OC)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
10041979 98900 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 325 6 3 6 1.6 Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2)c1C 10.1021/jm00008a013
CHEMBL282557 98900 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 325 6 3 6 1.6 Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2)c1C 10.1021/jm00008a013
44266654 97609 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 387 4 1 5 4.7 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccccc1 10.1016/0960-894X(96)00170-9
CHEMBL273258 97609 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 387 4 1 5 4.7 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccccc1 10.1016/0960-894X(96)00170-9
44385576 130842 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 539 10 1 10 3.4 C#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368929 130842 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 539 10 1 10 3.4 C#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
11799440 205238 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 11 1 6 4.3 CCCN(CCC)C(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9132 205238 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 11 1 6 4.3 CCCN(CCC)C(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
52949197 18225 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 555 10 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271746 18225 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 555 10 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10531506 11995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1 10.1021/jm990171i
CHEMBL1184076 11995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1 10.1021/jm990171i
CHEMBL331548 11995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1 10.1021/jm990171i
10650546 11999 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 562 7 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1 10.1021/jm990171i
CHEMBL1184091 11999 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 562 7 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1 10.1021/jm990171i
CHEMBL332144 11999 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 562 7 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1 10.1021/jm990171i
10814743 178781 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 484 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C2(Cc3ccc4c(c3)OCO4)OCCO2)c1Cl 10.1021/jm9700068
CHEMBL47383 178781 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 484 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C2(Cc3ccc4c(c3)OCO4)OCCO2)c1Cl 10.1021/jm9700068
10623888 162596 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 461 8 1 6 3.4 CCCCS(=O)(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL417971 162596 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 461 8 1 6 3.4 CCCCS(=O)(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10281573 59645 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 574 9 2 9 4.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL173358 59645 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 574 9 2 9 4.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
44385586 61318 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 531 10 1 9 4.7 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL177143 61318 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 531 10 1 9 4.7 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10645066 96733 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 406 4 1 5 3.3 CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Br)cn3)cccc12 10.1021/jm9604585
CHEMBL268339 96733 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 406 4 1 5 3.3 CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Br)cn3)cccc12 10.1021/jm9604585
11792960 161354 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 361 4 1 4 3.8 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)nc3)cccc12 10.1021/jm9604585
CHEMBL415292 161354 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 361 4 1 4 3.8 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)nc3)cccc12 10.1021/jm9604585
10593411 201746 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 342 4 1 5 2.8 Cc1cnc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cn1 10.1021/jm9604585
CHEMBL6583 201746 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 342 4 1 5 2.8 Cc1cnc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cn1 10.1021/jm9604585
127029202 136791 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 598 11 3 7 5.8 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3752680 136791 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 598 11 3 7 5.8 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
10122495 30640 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 665 12 1 10 6.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOCc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL139734 30640 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 665 12 1 10 6.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOCc1ccccc1 10.1016/s0960-894x(02)01084-3
44384177 119774 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 506 6 1 8 4.6 Cc1noc(NS(=O)(=O)c2ccsc2COc2cc3c(cc2Cl)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
CHEMBL352657 119774 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 506 6 1 8 4.6 Cc1noc(NS(=O)(=O)c2ccsc2COc2cc3c(cc2Cl)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
10550033 100884 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 419 5 2 9 2.9 Cc1nnc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)s1 10.1021/jm9608366
CHEMBL297048 100884 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 419 5 2 9 2.9 Cc1nnc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)s1 10.1021/jm9608366
10626521 59745 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 11 4 6 5.1 CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)o2)c2ccccc21 10.1021/jm950592+
CHEMBL173833 59745 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 11 4 6 5.1 CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)o2)c2ccccc21 10.1021/jm950592+
CHEMBL94983 214129 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10671036 6564 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c(OC)c1 10.1021/jm9606507
CHEMBL10834 6564 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c(OC)c1 10.1021/jm9606507
9932004 97712 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 422 5 1 6 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCC2)cc1 10.1021/jm9606507
CHEMBL273948 97712 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 422 5 1 6 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCC2)cc1 10.1021/jm9606507
10816110 108066 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 532 13 1 7 4.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OC(C)C(C)O1 10.1021/jm980217s
CHEMBL320254 108066 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 532 13 1 7 4.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OC(C)C(C)O1 10.1021/jm980217s
44314619 202970 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL 631 12 5 4 4.5 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL73925 202970 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL 631 12 5 4 4.5 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
10209324 14321 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 546 8 1 7 6.2 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C)c1)C(=O)CCCC2 10.1039/C4MD00499J
CHEMBL12013 14321 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 546 8 1 7 6.2 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C)c1)C(=O)CCCC2 10.1039/C4MD00499J
10740439 172169 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 412 5 2 7 3.5 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)nc1 10.1021/jm9608366
CHEMBL45087 172169 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 412 5 2 7 3.5 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)nc1 10.1021/jm9608366
135415889 58942 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 587 10 2 13 3.6 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL170401 58942 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 587 10 2 13 3.6 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10281943 59734 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 589 10 1 10 4.9 COCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL173743 59734 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 589 10 1 10 4.9 COCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10212088 96235 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 688 12 2 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL264035 96235 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 688 12 2 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL2370830 208174 0 None - 0 Pig 7.9 pIC50 = 7.9 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
42630531 18287 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 543 9 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)C)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1272299 18287 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 543 9 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)C)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
10768904 12009 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 544 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1184117 12009 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 544 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL333034 12009 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 544 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1 10.1021/jm990171i
10385400 95747 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 385 4 1 5 3.4 Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCC4=O)cccc23)c1C 10.1021/jm00008a013
CHEMBL26079 95747 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 385 4 1 5 3.4 Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCC4=O)cccc23)c1C 10.1021/jm00008a013
10426828 97680 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 331 4 2 5 3.3 CNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL27370 97680 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 331 4 2 5 3.3 CNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
10361993 99092 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 373 5 1 5 4.1 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C(C)C)cccc23)c1C 10.1021/jm00008a013
CHEMBL283652 99092 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 373 5 1 5 4.1 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C(C)C)cccc23)c1C 10.1021/jm00008a013
11103224 200957 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 510 14 1 6 7.3 CCCCCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL61406 200957 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 510 14 1 6 7.3 CCCCCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
11826847 201221 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccccc1OC)O2 10.1021/jm010382z
CHEMBL62814 201221 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccccc1OC)O2 10.1021/jm010382z
10837347 8766 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL109736 8766 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10298764 9746 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 468 8 1 6 3.2 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL114084 9746 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 468 8 1 6 3.2 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL317064 209441 13 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
44266552 4431 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10218 4431 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL337567 209842 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CSCC[C@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm00021a021
CHEMBL150719 207039 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
The inhibitory constant was evaluated against Endothelin A receptor in rabbit renal artery tissueThe inhibitory constant was evaluated against Endothelin A receptor in rabbit renal artery tissue
ChEMBL None None None CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC 10.1016/S0960-894X(01)81219-1
44371421 51145 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 459 5 1 5 5.8 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3Cl)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL158204 51145 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 459 5 1 5 5.8 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3Cl)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
10067008 97338 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1 10.1021/jm00008a013
CHEMBL27187 97338 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1 10.1021/jm00008a013
10423091 99496 3 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C 10.1021/jm00008a013
CHEMBL286521 99496 3 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C 10.1021/jm00008a013
10552007 6231 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 462 8 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c(OC)c(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10819 6231 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 462 8 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c(OC)c(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10961720 201782 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 472 6 1 5 6.3 CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(C(C)C)cc1)O2 10.1021/jm010382z
CHEMBL66094 201782 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 472 6 1 5 6.3 CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(C(C)C)cc1)O2 10.1021/jm010382z
10577405 9546 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1C(C)(C)CCCC 10.1021/jm980217s
CHEMBL112777 9546 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1C(C)(C)CCCC 10.1021/jm980217s
10573912 111119 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 415 7 1 5 5.5 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1Cl 10.1021/jm970847e
CHEMBL328444 111119 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 415 7 1 5 5.5 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1Cl 10.1021/jm970847e
10524954 205321 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 399 6 1 5 4.5 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1/C=C(/C(=O)O)c1ccccc1 10.1021/jm970847e
CHEMBL91741 205321 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 399 6 1 5 4.5 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1/C=C(/C(=O)O)c1ccccc1 10.1021/jm970847e
44298343 101310 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 485 9 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC#N)c1 10.1016/s0960-894x(00)00366-8
CHEMBL300066 101310 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 485 9 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC#N)c1 10.1016/s0960-894x(00)00366-8
44298279 193272 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 502 10 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(C)=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54274 193272 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 502 10 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(C)=O)c1 10.1016/s0960-894x(00)00366-8
155560344 175919 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting method
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/acs.jmedchem.5b01781
CHEMBL4568795 175919 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting method
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/acs.jmedchem.5b01781
CHEMBL4596821 175919 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting method
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/acs.jmedchem.5b01781
155535325 171433 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 549 10 2 8 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)cc(-c2ncccn2)cc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4471434 171433 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 549 10 2 8 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)cc(-c2ncccn2)cc1OCCO 10.1016/j.bmcl.2016.06.014
44276946 106350 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 440 5 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc(Cl)c4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144735 106350 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 440 5 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc(Cl)c4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
44309897 202915 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 469 5 1 7 4.9 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4c(c3)OCO4)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(97)10151-2
CHEMBL73506 202915 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 469 5 1 7 4.9 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4c(c3)OCO4)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(97)10151-2
44298988 100239 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 459 8 1 6 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL292580 100239 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 459 8 1 6 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
10067008 97338 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1 10.1021/jm00004a012
CHEMBL27187 97338 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1 10.1021/jm00004a012
10423091 99496 3 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C 10.1021/jm00004a012
CHEMBL286521 99496 3 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C 10.1021/jm00004a012
44266595 4312 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 507 6 1 7 6.0 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10136 4312 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 507 6 1 7 6.0 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
10337668 101654 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 346 4 2 5 2.9 Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C 10.1021/jm00029a001
CHEMBL30246 101654 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 346 4 2 5 2.9 Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C 10.1021/jm00029a001
10337668 101654 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 346 4 2 5 2.9 Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C 10.1021/jm00008a013
CHEMBL30246 101654 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 346 4 2 5 2.9 Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C 10.1021/jm00008a013
160743 202775 22 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 309 4 2 5 2.1 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00008a013
CHEMBL725 202775 22 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 309 4 2 5 2.1 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00008a013
18617314 203511 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78734 203511 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL38071 210515 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
44213959 169789 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 592 11 3 9 5.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(=O)Nc2ccccc2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4447655 169789 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 592 11 3 9 5.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(=O)Nc2ccccc2)nc1OCCO 10.1016/j.bmcl.2016.06.014
127026027 136736 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 628 12 3 8 5.8 CCCc1nc2c(C)cc(C(=O)NCCc3ccc(OC)cc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3752145 136736 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 628 12 3 8 5.8 CCCc1nc2c(C)cc(C(=O)NCCc3ccc(OC)cc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL1791280 207167 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(95)00152-J
10816667 11324 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 558 9 2 6 5.6 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1180341 11324 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 558 9 2 6 5.6 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL122933 11324 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 558 9 2 6 5.6 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1 10.1021/jm990171i
9853680 98182 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 771 17 2 14 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL277275 98182 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 771 17 2 14 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
10576378 100641 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1021/jm9608366
CHEMBL295207 100641 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1021/jm9608366
CHEMBL170229 207089 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1cn(C)c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)N1CCCCCC1)C(=O)O 10.1016/0960-894X(95)00144-I
23445219 111970 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 428 5 1 6 4.3 COc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
CHEMBL329861 111970 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 428 5 1 6 4.3 COc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
44386163 60046 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 577 14 2 10 3.4 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL174781 60046 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 577 14 2 10 3.4 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
23445537 60802 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
CHEMBL176538 60802 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
10766067 9631 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113379 9631 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
127035069 135863 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 663 11 2 8 7.7 CCCc1nc2c(C)cc(C(=O)Nc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3735300 135863 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 663 11 2 8 7.7 CCCc1nc2c(C)cc(C(=O)Nc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
10792785 166159 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 3 6 5.0 CCOC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C 10.1021/jm950592+
CHEMBL428298 166159 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 3 6 5.0 CCOC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C 10.1021/jm950592+
9831527 128947 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 698 14 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL367274 128947 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 698 14 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
10189776 59727 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 651 11 1 10 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL173689 59727 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 651 11 1 10 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOc1ccccc1 10.1016/s0960-894x(02)01084-3
10743478 108768 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm031041j
CHEMBL321852 108768 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm031041j
10504389 130139 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 466 7 1 5 5.5 COc1ccc(C(=O)/C(Cc2cccc3ccccc23)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL368270 130139 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 466 7 1 5 5.5 COc1ccc(C(=O)/C(Cc2cccc3ccccc23)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
10505209 9212 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 490 6 1 9 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL11106 9212 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 490 6 1 9 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
10742841 96887 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 466 5 1 6 5.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3ccccc3c2)cc1 10.1021/jm9606507
CHEMBL269453 96887 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 466 5 1 6 5.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3ccccc3c2)cc1 10.1021/jm9606507
44314645 172093 0 None - 0 Pig 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 601 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC1CC1)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL449962 172093 0 None - 0 Pig 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 601 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC1CC1)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
10743478 108768 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL321852 108768 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10166561 9954 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 562 9 2 8 5.4 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CO)c1)C(=O)CCCC2 10.1039/C4MD00499J
CHEMBL11528 9954 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 562 9 2 8 5.4 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CO)c1)C(=O)CCCC2 10.1039/C4MD00499J
44214320 84912 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 510 6 1 7 4.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(F)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261364 84912 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 510 6 1 7 4.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(F)ccc12 10.1007/s00044-004-0021-y
10240093 81261 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 603 12 1 12 3.5 CCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163713 81261 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 603 12 1 12 3.5 CCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
71458721 81275 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 642 14 2 10 4.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(C2CC2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163726 81275 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 642 14 2 10 4.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(C2CC2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
10812894 119757 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 437 7 1 6 4.7 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
CHEMBL352536 119757 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 437 7 1 6 4.7 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
17869371 14605 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 478 8 1 7 4.8 COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1206716 14605 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 478 8 1 7 4.8 COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL299521 14605 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 478 8 1 7 4.8 COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44293417 186743 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 563 11 2 8 4.9 CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(C)(C)C(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL49312 186743 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 563 11 2 8 4.9 CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(C)(C)C(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
443289 702 40 None -2 3 Rat 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL None None None None 10.1021/jm9707131
997 702 40 None -2 3 Rat 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL None None None None 10.1021/jm9707131
CHEMBL314691 702 40 None -2 3 Rat 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL None None None None 10.1021/jm9707131
DB12054 702 40 None -2 3 Rat 7.9 pIC50 = 7.9 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL None None None None 10.1021/jm9707131
10814746 181002 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 484 6 1 8 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL47706 181002 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 484 6 1 8 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
10122675 98007 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 682 12 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
CHEMBL275897 98007 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 682 12 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
CHEMBL1791271 207163 2 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
9831249 59370 0 None - 2 Human 7.9 pIC50 = 7.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 672 14 2 10 6.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL172297 59370 0 None - 2 Human 7.9 pIC50 = 7.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 672 14 2 10 6.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
44311283 101850 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 649 11 2 10 6.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)(C)C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL303649 101850 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 649 11 2 10 6.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)(C)C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44320590 106066 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 556 10 2 9 4.8 COc1ccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL314206 106066 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 556 10 2 9 4.8 COc1ccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL1788127 209360 8 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL313760 209360 8 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
44382933 164536 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 541 12 4 5 3.2 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCCCC(=O)O 10.1016/0960-894X(95)00144-I
CHEMBL422720 164536 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 541 12 4 5 3.2 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCCCC(=O)O 10.1016/0960-894X(95)00144-I
CHEMBL330144 209571 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C 10.1021/jm00015a003
22616257 203295 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 272 3 1 4 2.4 Cc1noc(NS(=O)(=O)c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
CHEMBL76860 203295 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 272 3 1 4 2.4 Cc1noc(NS(=O)(=O)c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
44317109 104400 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 472 3 1 4 4.1 Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL311216 104400 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 472 3 1 4 4.1 Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1Br 10.1016/0960-894X(96)00441-6
18617327 203535 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1ccccc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78929 203535 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1ccccc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
44276969 106343 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 506 7 1 5 4.8 COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144607 106343 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 506 7 1 5 4.8 COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
9961131 131622 0 None - 2 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 650 15 2 12 3.1 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL369676 131622 0 None - 2 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 650 15 2 12 3.1 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL342617 209920 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL407639 210915 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CS(=O)(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10381121 95773 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3ccc(N)cc23)c1C 10.1021/jm00008a013
CHEMBL26090 95773 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3ccc(N)cc23)c1C 10.1021/jm00008a013
9974856 98881 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2ccc3ccc(N(C)C)cc3c2)c1C 10.1021/jm00008a013
CHEMBL282401 98881 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2ccc3ccc(N(C)C)cc3c2)c1C 10.1021/jm00008a013
CHEMBL1790499 207139 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
ChEMBL None None None CC[C@@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC1=O 10.1021/jm00089a028
CHEMBL327350 209534 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
18617355 203236 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/0960-894X(96)00441-6
CHEMBL76438 203236 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/0960-894X(96)00441-6
CHEMBL432683 211876 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00087a001
10618969 205601 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 367 7 1 5 4.8 O=[N+]([O-])c1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1 10.1021/jm970847e
CHEMBL93596 205601 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 367 7 1 5 4.8 O=[N+]([O-])c1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1 10.1021/jm970847e
127034901 135942 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 670 12 2 9 5.5 CCCc1nc2c(C)cc(C(=O)NCCN3CCOCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3736037 135942 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 670 12 2 9 5.5 CCCc1nc2c(C)cc(C(=O)NCCN3CCOCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
44298382 193432 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 502 11 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCC=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54998 193432 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 502 11 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCC=O)c1 10.1016/s0960-894x(00)00366-8
9974856 98881 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2ccc3ccc(N(C)C)cc3c2)c1C 10.1021/jm00004a012
CHEMBL282401 98881 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2ccc3ccc(N(C)C)cc3c2)c1C 10.1021/jm00004a012
CHEMBL343379 209943 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Inhibitory effect against porcine Endothelin A receptorInhibitory effect against porcine Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O 10.1021/jm00021a021
CHEMBL343379 209943 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O 10.1021/jm00021a021
CHEMBL315780 209436 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@H](C(=O)O)c1csc2ccccc12)[C@@H](C)CC 10.1021/jm00070a001
10334781 95551 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL25970 95551 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1C 10.1016/0960-894X(96)00441-6
18617299 203553 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1C 10.1016/0960-894X(96)00441-6
CHEMBL79054 203553 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1C 10.1016/0960-894X(96)00441-6
127028930 136767 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 570 9 3 7 6.0 CCCc1nc2c(C)cc(C(=O)Nc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3752444 136767 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 570 9 3 7 6.0 CCCc1nc2c(C)cc(C(=O)Nc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
10769025 59939 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL174171 59939 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O 10.1021/jm950592+
44384656 129560 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 5 1 7 4.5 Cc1noc(NS(=O)(=O)c2ccsc2/C=C/c2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL367763 129560 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 5 1 7 4.5 Cc1noc(NS(=O)(=O)c2ccsc2/C=C/c2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
10577111 205160 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 493 7 1 6 4.0 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)COc2ccc(F)cc2)cc1 10.1021/jm9505369
CHEMBL9084 205160 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 493 7 1 6 4.0 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)COc2ccc(F)cc2)cc1 10.1021/jm9505369
10723203 11330 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 678 14 2 7 6.8 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL1180350 11330 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 678 14 2 7 6.8 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL123206 11330 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 678 14 2 7 6.8 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
44291584 100751 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 501 8 3 9 3.5 COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)O)c1 10.1021/jm9608366
CHEMBL296074 100751 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 501 8 3 9 3.5 COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)O)c1 10.1021/jm9608366
10625875 129113 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 523 9 4 5 4.6 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
CHEMBL367313 129113 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 523 9 4 5 4.6 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
10625875 129113 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 523 9 4 5 4.6 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL367313 129113 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 523 9 4 5 4.6 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
22998447 204938 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 414 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2sccc2Oc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL89457 204938 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 414 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2sccc2Oc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
10381121 95773 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3ccc(N)cc23)c1C 10.1021/jm00004a012
CHEMBL26090 95773 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3ccc(N)cc23)c1C 10.1021/jm00004a012
10718688 183034 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 5 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(O)c2)c1Br 10.1021/jm9608366
CHEMBL48024 183034 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 5 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(O)c2)c1Br 10.1021/jm9608366
23445325 201687 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 397 5 2 6 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Cl 10.1016/S0960-894X(97)00367-3
CHEMBL65407 201687 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 397 5 2 6 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Cl 10.1016/S0960-894X(97)00367-3
10961546 96298 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm031041j
CHEMBL264543 96298 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm031041j
122272 96637 23 None -1 2 Rat 7.8 pIC50 = 7.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00008a013
CHEMBL267458 96637 23 None -1 2 Rat 7.8 pIC50 = 7.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00008a013
10961546 96298 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL264543 96298 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
44314751 160796 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 603 13 5 4 5.0 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL412602 160796 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 603 13 5 4 5.0 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
10602620 16399 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 544 10 2 6 5.4 CCCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL123997 16399 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 544 10 2 6 5.4 CCCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
10529868 163628 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 516 8 2 6 4.8 CCc1cccc(C)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL421073 163628 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 516 8 2 6 4.8 CCc1cccc(C)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
127035410 135849 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 557 8 1 8 5.7 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C#N)c1)C(=O)CCCC2 10.1039/C4MD00499J
CHEMBL3735155 135849 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 557 8 1 8 5.7 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C#N)c1)C(=O)CCCC2 10.1039/C4MD00499J
44320474 106572 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 440 8 1 5 5.7 CCC(CC)Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
CHEMBL315752 106572 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 440 8 1 5 5.7 CCC(CC)Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
10575845 11110 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 8 3.8 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
CHEMBL1178807 11110 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 8 3.8 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
CHEMBL43788 11110 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 8 3.8 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
10811595 98299 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9608366
10811595 98299 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
CHEMBL278114 98299 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9608366
CHEMBL278114 98299 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
CHEMBL328942 209560 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
10360201 95229 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1onc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00004a012
CHEMBL25816 95229 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1onc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00004a012
122272 96637 23 None -1 2 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00004a012
CHEMBL267458 96637 23 None -1 2 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00004a012
44283349 99849 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 603 13 5 4 5.0 CCCC[C@H](NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL289410 99849 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 603 13 5 4 5.0 CCCC[C@H](NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
44334053 4468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 465 5 1 5 5.5 COc1ccc([C@@H]2c3nc(-c4ccccc4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL102411 4468 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 465 5 1 5 5.5 COc1ccc([C@@H]2c3nc(-c4ccccc4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
10811595 98299 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm000349x
CHEMBL278114 98299 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm000349x
CHEMBL336563 209828 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL347948 209957 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
The inhibitory constant was evaluated against Endothelin A receptorThe inhibitory constant was evaluated against Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81219-1
11072080 11983 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 600 11 1 9 6.4 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccc3ccccc3n2)c1 10.1021/jm0102304
CHEMBL1183970 11983 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 600 11 1 9 6.4 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccc3ccccc3n2)c1 10.1021/jm0102304
CHEMBL326160 11983 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 600 11 1 9 6.4 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccc3ccccc3n2)c1 10.1021/jm0102304
155562688 174598 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 554 13 2 10 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL4570529 174598 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 554 13 2 10 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
22616258 104914 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 372 5 1 4 3.8 CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL311781 104914 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 372 5 1 4 3.8 CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
10740943 201706 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 422 5 2 6 3.2 CNc1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12 10.1021/jm9604585
CHEMBL6555 201706 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 422 5 2 6 3.2 CNc1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12 10.1021/jm9604585
CHEMBL67074 201911 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
Tested for its ability to inhibit the binding of [125I]ET1 to the Endothelin A receptor in porcine thoracic aorta membranes.Tested for its ability to inhibit the binding of [125I]ET1 to the Endothelin A receptor in porcine thoracic aorta membranes.
ChEMBL 646 8 2 13 5.8 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC(=O)C2=C(C)N=C(C)/C(=C(/O)OC)[C@@H]2c2cccc([N+](=O)[O-])c2)[C@@H]1c1cccc([N+](=O)[O-])c1 10.1016/S0960-894X(01)81025-8
122272 96637 23 None 1 2 Human 6.8 pIC50 = 6.8 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00029a001
CHEMBL267458 96637 23 None 1 2 Human 6.8 pIC50 = 6.8 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00029a001
10095393 97096 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 452 5 3 5 5.3 Cc1noc(NS(=O)(=O)c2cccc3c(N/C(S)=N/c4ccccc4)cccc23)c1C 10.1021/jm00008a013
CHEMBL27063 97096 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 452 5 3 5 5.3 Cc1noc(NS(=O)(=O)c2cccc3c(N/C(S)=N/c4ccccc4)cccc23)c1C 10.1021/jm00008a013
10576863 8189 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 484 5 1 6 5.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)c(Cl)c2)cc1 10.1021/jm9606507
CHEMBL10926 8189 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 484 5 1 6 5.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)c(Cl)c2)cc1 10.1021/jm9606507
44279338 106199 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 487 11 6 4 2.3 CC(C)C[C@H](NC(=O)NC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31436 106199 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 487 11 6 4 2.3 CC(C)C[C@H](NC(=O)NC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
44279309 161256 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 412 3 2 3 4.5 Cc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
CHEMBL414408 161256 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 412 3 2 3 4.5 Cc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
10641986 205495 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 356 6 1 4 4.2 N#Cc1ccc(OCc2cccnc2)cc1/C=C(/C(=O)O)c1ccccc1 10.1021/jm970847e
CHEMBL92842 205495 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 356 6 1 4 4.2 N#Cc1ccc(OCc2cccnc2)cc1/C=C(/C(=O)O)c1ccccc1 10.1021/jm970847e
44266646 98100 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/s0960-894x(97)10151-2
CHEMBL276638 98100 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/s0960-894x(97)10151-2
10087191 101354 1 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C 10.1021/jm00004a012
CHEMBL30039 101354 1 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C 10.1021/jm00004a012
CHEMBL424227 211564 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00349-X
44334084 109152 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 461 7 2 6 3.8 COc1ccc([C@@H]2c3nc(CCC(=O)O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL322434 109152 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 461 7 2 6 3.8 COc1ccc([C@@H]2c3nc(CCC(=O)O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
122272 96637 23 None 1 2 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm030480f
CHEMBL267458 96637 23 None 1 2 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm030480f
44266646 98100 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1021/jm0300429
CHEMBL276638 98100 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1021/jm0300429
CHEMBL137671 206995 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL335128 209789 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44371429 48621 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 455 6 1 6 5.2 COc1cccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1 10.1016/s0960-894x(99)00040-2
CHEMBL155973 48621 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 455 6 1 6 5.2 COc1cccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1 10.1016/s0960-894x(99)00040-2
44316993 203221 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL76360 203221 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
10650477 113737 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 10 2 6 5.8 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC(C)C)cc1 10.1021/jm990170q
CHEMBL333009 113737 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 10 2 6 5.8 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC(C)C)cc1 10.1021/jm990170q
44298356 193305 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 503 10 2 8 5.7 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC/C=N/O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54703 193305 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 503 10 2 8 5.7 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC/C=N/O)c1 10.1016/s0960-894x(00)00366-8
10983585 172693 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 473 9 2 8 3.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4525321 172693 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 473 9 2 8 3.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO 10.1016/j.bmcl.2016.06.014
66875612 174690 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 495 10 2 10 2.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4572634 174690 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 495 10 2 10 2.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1016/j.bmcl.2016.06.014
10693981 59223 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 431 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL171702 59223 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 431 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
15340612 106336 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 406 5 1 5 3.6 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144599 106336 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 406 5 1 5 3.6 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
10744921 59723 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 536 10 5 4 4.6 CCc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
CHEMBL173666 59723 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 536 10 5 4 4.6 CCc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
44299023 194813 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 457 6 1 6 4.7 CCc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL56343 194813 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 457 6 1 6 4.7 CCc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
44332577 4623 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 341 3 0 4 4.4 O=CC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
CHEMBL103484 4623 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 341 3 0 4 4.4 O=CC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
44266540 4821 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 447 6 1 7 4.8 COc1ccc2c(c1)c(-c1ccc(OC)c(OC)c1)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10457 4821 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 447 6 1 7 4.8 COc1ccc2c(c1)c(-c1ccc(OC)c(OC)c1)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
44266549 161805 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 415 4 1 6 4.5 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL416518 161805 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 415 4 1 6 4.5 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
19432649 202773 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 487 9 2 8 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCO 10.1016/S0960-894X(97)00400-9
CHEMBL72473 202773 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 487 9 2 8 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCO 10.1016/S0960-894X(97)00400-9
CHEMBL342215 209907 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2cn(C(=O)OC(C)(C)C)c3ccccc23)NC1=O 10.1021/jm00021a021
44279349 167573 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 448 3 2 3 5.3 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cccc4ccccc34)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL433039 167573 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 448 3 2 3 5.3 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cccc4ccccc34)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL336087 209821 0 None - 0 Pig 4.8 pIC50 = 4.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm00021a021
44386537 127275 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 532 10 4 7 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccnc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL366391 127275 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 532 10 4 7 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccnc2)nc1C(=O)O 10.1021/jm950592+
10188517 61422 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 582 9 2 10 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL177203 61422 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 582 9 2 10 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
10122442 130162 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 660 14 2 11 5.6 CCCCNC(=O)OCC#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368383 130162 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 660 14 2 11 5.6 CCCCNC(=O)OCC#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10832511 201704 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 362 4 1 5 3.2 CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Cl)cn3)cccc12 10.1021/jm9604585
CHEMBL6553 201704 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 362 4 1 5 3.2 CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Cl)cn3)cccc12 10.1021/jm9604585
104865 697 94 None 1 4 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
3494 697 94 None 1 4 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
392 697 94 None 1 4 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
CHEMBL957 697 94 None 1 4 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
DB00559 697 94 None 1 4 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstrictionAntagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
10569313 96742 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 342 4 1 5 2.8 Cc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1 10.1021/jm9604585
CHEMBL268387 96742 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 342 4 1 5 2.8 Cc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1 10.1021/jm9604585
5018984 201431 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 405 4 1 4 3.9 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)cn3)cccc12 10.1021/jm9604585
CHEMBL6411 201431 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 405 4 1 4 3.9 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)cn3)cccc12 10.1021/jm9604585
10690058 201498 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 362 4 1 5 3.2 CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Cl)cn3)cccc12 10.1021/jm9604585
CHEMBL6433 201498 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 362 4 1 5 3.2 CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Cl)cn3)cccc12 10.1021/jm9604585
5017966 201566 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 341 4 1 4 3.4 Cc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nc1 10.1021/jm9604585
CHEMBL6463 201566 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 341 4 1 4 3.4 Cc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nc1 10.1021/jm9604585
23445285 111871 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 454 7 1 5 5.6 CCCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL329560 111871 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 454 7 1 5 5.6 CCCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
10250826 98635 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 407 5 1 5 4.7 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1-c1ccccc1 10.1021/jm00008a013
CHEMBL280823 98635 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 407 5 1 5 4.7 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1-c1ccccc1 10.1021/jm00008a013
9980084 101650 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 429 10 1 5 5.7 CCCCN(CCCC)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL30245 101650 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 429 10 1 5 5.7 CCCCN(CCCC)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
9852624 128146 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 656 14 2 11 4.5 CCS(=O)(=O)NCCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL366872 128146 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 656 14 2 11 4.5 CCS(=O)(=O)NCCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
10744040 113057 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1 10.1021/jm031041j
CHEMBL332231 113057 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1 10.1021/jm031041j
10815726 11328 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 516 8 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL1180348 11328 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 516 8 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL123146 11328 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 516 8 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2C)cc1 10.1021/jm990171i
10671649 98101 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 460 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL276639 98101 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 460 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
10299975 109752 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(C)CC 10.1021/jm980217s
CHEMBL323791 109752 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(C)CC 10.1021/jm980217s
10816152 16142 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 534 9 2 8 3.9 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(OC)cccc2OC)cc1 10.1021/jm990170q
CHEMBL122832 16142 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 534 9 2 8 3.9 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(OC)cccc2OC)cc1 10.1021/jm990170q
10744040 113057 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1 10.1021/jm990170q
CHEMBL332231 113057 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1 10.1021/jm990170q
10552344 58888 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 471 7 1 6 5.1 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1C(F)(F)F 10.1021/jm990378b
CHEMBL170202 58888 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 471 7 1 6 5.1 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1C(F)(F)F 10.1021/jm990378b
44295156 14443 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 520 10 1 9 4.7 COc1ccccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1 10.1016/s0960-894x(98)00301-1
CHEMBL1205062 14443 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 520 10 1 9 4.7 COc1ccccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1 10.1016/s0960-894x(98)00301-1
CHEMBL48411 14443 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 520 10 1 9 4.7 COc1ccccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1 10.1016/s0960-894x(98)00301-1
10231591 130825 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 569 10 2 11 2.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL368828 130825 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 569 10 2 11 2.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
10338502 118957 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2c(S(=O)(=O)Nc3noc(C)c3C)cccc12 10.1021/jm00004a012
CHEMBL345247 118957 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2c(S(=O)(=O)Nc3noc(C)c3C)cccc12 10.1021/jm00004a012
44386370 60079 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 531 10 4 6 4.8 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL175066 60079 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 531 10 4 6 4.8 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O 10.1021/jm950592+
15453177 203800 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL80857 203800 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
10601795 96511 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 10 1 6 4.4 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CC(C)C)CC(C)C)cc1 10.1021/jm9505369
CHEMBL266354 96511 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 10 1 6 4.4 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CC(C)C)CC(C)C)cc1 10.1021/jm9505369
44265869 96800 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 466 7 2 6 3.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2CCCC2)cc1 10.1021/jm9505369
CHEMBL268864 96800 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 466 7 2 6 3.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2CCCC2)cc1 10.1021/jm9505369
44278003 98798 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 449 8 1 6 5.6 COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL28188 98798 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 449 8 1 6 5.6 COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
18617302 103924 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccccc2F)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL310361 103924 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccccc2F)c1Br 10.1016/0960-894X(96)00441-6
15453180 104733 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 348 4 1 4 4.1 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Cl 10.1016/0960-894X(96)00441-6
CHEMBL311510 104733 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 348 4 1 4 4.1 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Cl 10.1016/0960-894X(96)00441-6
10951244 201255 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cc(OC)ccc1OC)O2 10.1021/jm010382z
CHEMBL62962 201255 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cc(OC)ccc1OC)O2 10.1021/jm010382z
11100307 201502 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 354 5 1 5 3.8 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL64340 201502 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 354 5 1 5 3.8 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
44314461 203061 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 605 13 5 4 3.9 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCC1)C(=O)O 10.1021/jm9600914
CHEMBL74837 203061 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 605 13 5 4 3.9 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCC1)C(=O)O 10.1021/jm9600914
10767778 16210 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)cc(C)c2)cc1 10.1021/jm990170q
CHEMBL123077 16210 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)cc(C)c2)cc1 10.1021/jm990170q
44295114 14696 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 556 11 1 9 5.3 COc1cc(C/C(C(=O)c2ccc(OC(F)F)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1207717 14696 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 556 11 1 9 5.3 COc1cc(C/C(C(=O)c2ccc(OC(F)F)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL433090 14696 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 556 11 1 9 5.3 COc1cc(C/C(C(=O)c2ccc(OC(F)F)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
122044 10063 47 None - 0 Pig 6.8 pIC50 = 6.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1021/jm0102304
CHEMBL115951 10063 47 None - 0 Pig 6.8 pIC50 = 6.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1021/jm0102304
44309814 102519 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 487 8 1 7 6.2 CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1cc2nsnc2cc1C 10.1016/s0960-894x(97)10151-2
CHEMBL306863 102519 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 487 8 1 7 6.2 CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1cc2nsnc2cc1C 10.1016/s0960-894x(97)10151-2
44327380 111101 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 457 6 1 9 1.4 COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C)ccc2=O)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL328311 111101 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 457 6 1 9 1.4 COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C)ccc2=O)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL136634 206988 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm00021a021
CHEMBL337031 209834 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL342840 209938 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10926281 102272 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@H](c1ccc3c(c1)OCO3)O2 10.1021/jm031041j
CHEMBL305117 102272 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@H](c1ccc3c(c1)OCO3)O2 10.1021/jm031041j
10926281 102272 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@H](c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL305117 102272 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@H](c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
11026419 201483 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3c(OC)cccc32)cc1 10.1021/jm010382z
CHEMBL64266 201483 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3c(OC)cccc32)cc1 10.1021/jm010382z
44368819 168315 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL 1637 31 19 20 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
77282140 168315 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL 1637 31 19 20 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL438380 168315 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL 1637 31 19 20 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
44270524 97742 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 682 13 1 9 6.9 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccccc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL274243 97742 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 682 13 1 9 6.9 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccccc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
44267002 98094 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 546 5 1 7 5.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3c2CCc2ccccc2C3=O)cc1 10.1021/jm9606507
CHEMBL276601 98094 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 546 5 1 7 5.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3c2CCc2ccccc2C3=O)cc1 10.1021/jm9606507
10627398 130152 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 599 11 4 5 5.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)o1 10.1021/jm950591h
CHEMBL368339 130152 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 599 11 4 5 5.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)o1 10.1021/jm950591h
10841170 11998 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL1184090 11998 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL332109 11998 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
10579647 167902 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 612 11 4 5 5.8 Cc1c(C(=O)O)nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)n1Cc1ccccc1 10.1021/jm950592+
CHEMBL435156 167902 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 612 11 4 5 5.8 Cc1c(C(=O)O)nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)n1Cc1ccccc1 10.1021/jm950592+
10575061 205156 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 439 9 1 6 4.0 CCCCC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9082 205156 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 439 9 1 6 4.0 CCCCC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10646637 205309 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 437 8 1 5 4.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C/C=C/CC(C)C)cc1 10.1021/jm9505369
CHEMBL9168 205309 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 437 8 1 5 4.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C/C=C/CC(C)C)cc1 10.1021/jm9505369
44368416 44425 0 None - 0 Pig 4.8 pIC50 = 4.8 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 540 8 2 6 5.6 O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)Cc1cc2c(cc1Cl)OCO2 10.1016/s0960-894x(01)00009-9
CHEMBL152098 44425 0 None - 0 Pig 4.8 pIC50 = 4.8 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 540 8 2 6 5.6 O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)Cc1cc2c(cc1Cl)OCO2 10.1016/s0960-894x(01)00009-9
10478562 131263 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
CHEMBL369359 131263 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
127026043 136815 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 607 11 3 9 3.8 CCCc1nc2c(C)cc(C(=O)NCCN3CCOCC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3752947 136815 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 607 11 3 9 3.8 CCCc1nc2c(C)cc(C(=O)NCCN3CCOCC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
44386162 60073 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 575 11 1 9 6.2 CC/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL175005 60073 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 575 11 1 9 6.2 CC/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10503334 172762 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 441 5 2 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br 10.1016/S0960-894X(97)00367-3
CHEMBL45269 172762 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 441 5 2 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br 10.1016/S0960-894X(97)00367-3
10503334 172762 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 5 2 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br 10.1021/jm9608366
CHEMBL45269 172762 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 5 2 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br 10.1021/jm9608366
10140871 58924 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 484 9 2 9 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)ncnc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL170342 58924 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 484 9 2 9 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)ncnc1OCC#CCO 10.1016/s0960-894x(02)01084-3
44383754 59554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 452 5 1 5 5.4 Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL172987 59554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 452 5 1 5 5.4 Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL319660 209464 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
11005243 201681 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL65337 201681 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
9801093 58909 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 399 7 1 5 5.1 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
CHEMBL170296 58909 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 399 7 1 5 5.1 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
44295089 14448 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 476 8 1 7 5.4 COc1ccc(C(=O)/C(Cc2ccc(SC)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205088 14448 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 476 8 1 7 5.4 COc1ccc(C(=O)/C(Cc2ccc(SC)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL51030 14448 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 476 8 1 7 5.4 COc1ccc(C(=O)/C(Cc2ccc(SC)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44320192 106560 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 480 6 1 5 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1cccc(Cl)c1 10.1016/s0960-894x(00)00513-8
CHEMBL315622 106560 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 480 6 1 5 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1cccc(Cl)c1 10.1016/s0960-894x(00)00513-8
10504542 178973 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 469 6 2 6 4.4 CCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL47418 178973 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 469 6 2 6 4.4 CCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
44386536 130178 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2F)nc1C(=O)O 10.1021/jm950592+
CHEMBL368461 130178 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2F)nc1C(=O)O 10.1021/jm950592+
10626245 130627 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 539 10 2 8 5.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)OC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL368629 130627 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 539 10 2 8 5.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)OC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
44311516 202409 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 678 12 2 12 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70339 202409 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 678 12 2 12 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
137633242 155927 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 569 10 2 10 3.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4067475 155927 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 569 10 2 10 3.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10599230 205257 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9141 205257 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
71458718 81248 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 615 14 1 12 4.3 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C)cn1 10.1021/jm3009103
CHEMBL2163700 81248 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 615 14 1 12 4.3 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C)cn1 10.1021/jm3009103
44320783 106198 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccnc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL314357 106198 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccnc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
18995986 99107 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 537 8 1 10 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL283858 99107 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 537 8 1 10 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
18617379 203503 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 364 3 1 4 3.5 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78669 203503 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 364 3 1 4 3.5 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1Br 10.1016/0960-894X(96)00441-6
10622616 7960 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 5 1 6 4.5 CSc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10911 7960 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 5 1 6 4.5 CSc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10412464 9034 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 470 6 1 5 5.4 COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL10996 9034 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 470 6 1 5 5.4 COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
11826883 198457 1 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 476 8 1 6 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)c(OC)c3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL59635 198457 1 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 476 8 1 6 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)c(OC)c3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
11017198 108513 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 563 12 1 8 6.0 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOCc2ccccc2)c1 10.1021/jm0102304
CHEMBL321226 108513 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 563 12 1 8 6.0 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOCc2ccccc2)c1 10.1021/jm0102304
10765567 110853 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 440 9 1 5 3.4 CCCN(C)C(=O)CN1C[C@H](c2cccc(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL326951 110853 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 440 9 1 5 3.4 CCCN(C)C(=O)CN1C[C@H](c2cccc(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
9870117 193207 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 488 10 1 7 5.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1 10.1016/j.bmcl.2016.06.014
CHEMBL54057 193207 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 488 10 1 7 5.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1 10.1016/j.bmcl.2016.06.014
9870117 193207 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 488 10 1 7 5.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54057 193207 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 488 10 1 7 5.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1 10.1016/s0960-894x(00)00366-8
44277367 106342 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 392 4 2 5 3.3 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144606 106342 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 392 4 2 5 3.3 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(O)c1 10.1016/s0960-894x(00)00232-8
44387128 168013 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 558 12 2 10 3.8 CNCC(=O)OCCOc1nc(C)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/S0960-894X(97)00400-9
CHEMBL435895 168013 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 558 12 2 10 3.8 CNCC(=O)OCCOc1nc(C)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/S0960-894X(97)00400-9
CHEMBL422464 211529 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
5310990 166266 9 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL428504 166266 9 None - 1 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
23445506 112053 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 428 5 1 6 4.3 COc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL330003 112053 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 428 5 1 6 4.3 COc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
10452145 97739 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 376 5 1 7 2.9 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1[N+](=O)[O-] 10.1021/jm00008a013
CHEMBL27420 97739 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 376 5 1 7 2.9 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1[N+](=O)[O-] 10.1021/jm00008a013
10813007 112808 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 440 9 1 5 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL331577 112808 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 440 9 1 5 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
44384852 59909 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 544 9 1 8 5.5 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL174094 59909 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 544 9 1 8 5.5 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10362674 97320 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 385 4 1 5 4.2 Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCCC4)cccc23)c1C 10.1021/jm00008a013
CHEMBL27178 97320 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 385 4 1 5 4.2 Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCCC4)cccc23)c1C 10.1021/jm00008a013
10742446 205274 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 456 9 2 7 2.0 COCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9147 205274 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 456 9 2 7 2.0 COCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10650638 9079 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 566 13 1 6 4.8 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1 10.1021/jm970101g
CHEMBL110305 9079 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 566 13 1 6 4.8 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1 10.1021/jm970101g
10647898 96884 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 466 5 1 6 5.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3ccccc23)cc1 10.1021/jm9606507
CHEMBL269409 96884 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 466 5 1 6 5.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3ccccc23)cc1 10.1021/jm9606507
10993781 199654 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 434 7 1 7 5.0 CCCCC1=C(c2nnn[nH]2)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL60440 199654 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 434 7 1 7 5.0 CCCCC1=C(c2nnn[nH]2)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10896412 201107 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1OC)O2 10.1021/jm010382z
CHEMBL62277 201107 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1OC)O2 10.1021/jm010382z
15410997 4625 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 563 8 1 7 6.3 COc1ccc(C2(OC(=O)N[C@@H](C)c3ccccc3)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL103501 4625 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 563 8 1 7 6.3 COc1ccc(C2(OC(=O)N[C@@H](C)c3ccccc3)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL2370534 208114 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](N)Cc2ccccc2)C(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm990170q
151174 201023 37 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
ChEMBL 605 12 3 13 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL61780 201023 37 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
ChEMBL 605 12 3 13 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO 10.1016/j.bmcl.2016.06.014
76319370 84918 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 564 8 1 9 4.0 CCOC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1007/s00044-004-0021-y
CHEMBL2261602 84918 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 564 8 1 9 4.0 CCOC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1007/s00044-004-0021-y
10050696 96317 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 476 7 1 6 5.3 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL26474 96317 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 476 7 1 6 5.3 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00513-8
10050696 96317 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 476 7 1 6 5.3 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL26474 96317 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 476 7 1 6 5.3 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00232-8
10138169 98889 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 440 6 1 8 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL282470 98889 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 440 6 1 8 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
10211772 56214 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 660 11 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL163638 56214 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 660 11 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
10165809 131264 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 541 9 2 11 2.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL369362 131264 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 541 9 2 11 2.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL61900 214054 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00349-X
44327412 205837 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL94929 205837 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44385621 127661 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O 10.1021/jm950592+
CHEMBL366544 127661 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O 10.1021/jm950592+
44356917 118723 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL 638 8 5 8 0.3 CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2cn(C=O)c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL343516 118723 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL 638 8 5 8 0.3 CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2cn(C=O)c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL2370825 208173 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2C[C@@H](O)CN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
11091217 100585 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cc(OCCC)ccc21 10.1021/jm010382z
CHEMBL294787 100585 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cc(OCCC)ccc21 10.1021/jm010382z
44314722 155198 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 597 14 5 4 4.9 CCCCC(NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL405724 155198 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 597 14 5 4 4.9 CCCCC(NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL293216 209134 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00349-X
44283421 99681 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 597 14 5 4 4.9 CCCC[C@H](NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL287888 99681 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 597 14 5 4 4.9 CCCC[C@H](NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
44383742 167929 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 452 5 1 5 5.4 Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL435346 167929 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 452 5 1 5 5.4 Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL137361 206992 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL313382 209357 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL86814 214105 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
44368819 168315 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL 1637 31 19 20 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
77282140 168315 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL 1637 31 19 20 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL438380 168315 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL 1637 31 19 20 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
44316973 203883 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL81593 203883 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1C 10.1016/0960-894X(96)00441-6
127035067 135856 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 683 12 2 9 5.4 CCCc1nc2c(C)cc(C(=O)NCCN3CCN(C)CC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3735236 135856 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 683 12 2 9 5.4 CCCc1nc2c(C)cc(C(=O)NCCN3CCN(C)CC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
44368824 96366 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL 1595 31 19 20 0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
77282142 96366 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL 1595 31 19 20 0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL265164 96366 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL 1595 31 19 20 0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL436899 211936 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
44277034 106347 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 406 5 1 5 3.6 COc1ccccc1Cn1[nH]c(C(F)(F)F)c(Cc2ccc3c(c2)OCO3)c1=O 10.1016/s0960-894x(00)00232-8
CHEMBL3144729 106347 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 406 5 1 5 3.6 COc1ccccc1Cn1[nH]c(C(F)(F)F)c(Cc2ccc3c(c2)OCO3)c1=O 10.1016/s0960-894x(00)00232-8
CHEMBL1791279 207166 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)[C@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
19735343 175467 0 None - 1 Human 4.8 pIC50 = 4.8 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 473 7 2 6 4.0 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4590568 175467 0 None - 1 Human 4.8 pIC50 = 4.8 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 473 7 2 6 4.0 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2016.06.014
23445516 106133 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 468 7 1 5 5.9 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CCC(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL314307 106133 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 468 7 1 5 5.9 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CCC(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
23445354 204899 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 426 5 1 5 4.8 CCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL89203 204899 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 426 5 1 5 4.8 CCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL273391 209054 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL273391 209054 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
18184206 59998 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 600 13 2 11 3.2 CCS(=O)(=O)NCCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL174413 59998 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 600 13 2 11 3.2 CCS(=O)(=O)NCCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
44385792 60017 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 617 13 2 11 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL174547 60017 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 617 13 2 11 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
44384966 59667 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 545 9 1 9 4.8 C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL173465 59667 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 545 9 1 9 4.8 C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
71460537 81271 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 660 12 1 13 2.7 COc1ccccc1Oc1c(NS(=O)(=O)N2CCOCC2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163722 81271 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 660 12 1 13 2.7 COc1ccccc1Oc1c(NS(=O)(=O)N2CCOCC2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
10765057 162598 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 430 4 1 7 3.5 O=C1OC(O)(c2ccc3c(c2)OCO3)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL417978 162598 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 430 4 1 7 3.5 O=C1OC(O)(c2ccc3c(c2)OCO3)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL2304012 207713 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC1=O 10.1021/jm9600914
44458399 98522 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 520 7 2 7 4.2 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL279947 98522 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 520 7 2 7 4.2 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1 10.1016/s0960-894x(01)00660-6
73669992 117115 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 387 9 1 4 5.4 N#CCCC(Oc1cc(OCc2ccccc2)ccc1C(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400998 117115 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 387 9 1 4 5.4 N#CCCC(Oc1cc(OCc2ccccc2)ccc1C(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
10814776 99001 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9608366
10814776 99001 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL283136 99001 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9608366
CHEMBL283136 99001 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
44387111 165618 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 548 10 5 5 4.2 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL426413 165618 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 548 10 5 5 4.2 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
9830773 129691 0 None - 2 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 636 14 2 12 2.8 CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL367958 129691 0 None - 2 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 636 14 2 12 2.8 CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
10814776 99001 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm000349x
CHEMBL283136 99001 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm000349x
CHEMBL341994 209905 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C2=CCC=CC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10410546 9307 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL11162 9307 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
44279481 111877 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 555 11 5 4 4.0 CC(C)C[C@H](NC(=O)N1C(C)(C)CCCC1(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL32959 111877 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 555 11 5 4 4.0 CC(C)C[C@H](NC(=O)N1C(C)(C)CCCC1(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
10674095 113001 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 544 9 1 6 5.1 CCc1cccc(CC)c1N(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL332093 113001 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 544 9 1 6 5.1 CCc1cccc(CC)c1N(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL135906 206982 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44316983 104304 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 312 5 1 6 2.1 COc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1OC 10.1016/0960-894X(96)00441-6
CHEMBL310944 104304 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 312 5 1 6 2.1 COc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1OC 10.1016/0960-894X(96)00441-6
44371670 141119 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor
ChEMBL 1082 23 11 10 3.7 CC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1c2ccccc2CCc2ccccc21 10.1016/0960-894X(95)00084-7
CHEMBL385405 141119 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor
ChEMBL 1082 23 11 10 3.7 CC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1c2ccccc2CCc2ccccc21 10.1016/0960-894X(95)00084-7
44277035 106356 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 410 4 1 4 4.2 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(Cl)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144806 106356 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 410 4 1 4 4.2 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(Cl)c1 10.1016/s0960-894x(00)00232-8
10554385 59884 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 537 10 4 5 4.8 CCc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
CHEMBL174000 59884 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 537 10 4 5 4.8 CCc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
10721963 60220 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 580 11 5 6 3.7 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)NCC(=O)O 10.1021/jm950592+
CHEMBL175924 60220 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 580 11 5 6 3.7 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)NCC(=O)O 10.1021/jm950592+
44386620 170028 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccc(F)cc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL445076 170028 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccc(F)cc2)nc1C(=O)O 10.1021/jm950592+
44311218 102639 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccncc1 10.1016/S0960-894X(97)00400-9
CHEMBL307803 102639 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccncc1 10.1016/S0960-894X(97)00400-9
18617344 203557 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 361 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL79080 203557 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 361 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1Br 10.1016/0960-894X(96)00441-6
15342056 205275 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 322 3 1 5 2.6 Cc1noc(NS(=O)(=O)c2cccs2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL91470 205275 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 322 3 1 5 2.6 Cc1noc(NS(=O)(=O)c2cccs2)c1Br 10.1016/S0960-894X(96)00496-9
10503976 11119 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N(C)c2ccccc2)c1Br 10.1021/jm9608366
CHEMBL1178874 11119 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N(C)c2ccccc2)c1Br 10.1021/jm9608366
CHEMBL47536 11119 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N(C)c2ccccc2)c1Br 10.1021/jm9608366
10211543 130850 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 640 13 2 12 3.5 CCCCNC(=O)OCC#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368989 130850 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 640 13 2 12 3.5 CCCCNC(=O)OCC#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10341117 162634 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 403 8 3 6 3.5 Cc1noc(NS(=O)(=O)c2cccc3c(NCCCC(=O)O)cccc23)c1C 10.1021/jm00008a013
CHEMBL418202 162634 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 403 8 3 6 3.5 Cc1noc(NS(=O)(=O)c2cccc3c(NCCCC(=O)O)cccc23)c1C 10.1021/jm00008a013
10554085 100804 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 524 6 1 9 3.2 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N2CCN(Cc3ccc4c(c3)OCO4)CC2)c1Cl 10.1021/jm9700068
CHEMBL296427 100804 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 524 6 1 9 3.2 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)N2CCN(Cc3ccc4c(c3)OCO4)CC2)c1Cl 10.1021/jm9700068
10817024 12007 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 578 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1184112 12007 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 578 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL332808 12007 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 578 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
44279140 110130 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 588 12 2 6 5.8 CCCCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL32574 110130 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 588 12 2 6 5.8 CCCCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
11793037 202003 3 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 362 4 1 5 3.2 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)nn3)cccc12 10.1021/jm9604585
CHEMBL6761 202003 3 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 362 4 1 5 3.2 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)nn3)cccc12 10.1021/jm9604585
9885296 96508 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 361 4 1 4 3.8 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)cn3)cccc12 10.1021/jm9604585
CHEMBL266315 96508 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 361 4 1 4 3.8 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)cn3)cccc12 10.1021/jm9604585
10786783 201734 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 393 4 1 5 3.2 COc1nc(Br)cnc1NS(=O)(=O)c1cccc2ccccc12 10.1021/jm9604585
CHEMBL6576 201734 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 393 4 1 5 3.2 COc1nc(Br)cnc1NS(=O)(=O)c1cccc2ccccc12 10.1021/jm9604585
10740137 201810 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 406 4 1 5 3.3 CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)cn3)cccc12 10.1021/jm9604585
CHEMBL6630 201810 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 406 4 1 5 3.3 CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)cn3)cccc12 10.1021/jm9604585
10230836 8806 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 546 13 1 7 4.1 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL109765 8806 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 546 13 1 7 4.1 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
10209319 9265 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 546 13 1 7 4.1 CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC 10.1021/jm970101g
CHEMBL111355 9265 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 546 13 1 7 4.1 CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC 10.1021/jm970101g
10507211 109869 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 566 13 1 7 3.9 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL324214 109869 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 566 13 1 7 3.9 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCCCl 10.1021/jm970101g
9807691 99589 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 553 10 1 10 5.3 COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL287169 99589 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 553 10 1 10 5.3 COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
11732669 201418 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCC)cc21 10.1021/jm010382z
CHEMBL64039 201418 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCC)cc21 10.1021/jm010382z
10602267 8486 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 529 13 1 6 3.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCCC1=O 10.1021/jm980217s
CHEMBL109478 8486 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 529 13 1 6 3.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCCC1=O 10.1021/jm980217s
44332842 109220 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 703 11 1 10 7.5 COc1ccc(C2(OC(=O)N[C@@H](C)c3cccc4ccccc34)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL322920 109220 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 703 11 1 10 7.5 COc1ccc(C2(OC(=O)N[C@@H](C)c3cccc4ccccc34)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/S0960-894X(97)00002-4
44315009 102718 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 665 13 5 5 4.7 CSCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL308403 102718 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 665 13 5 5 4.7 CSCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
10791702 194133 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL558148 194133 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
9895957 10558 12 None 3 3 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1039/C4MD00499J
CHEMBL11706 10558 12 None 3 3 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1039/C4MD00499J
21041288 173344 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 526 10 2 9 2.8 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4540866 173344 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 526 10 2 9 2.8 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
155563100 174694 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 619 13 2 10 4.6 COc1cnc(OCCOc2nc(-c3ccncc3)nc(NS(=O)(=O)NCc3ccccc3)c2-c2ccc(Cl)cc2)nc1 10.1016/j.bmcl.2016.06.014
CHEMBL4572734 174694 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 619 13 2 10 4.6 COc1cnc(OCCOc2nc(-c3ccncc3)nc(NS(=O)(=O)NCc3ccccc3)c2-c2ccc(Cl)cc2)nc1 10.1016/j.bmcl.2016.06.014
9829478 174743 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 567 10 1 8 4.9 Cc1ccc(-c2c(NS(=O)(=O)/C=C/c3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4573806 174743 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 567 10 1 8 4.9 Cc1ccc(-c2c(NS(=O)(=O)/C=C/c3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
10146377 60078 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 662 11 2 14 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
CHEMBL175058 60078 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 662 11 2 14 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
10816682 101658 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 559 10 1 9 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCOCC3)c2)cc1 10.1021/jm980504w
CHEMBL302493 101658 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 559 10 1 9 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCOCC3)c2)cc1 10.1021/jm980504w
10579885 102221 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 632 12 1 11 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN3CCN(C)CC3)c2)cc1 10.1021/jm980504w
CHEMBL304802 102221 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 632 12 1 11 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN3CCN(C)CC3)c2)cc1 10.1021/jm980504w
10814440 97682 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)ccc2OC)cc1 10.1021/jm9606507
CHEMBL273723 97682 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)ccc2OC)cc1 10.1021/jm9606507
71462247 81272 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2cnccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163723 81272 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2cnccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
23548253 81250 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 679 14 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL2163702 81250 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 679 14 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
11014820 201214 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 398 6 1 6 4.2 CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL62780 201214 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 398 6 1 6 4.2 CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10602183 9134 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 525 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1ccccc1=O 10.1021/jm980217s
CHEMBL110695 9134 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 525 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1ccccc1=O 10.1021/jm980217s
10625152 109957 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 498 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccoc1 10.1021/jm980217s
CHEMBL324685 109957 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 498 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccoc1 10.1021/jm980217s
90766557 169950 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 528 10 2 8 3.1 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4449731 169950 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 528 10 2 8 3.1 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
76312118 84909 0 None 691 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261361 84909 0 None 691 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
9916121 81241 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 571 10 1 8 4.1 CCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2163693 81241 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 571 10 1 8 4.1 CCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
23548253 81250 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 679 14 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163702 81250 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 679 14 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
44334130 4427 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 458 5 1 6 4.4 COc1ccc([C@@H]2c3nc(N4CCCC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL102173 4427 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 458 5 1 6 4.4 COc1ccc([C@@H]2c3nc(N4CCCC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
9808602 108709 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 590 15 1 8 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1 10.1021/jm970101g
CHEMBL321673 108709 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 590 15 1 8 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1 10.1021/jm970101g
11826062 201291 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 8 2 6 4.3 CC(C)Oc1ccc2c(c1)C(CCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL63113 201291 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 8 2 6 4.3 CC(C)Oc1ccc2c(c1)C(CCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10696876 109834 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 504 13 1 7 3.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCO1 10.1021/jm980217s
CHEMBL323989 109834 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 504 13 1 7 3.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCO1 10.1021/jm980217s
22467235 96065 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 533 7 2 7 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL262784 96065 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 533 7 2 7 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
22467235 96065 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 533 7 2 7 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1007/s00044-004-0021-y
CHEMBL262784 96065 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 533 7 2 7 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1007/s00044-004-0021-y
71462321 81581 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 584 12 2 8 4.2 CCc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL2165335 81581 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 584 12 2 8 4.2 CCc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
9890440 8155 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 460 6 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1 10.1021/jm9606507
CHEMBL10924 8155 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 460 6 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1 10.1021/jm9606507
10577306 109187 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 499 13 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ncco1 10.1021/jm980217s
CHEMBL322732 109187 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 499 13 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ncco1 10.1021/jm980217s
44315007 202833 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 679 14 5 5 5.1 CCCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL72891 202833 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 679 14 5 5 5.1 CCCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
21041273 173166 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 538 12 2 9 2.8 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4536769 173166 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 538 12 2 9 2.8 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
9821701 4529 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 389 4 1 5 3.8 COc1ccc([C@@H]2c3ncccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL102825 4529 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 389 4 1 5 3.8 COc1ccc([C@@H]2c3ncccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
10698065 11992 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 558 11 2 6 5.6 CCC(CC)C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL1184065 11992 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 558 11 2 6 5.6 CCC(CC)C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL330895 11992 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 558 11 2 6 5.6 CCC(CC)C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL171198 207093 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL None None None CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)O 10.1016/0960-894X(95)00144-I
10529742 8093 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 511 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1cccn1C 10.1021/jm980217s
CHEMBL109206 8093 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 511 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1cccn1C 10.1021/jm980217s
10116355 8167 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 474 14 1 5 4.9 CCCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL109248 8167 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 474 14 1 5 4.9 CCCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
10648715 109168 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC(C)C 10.1021/jm980217s
CHEMBL322547 109168 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC(C)C 10.1021/jm980217s
44320291 105445 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 548 7 2 8 4.8 O=C(O)c1cc2c(c(Cn3nc(-c4ccccc4)c(Cc4cc5c(cc4Cl)OCO5)c3C(=O)O)c1)OCOC2 10.1016/s0960-894x(00)00513-8
CHEMBL312854 105445 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 548 7 2 8 4.8 O=C(O)c1cc2c(c(Cn3nc(-c4ccccc4)c(Cc4cc5c(cc4Cl)OCO5)c3C(=O)O)c1)OCOC2 10.1016/s0960-894x(00)00513-8
17885912 106602 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 496 7 2 6 5.1 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCC(C(=O)O)C1 10.1016/s0960-894x(00)00513-8
CHEMBL315936 106602 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 496 7 2 6 5.1 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCC(C(=O)O)C1 10.1016/s0960-894x(00)00513-8
44279295 105509 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 482 8 1 6 4.2 COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(=O)N(C)C)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL31324 105509 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 482 8 1 6 4.2 COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(=O)N(C)C)c1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
10670600 96115 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 436 6 2 6 3.6 CCNc1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12 10.1021/jm9604585
CHEMBL263079 96115 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 436 6 2 6 3.6 CCNc1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12 10.1021/jm9604585
10646831 183328 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 6 2 7 4.1 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9608366
10646831 183328 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 6 2 7 4.1 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9700068
CHEMBL48134 183328 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 6 2 7 4.1 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9608366
CHEMBL48134 183328 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 6 2 7 4.1 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9700068
11751754 101878 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 469 6 3 7 4.1 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)O)c1 10.1021/jm030528p
CHEMBL303806 101878 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 469 6 3 7 4.1 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)O)c1 10.1021/jm030528p
10555516 9136 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 598 12 1 7 4.6 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)Cc1ccccc1 10.1021/jm970101g
CHEMBL110700 9136 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 598 12 1 7 4.6 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)Cc1ccccc1 10.1021/jm970101g
11799503 9646 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 498 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccco1 10.1021/jm980217s
CHEMBL113472 9646 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 498 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccco1 10.1021/jm980217s
10289311 109933 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 514 13 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C=C(C)C 10.1021/jm980217s
CHEMBL324586 109933 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 514 13 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C=C(C)C 10.1021/jm980217s
CHEMBL2304007 207708 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
44380954 57357 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 643 11 1 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
CHEMBL166875 57357 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 643 11 1 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOc1ncc(Br)cn1 10.1016/s0960-894x(01)00682-5
10525281 182258 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 404 6 1 6 4.2 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1021/jm9700068
CHEMBL47915 182258 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 404 6 1 6 4.2 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1021/jm9700068
9888574 103686 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 422 4 1 4 3.9 CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL309692 103686 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 422 4 1 4 3.9 CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
11102844 201541 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 476 7 2 7 4.2 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)CO)cc32)cc1 10.1021/jm010382z
CHEMBL64536 201541 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 476 7 2 7 4.2 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)CO)cc32)cc1 10.1021/jm010382z
44314906 103090 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 607 12 6 5 3.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
CHEMBL308621 103090 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 607 12 6 5 3.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
44458670 98582 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 521 7 2 8 2.7 COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL280379 98582 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 521 7 2 8 2.7 COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
71455060 81237 1 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 614 9 1 9 2.9 O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)N1CCOCC1 10.1021/jm3009103
CHEMBL2163689 81237 1 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 614 9 1 9 2.9 O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)N1CCOCC1 10.1021/jm3009103
71451526 81249 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 635 14 1 12 4.6 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Cl)cn1 10.1021/jm3009103
CHEMBL2163701 81249 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 635 14 1 12 4.6 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Cl)cn1 10.1021/jm3009103
10875868 114450 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 619 9 1 8 5.0 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(Br)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL334263 114450 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 619 9 1 8 5.0 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(Br)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
9810190 102579 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 563 11 1 10 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN(C)C)c2)cc1 10.1021/jm980504w
CHEMBL307330 102579 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 563 11 1 10 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN(C)C)c2)cc1 10.1021/jm980504w
CHEMBL2304015 207716 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
10875239 9481 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 541 10 1 10 4.8 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccco2)nc1 10.1021/jm0102304
CHEMBL112502 9481 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 541 10 1 10 4.8 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccco2)nc1 10.1021/jm0102304
10791823 9343 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 510 12 1 6 4.7 CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)C(=O)CCC 10.1021/jm970101g
CHEMBL111783 9343 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 510 12 1 6 4.7 CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)C(=O)CCC 10.1021/jm970101g
15289330 99328 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 493 8 1 8 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL285368 99328 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 493 8 1 8 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
10361107 161487 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 5 2 5 4.1 Cc1noc(NS(=O)(=O)c2cccc3c(NC(C)C)cccc23)c1C 10.1021/jm00008a013
CHEMBL416026 161487 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 5 2 5 4.1 Cc1noc(NS(=O)(=O)c2cccc3c(NC(C)C)cccc23)c1C 10.1021/jm00008a013
44314658 203447 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 589 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL78230 203447 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 589 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
9951753 165773 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 379 7 1 5 4.7 Cc1ccccc1C(Oc1cc(OCc2ccsc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL427294 165773 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 379 7 1 5 4.7 Cc1ccccc1C(Oc1cc(OCc2ccsc2)ccc1C#N)C(=O)O 10.1021/jm990378b
11797717 205322 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 448 10 2 5 6.0 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc[nH]n1 10.1021/jm9707131
CHEMBL91753 205322 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 448 10 2 5 6.0 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc[nH]n1 10.1021/jm9707131
10668808 205422 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccncc2)ccc1C#N 10.1021/jm9707131
CHEMBL92353 205422 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccncc2)ccc1C#N 10.1021/jm9707131
10694804 206075 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 449 10 1 6 6.3 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ncco1 10.1021/jm9707131
CHEMBL96301 206075 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 449 10 1 6 6.3 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ncco1 10.1021/jm9707131
10695071 100676 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 6 4.3 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9700068
CHEMBL295477 100676 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 6 4.3 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9700068
10672494 178963 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 6 5.0 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)C)cc2)c1Br 10.1021/jm9608366
CHEMBL47417 178963 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 6 5.0 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)C)cc2)c1Br 10.1021/jm9608366
44327412 205837 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL94929 205837 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL343062 209940 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
443289 702 40 None 2 3 Human 7.7 pIC50 = 7.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL None None None None 10.1021/jm3009103
997 702 40 None 2 3 Human 7.7 pIC50 = 7.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL None None None None 10.1021/jm3009103
CHEMBL314691 702 40 None 2 3 Human 7.7 pIC50 = 7.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL None None None None 10.1021/jm3009103
DB12054 702 40 None 2 3 Human 7.7 pIC50 = 7.7 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL None None None None 10.1021/jm3009103
44320431 106460 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 526 9 2 7 4.9 O=C(O)COC1CCCCC1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
CHEMBL314973 106460 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 526 9 2 7 4.9 O=C(O)COC1CCCCC1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
10767442 130688 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 492 8 1 5 6.1 COc1ccc(C(=O)/C(Cc2ccc(-c3ccccc3)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL368668 130688 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 492 8 1 5 6.1 COc1ccc(C(=O)/C(Cc2ccc(-c3ccccc3)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL313984 209367 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL265116 208880 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
10815005 9641 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 492 6 1 6 5.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm9606507
CHEMBL11345 9641 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 492 6 1 6 5.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm9606507
10506430 113278 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 532 9 2 7 4.5 CCc1cccc(OC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL332387 113278 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 532 9 2 7 4.5 CCc1cccc(OC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
10669001 112112 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 405 6 1 6 4.6 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm970847e
CHEMBL330255 112112 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 405 6 1 6 4.6 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm970847e
10692108 167596 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 395 6 1 4 5.5 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccccc1Cl 10.1021/jm970847e
CHEMBL433201 167596 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 395 6 1 4 5.5 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccccc1Cl 10.1021/jm970847e
CHEMBL313984 209367 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
10577255 174836 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 8 2 6 5.2 CCCCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL45760 174836 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 8 2 6 5.2 CCCCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL1793926 207177 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
10769045 130682 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2(C)CCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368641 130682 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2(C)CCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL134562 206978 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL436899 211936 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL407933 210937 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)NC1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
18617284 203487 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78552 203487 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1Br 10.1016/0960-894X(96)00441-6
44314579 102431 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 580 12 5 5 3.8 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL306123 102431 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 580 12 5 5 3.8 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
10549516 109888 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 410 8 1 4 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccccc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL324301 109888 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 410 8 1 4 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccccc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
22010208 205356 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 362 9 1 3 5.3 O=C(O)CCC(Oc1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
CHEMBL91965 205356 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 362 9 1 3 5.3 O=C(O)CCC(Oc1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
10717670 205456 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 433 7 1 5 5.7 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1c(F)cccc1Cl 10.1021/jm970847e
CHEMBL92570 205456 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 433 7 1 5 5.7 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1c(F)cccc1Cl 10.1021/jm970847e
19735404 175238 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 471 9 2 7 3.5 COc1ccccc1Cc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4584753 175238 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 471 9 2 7 3.5 COc1ccccc1Cc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO 10.1016/j.bmcl.2016.06.014
10528383 11116 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 470 5 1 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL1178854 11116 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 470 5 1 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL46357 11116 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 470 5 1 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
10604797 101861 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 704 14 1 13 3.3 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OCCN3CCOCC3)c(OC)c(OCCN3CCOCC3)c2)cc1 10.1021/jm980504w
CHEMBL303712 101861 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 704 14 1 13 3.3 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OCCN3CCOCC3)c(OC)c(OCCN3CCOCC3)c2)cc1 10.1021/jm980504w
10238141 194168 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 429 5 1 6 4.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2ccccc21 10.1016/S0960-894X(97)00319-3
CHEMBL55853 194168 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 429 5 1 6 4.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2ccccc21 10.1016/S0960-894X(97)00319-3
44283270 167307 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 580 12 5 5 3.8 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL431124 167307 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 580 12 5 5 3.8 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1016/0960-894X(95)00237-N
10357554 97102 1 None - 0 Human 4.7 pIC50 = 4.7 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1021/jm00029a001
CHEMBL27065 97102 1 None - 0 Human 4.7 pIC50 = 4.7 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1021/jm00029a001
44278161 99330 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 569 10 1 8 6.9 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL285380 99330 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 569 10 1 8 6.9 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
10357554 97102 1 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1021/jm00008a013
CHEMBL27065 97102 1 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1021/jm00008a013
10495634 206180 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 316 6 1 2 4.8 OC/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
CHEMBL96836 206180 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 316 6 1 2 4.8 OC/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
44276966 106360 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 352 5 1 5 2.9 COc1cccc(Cn2[nH]c(C)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144846 106360 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 352 5 1 5 2.9 COc1cccc(Cn2[nH]c(C)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
44386894 62137 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 412 7 2 6 2.1 COc1ccc([C@@H]2[C@@H](CC(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1 10.1021/jm031041j
CHEMBL177999 62137 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 412 7 2 6 2.1 COc1ccc([C@@H]2[C@@H](CC(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1 10.1021/jm031041j
11795139 165973 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 398 6 2 6 1.8 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1 10.1021/jm9505369
CHEMBL427935 165973 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 398 6 2 6 1.8 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1 10.1021/jm9505369
10212163 129561 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 696 11 2 13 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
CHEMBL367767 129561 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 696 11 2 13 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
23445256 59858 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 7 4.1 Cc1noc(NS(=O)(=O)c2ccsc2CCc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL173982 59858 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 7 4.1 Cc1noc(NS(=O)(=O)c2ccsc2CCc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
10604119 11337 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 636 12 2 7 5.8 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL1180361 11337 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 636 12 2 7 5.8 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL123654 11337 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 636 12 2 7 5.8 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
44325305 205724 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 426 10 2 5 5.3 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(=O)O 10.1021/jm9707131
CHEMBL94279 205724 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 426 10 2 5 5.3 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(=O)O 10.1021/jm9707131
10005597 119300 0 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1 10.1021/jm031041j
CHEMBL348407 119300 0 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1 10.1021/jm031041j
10005597 119300 0 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL348407 119300 0 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL433349 211879 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44314890 104584 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 647 12 5 4 5.0 CC(C)CC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL311384 104584 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 647 12 5 4 5.0 CC(C)CC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
3539 4062 78 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 424 6 1 9 2.7 COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1 10.1016/j.bmcl.2016.06.014
9910224 4062 78 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 424 6 1 9 2.7 COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1 10.1016/j.bmcl.2016.06.014
CHEMBL1628688 4062 78 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 424 6 1 9 2.7 COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1 10.1016/j.bmcl.2016.06.014
DB06629 4062 78 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 424 6 1 9 2.7 COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1 10.1016/j.bmcl.2016.06.014
10168597 60993 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cccnc1 10.1016/s0960-894x(02)01084-3
CHEMBL176741 60993 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cccnc1 10.1016/s0960-894x(02)01084-3
10673969 61761 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 538 10 3 7 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL177546 61761 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 538 10 3 7 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
10138169 98889 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 440 6 1 8 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm000349x
CHEMBL282470 98889 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 440 6 1 8 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm000349x
CHEMBL342615 209919 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Inhibitory effect against porcine Endothelin A receptorInhibitory effect against porcine Endothelin A receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CS(=O)(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL342615 209919 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CS(=O)(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10527706 96540 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 454 8 1 6 3.1 CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL266594 96540 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 454 8 1 6 3.1 CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44439114 161069 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 993 32 2 15 7.3 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CCC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL413001 161069 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 993 32 2 15 7.3 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CCC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1 10.1016/j.bmcl.2006.10.009
18738889 87524 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 562 8 1 8 4.9 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)OC)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL23418 87524 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 562 8 1 8 4.9 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)OC)cc21 10.1016/s0960-894x(01)00660-6
10310877 202182 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 473 8 1 7 5.9 CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1016/s0960-894x(97)10151-2
CHEMBL68896 202182 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 473 8 1 7 5.9 CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1016/s0960-894x(97)10151-2
CHEMBL136210 206985 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
21462927 119724 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 500 7 1 8 5.1 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc([N+](=O)[O-])ccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL352241 119724 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 500 7 1 8 5.1 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc([N+](=O)[O-])ccc23)cc1 10.1016/s0960-894x(99)00040-2
10086660 98690 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 309 6 2 5 2.9 CCCNc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1 10.1021/jm00008a013
CHEMBL281199 98690 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 309 6 2 5 2.9 CCCNc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1 10.1021/jm00008a013
44279308 99658 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 521 12 6 4 3.3 Cc1cccc(NC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(=O)O)c1 10.1016/0960-894X(95)00221-E
CHEMBL287676 99658 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 521 12 6 4 3.3 Cc1cccc(NC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(=O)O)c1 10.1016/0960-894X(95)00221-E
44279307 107515 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 541 12 6 4 3.7 CC(C)C[C@H](NC(=O)Nc1cccc(Cl)c1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31944 107515 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 541 12 6 4 3.7 CC(C)C[C@H](NC(=O)Nc1cccc(Cl)c1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL319537 209463 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10621049 205502 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 400 6 1 3 5.6 OC/C(=C/c1cc(OCc2ccsc2)ccc1Br)c1ccccc1 10.1021/jm970847e
CHEMBL92876 205502 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 400 6 1 3 5.6 OC/C(=C/c1cc(OCc2ccsc2)ccc1Br)c1ccccc1 10.1021/jm970847e
44213278 106353 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 406 5 1 5 3.6 COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)cc1 10.1016/s0960-894x(00)00232-8
CHEMBL3144799 106353 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 406 5 1 5 3.6 COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)cc1 10.1016/s0960-894x(00)00232-8
10719007 11122 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 465 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)C(C#N)c2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL1178895 11122 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 465 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)C(C#N)c2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL48448 11122 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 465 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)C(C#N)c2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
10626054 130813 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 530 11 6 4 4.2 Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368788 130813 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 530 11 6 4 4.2 Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL1206645 206856 0 None - 0 Pig 4.7 pIC50 = 4.7 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL None None None CC(C)C[C@@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm00087a001
CHEMBL290454 206856 0 None - 0 Pig 4.7 pIC50 = 4.7 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL None None None CC(C)C[C@@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm00087a001
10742968 12240 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 469 7 1 8 4.1 Cc1noc(NS(=O)(=O)c2ccsc2C(Cc2ccc3c(c2)OCO3)N(C)C)c1Cl 10.1021/jm9700068
CHEMBL1185472 12240 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 469 7 1 8 4.1 Cc1noc(NS(=O)(=O)c2ccsc2C(Cc2ccc3c(c2)OCO3)N(C)C)c1Cl 10.1021/jm9700068
CHEMBL416453 12240 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 469 7 1 8 4.1 Cc1noc(NS(=O)(=O)c2ccsc2C(Cc2ccc3c(c2)OCO3)N(C)C)c1Cl 10.1021/jm9700068
44368481 120993 0 None - 0 Pig 4.7 pIC50 = 4.7 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 435 9 2 7 2.8 CCOC(=O)CN(Cc1cc2c(cc1Cl)OCO2)C(Cc1ccc(O)cc1)C(=O)O 10.1016/s0960-894x(01)00009-9
CHEMBL358444 120993 0 None - 0 Pig 4.7 pIC50 = 4.7 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 435 9 2 7 2.8 CCOC(=O)CN(Cc1cc2c(cc1Cl)OCO2)C(Cc1ccc(O)cc1)C(=O)O 10.1016/s0960-894x(01)00009-9
10576888 170268 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 6 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2C(=O)O)c1Br 10.1021/jm9608366
CHEMBL44539 170268 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 6 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2C(=O)O)c1Br 10.1021/jm9608366
23445284 112292 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 440 5 1 5 5.4 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(C(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL330674 112292 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 440 5 1 5 5.4 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(C(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
23445458 59966 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 5 1 7 4.5 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL174363 59966 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 5 1 7 4.5 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
5344 172891 98 None - 1 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C nan
CHEMBL453 172891 98 None - 1 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C nan
44385412 130843 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 711 14 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(Cc2ccc3c(c2)OCO3)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL368945 130843 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 711 14 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(Cc2ccc3c(c2)OCO3)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
18184249 127937 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 662 13 2 11 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL366628 127937 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 662 13 2 11 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL303185 209162 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00089a028
10696818 9544 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 502 15 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(CC)CC 10.1021/jm980217s
CHEMBL112770 9544 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 502 15 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(CC)CC 10.1021/jm980217s
CHEMBL303185 209162 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm9600914
10792711 114280 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 548 9 2 6 5.2 CCc1cc(F)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL333972 114280 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 548 9 2 6 5.2 CCc1cc(F)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
9917706 129204 0 None - 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/j.bmcl.2016.06.014
CHEMBL367444 129204 0 None - 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/j.bmcl.2016.06.014
18738881 79158 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 534 7 2 7 4.4 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(=O)O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL2114305 79158 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 534 7 2 7 4.4 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(=O)O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
443289 702 40 None 2 3 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL None None None None 10.1021/jm030528p
997 702 40 None 2 3 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL None None None None 10.1021/jm030528p
CHEMBL314691 702 40 None 2 3 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL None None None None 10.1021/jm030528p
DB12054 702 40 None 2 3 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL None None None None 10.1021/jm030528p
9886303 59210 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 383 7 1 5 4.5 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1F 10.1021/jm990378b
CHEMBL171638 59210 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 383 7 1 5 4.5 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1F 10.1021/jm990378b
44293761 168637 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 549 12 2 8 4.6 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL440853 168637 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 549 12 2 8 4.6 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10908075 11623 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 591 9 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3cccc4ccccc34)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL1181549 11623 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 591 9 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3cccc4ccccc34)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL177373 11623 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 591 9 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3cccc4ccccc34)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
10302118 60088 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 533 9 2 10 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL175111 60088 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 533 9 2 10 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
135512539 127939 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 615 11 2 13 4.4 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL366652 127939 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 615 11 2 13 4.4 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
9864880 101905 0 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 384 4 1 6 3.7 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4nsnc4c3)cccc12 10.1016/s0960-894x(97)10151-2
CHEMBL303902 101905 0 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 384 4 1 6 3.7 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4nsnc4c3)cccc12 10.1016/s0960-894x(97)10151-2
443289 702 40 None - 3 Pig 7.7 pIC50 = 7.7 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
997 702 40 None - 3 Pig 7.7 pIC50 = 7.7 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
CHEMBL314691 702 40 None - 3 Pig 7.7 pIC50 = 7.7 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
DB12054 702 40 None - 3 Pig 7.7 pIC50 = 7.7 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
10578601 128510 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 550 10 4 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)N(C)C(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL367033 128510 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 550 10 4 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)N(C)C(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
9917706 129204 0 None - 2 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL367444 129204 0 None - 2 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL336033 209818 1 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Inhibitory effect against porcine Endothelin A receptorInhibitory effect against porcine Endothelin A receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL336033 209818 1 None - 0 Pig 7.7 pIC50 = 7.7 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL170121 207088 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL None None None CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCC(=O)O 10.1016/0960-894X(95)00144-I
11070564 201700 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2 10.1021/jm010382z
CHEMBL65494 201700 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2 10.1021/jm010382z
122044 10063 47 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-ET1 from human smooth muscle ETA receptor expressed in fall armyworm sf9 cell membranesDisplacement of 125I-ET1 from human smooth muscle ETA receptor expressed in fall armyworm sf9 cell membranes
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1016/j.bmcl.2016.06.014
CHEMBL115951 10063 47 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-ET1 from human smooth muscle ETA receptor expressed in fall armyworm sf9 cell membranesDisplacement of 125I-ET1 from human smooth muscle ETA receptor expressed in fall armyworm sf9 cell membranes
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1016/j.bmcl.2016.06.014
10571812 128113 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 380 7 1 6 4.1 Cc1ccccc1C(Oc1cc(OCc2ccsn2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL366788 128113 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 380 7 1 6 4.1 Cc1ccccc1C(Oc1cc(OCc2ccsn2)ccc1C#N)C(=O)O 10.1021/jm990378b
2802888 60218 9 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cellsInhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cells
ChEMBL 414 9 4 5 2.5 CC(C)C(NC(=O)OCc1ccccc1)C(=O)NC(Cc1ccc(O)cc1)C(=O)O 10.1021/jm031041j
CHEMBL175916 60218 9 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cellsInhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cells
ChEMBL 414 9 4 5 2.5 CC(C)C(NC(=O)OCc1ccccc1)C(=O)NC(Cc1ccc(O)cc1)C(=O)O 10.1021/jm031041j
10789279 204829 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 441 10 1 6 4.1 CCCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8878 204829 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 441 10 1 6 4.1 CCCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10554384 168668 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 537 10 4 6 4.6 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL441112 168668 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 537 10 4 6 4.6 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
10554384 168668 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 537 10 4 6 4.6 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL441112 168668 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 537 10 4 6 4.6 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL2370254 208063 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10024044 7742 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 402 6 1 5 4.1 COc1ccc(CC2=C(c3ccccc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL10897 7742 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 402 6 1 5 4.1 COc1ccc(CC2=C(c3ccccc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
11732155 200970 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 402 4 1 5 4.4 COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL61460 200970 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 402 4 1 5 4.4 COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL2304014 207715 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(C#N)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
443289 702 40 None - 3 Pig 4.7 pIC50 = 4.7 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle
ChEMBL None None None None 10.1021/jm00087a001
997 702 40 None - 3 Pig 4.7 pIC50 = 4.7 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL314691 702 40 None - 3 Pig 4.7 pIC50 = 4.7 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle
ChEMBL None None None None 10.1021/jm00087a001
DB12054 702 40 None - 3 Pig 4.7 pIC50 = 4.7 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscleCompound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle
ChEMBL None None None None 10.1021/jm00087a001
10647488 176338 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 456 6 2 8 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(C)(O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL46195 176338 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 456 6 2 8 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(C)(O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
44320488 106489 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 438 5 1 5 5.7 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1C1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL315175 106489 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 438 5 1 5 5.7 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1C1CCCCC1 10.1016/s0960-894x(00)00513-8
10766198 162323 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 6 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NCc2ccccc2)c1Br 10.1021/jm9608366
CHEMBL417358 162323 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 6 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NCc2ccccc2)c1Br 10.1021/jm9608366
76324075 85399 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL 340 4 1 6 4.0 Cc1c(C(=O)O)oc2cccc(OCc3ccc4nsnc4c3)c12 10.1007/s00044-013-0542-3
CHEMBL2296899 85399 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL 340 4 1 6 4.0 Cc1c(C(=O)O)oc2cccc(OCc3ccc4nsnc4c3)c12 10.1007/s00044-013-0542-3
151174 201023 37 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 605 12 3 13 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO 10.1021/jm030528p
CHEMBL61780 201023 37 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
ChEMBL 605 12 3 13 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO 10.1021/jm030528p
10810505 59184 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 392 7 1 5 4.2 Cc1ccccc1C(Oc1cc(OCc2ccnc(F)c2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL171513 59184 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 392 7 1 5 4.2 Cc1ccccc1C(Oc1cc(OCc2ccnc(F)c2)ccc1C#N)C(=O)O 10.1021/jm990378b
10282163 60077 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 599 11 2 12 3.9 C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL175057 60077 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 599 11 2 12 3.9 C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10838921 204613 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 494 7 1 6 4.1 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)C2CCCCC2)cc1 10.1021/jm9505369
CHEMBL8736 204613 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 494 7 1 6 4.1 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)C2CCCCC2)cc1 10.1021/jm9505369
44279338 106199 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 487 11 6 4 2.3 CC(C)C[C@H](NC(=O)NC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31436 106199 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 487 11 6 4 2.3 CC(C)C[C@H](NC(=O)NC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL97431 214137 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
18617403 203552 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL79031 203552 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1Br 10.1016/0960-894X(96)00441-6
18617374 203795 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80808 203795 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
122044 10063 47 None - 0 Rat 6.6 pIC50 = 6.6 Binding
In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1021/jm0102304
CHEMBL115951 10063 47 None - 0 Rat 6.6 pIC50 = 6.6 Binding
In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1021/jm0102304
44327728 206149 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 505 5 1 8 2.1 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(Br)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL96662 206149 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 505 5 1 8 2.1 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(Br)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44327354 206306 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 427 5 1 8 1.4 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL97595 206306 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 427 5 1 8 1.4 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
10579210 168015 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 585 10 4 6 5.4 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL435901 168015 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 585 10 4 6 5.4 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL1791007 207160 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
21462925 119421 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 470 6 2 7 4.8 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N)ccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL349556 119421 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 470 6 2 7 4.8 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N)ccc23)cc1 10.1016/s0960-894x(99)00040-2
10766396 110077 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 460 8 1 4 4.6 CCCN(C)C(=O)CN1C[C@H](c2ccc3ccccc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL325418 110077 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 460 8 1 4 4.6 CCCN(C)C(=O)CN1C[C@H](c2ccc3ccccc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10837666 169310 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 460 8 1 4 4.6 CCCN(C)C(=O)CN1C[C@H](c2cccc3ccccc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL444061 169310 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 460 8 1 4 4.6 CCCN(C)C(=O)CN1C[C@H](c2cccc3ccccc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
44284290 12823 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL 589 13 4 5 3.9 CC(C)C[C@@H](NC(=O)C1CCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)O 10.1021/jm00087a001
CHEMBL1189291 12823 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL 589 13 4 5 3.9 CC(C)C[C@@H](NC(=O)C1CCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)O 10.1021/jm00087a001
CHEMBL538475 12823 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL 589 13 4 5 3.9 CC(C)C[C@@H](NC(=O)C1CCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)O 10.1021/jm00087a001
44320782 106576 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 482 7 1 6 5.8 COc1ccc(-c2nn(CC3CCCCC3)c(C(=O)O)c2Cc2cc3c(cc2Cl)OCO3)cc1 10.1016/s0960-894x(00)00513-8
CHEMBL315788 106576 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 482 7 1 6 5.8 COc1ccc(-c2nn(CC3CCCCC3)c(C(=O)O)c2Cc2cc3c(cc2Cl)OCO3)cc1 10.1016/s0960-894x(00)00513-8
44266629 4338 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 387 4 1 5 4.7 COc1ccc(-n2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1 10.1016/0960-894X(96)00170-9
CHEMBL10151 4338 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 387 4 1 5 4.7 COc1ccc(-n2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1 10.1016/0960-894X(96)00170-9
CHEMBL2304017 207718 0 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(C#N)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
44278270 161482 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor
ChEMBL 300 4 1 4 4.3 COc1cccc(Sc2c(C(=O)O)oc3ccccc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL416019 161482 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor
ChEMBL 300 4 1 4 4.3 COc1cccc(Sc2c(C(=O)O)oc3ccccc23)c1 10.1016/0960-894X(96)00232-6
23445430 60725 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 438 5 1 5 5.1 Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
CHEMBL176422 60725 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 438 5 1 5 5.1 Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
10530424 61746 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 536 9 4 5 4.3 Cc1c(C(=O)O)nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)n1C 10.1021/jm950592+
CHEMBL177502 61746 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 536 9 4 5 4.3 Cc1c(C(=O)O)nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)n1C 10.1021/jm950592+
23445438 61155 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 7 4.1 Cc1noc(NS(=O)(=O)c2sccc2CCc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL177070 61155 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 7 4.1 Cc1noc(NS(=O)(=O)c2sccc2CCc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
44384826 59646 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 561 10 1 9 5.8 C/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL173366 59646 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 561 10 1 9 5.8 C/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
9896251 98305 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Compound was evaluated for inhibitory activity against human Endothelin A receptor (ETA)Compound was evaluated for inhibitory activity against human Endothelin A receptor (ETA)
ChEMBL 682 12 1 9 7.1 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm020138n
CHEMBL278176 98305 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Compound was evaluated for inhibitory activity against human Endothelin A receptor (ETA)Compound was evaluated for inhibitory activity against human Endothelin A receptor (ETA)
ChEMBL 682 12 1 9 7.1 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm020138n
127034758 135834 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 681 12 1 8 7.7 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)cc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1039/C4MD00499J
CHEMBL3734968 135834 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 681 12 1 8 7.7 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)cc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1039/C4MD00499J
10576379 100788 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL296291 100788 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
10281192 60736 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 561 11 2 10 4.2 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176482 60736 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 561 11 2 10 4.2 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
9896251 98305 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 682 12 1 9 7.1 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL278176 98305 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 682 12 1 9 7.1 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
44404967 134882 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 680 12 1 8 7.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCC2 10.1021/jm058225d
CHEMBL372814 134882 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 680 12 1 8 7.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCC2 10.1021/jm058225d
CHEMBL343582 209944 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](c2ccccc2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
42630654 18205 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 545 10 2 8 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271531 18205 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 545 10 2 8 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
42630654 18205 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 545 10 2 8 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271531 18205 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 545 10 2 8 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
11763363 110005 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cnccn2)c1 10.1021/jm0102304
CHEMBL324943 110005 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cnccn2)c1 10.1021/jm0102304
443289 702 40 None 2 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL None None None None 10.1016/j.bmcl.2010.08.074
997 702 40 None 2 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL None None None None 10.1016/j.bmcl.2010.08.074
CHEMBL314691 702 40 None 2 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL None None None None 10.1016/j.bmcl.2010.08.074
DB12054 702 40 None 2 3 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL None None None None 10.1016/j.bmcl.2010.08.074
10915215 100323 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2 10.1021/jm031041j
CHEMBL293161 100323 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2 10.1021/jm031041j
18617389 162914 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 408 3 1 4 3.6 Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL420029 162914 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 408 3 1 4 3.6 Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
10646375 96597 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)ccc3OC)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL267096 96597 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)ccc3OC)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10915215 100323 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL293161 100323 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
44327727 167623 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 503 6 1 8 3.0 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL433373 167623 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 503 6 1 8 3.0 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44266640 97653 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 459 4 1 8 4.2 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3 10.1016/0960-894X(96)00170-9
CHEMBL273529 97653 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 459 4 1 8 4.2 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3 10.1016/0960-894X(96)00170-9
CHEMBL335780 209806 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL343768 209945 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10448516 98742 1 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3cc(N)ccc23)c1C 10.1021/jm00008a013
CHEMBL281511 98742 1 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3cc(N)ccc23)c1C 10.1021/jm00008a013
CHEMBL413880 211336 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor
ChEMBL None None None NC(=O)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00084-7
44314579 102431 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL 580 12 5 5 3.8 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL306123 102431 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL 580 12 5 5 3.8 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
10618166 59523 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 355 7 1 6 4.0 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccco1 10.1021/jm990378b
CHEMBL172880 59523 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 355 7 1 6 4.0 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccco1 10.1021/jm990378b
10151203 100320 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 429 5 1 6 4.2 COc1ccc(Cn2c(=O)c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1 10.1016/S0960-894X(97)00319-3
CHEMBL293151 100320 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 429 5 1 6 4.2 COc1ccc(Cn2c(=O)c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1 10.1016/S0960-894X(97)00319-3
10448516 98742 1 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3cc(N)ccc23)c1C 10.1021/jm00004a012
CHEMBL281511 98742 1 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3cc(N)ccc23)c1C 10.1021/jm00004a012
44266568 97633 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 493 7 1 6 6.3 COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OCc4ccccc4)cc23)cc1 10.1016/0960-894X(96)00170-9
CHEMBL273410 97633 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 493 7 1 6 6.3 COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OCc4ccccc4)cc23)cc1 10.1016/0960-894X(96)00170-9
10313743 95089 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3c(N)cccc3c2)c1C 10.1021/jm00008a013
CHEMBL25756 95089 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3c(N)cccc3c2)c1C 10.1021/jm00008a013
10314989 99386 1 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 336 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cccc3c(Cl)cccc23)c1C 10.1021/jm00008a013
CHEMBL285814 99386 1 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 336 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cccc3c(Cl)cccc23)c1C 10.1021/jm00008a013
127035379 135971 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 691 13 2 8 7.4 CCCc1nc2c(C)cc(C(=O)NCCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3736248 135971 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 691 13 2 8 7.4 CCCc1nc2c(C)cc(C(=O)NCCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
10507191 128257 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 565 10 4 5 5.6 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)s1 10.1021/jm950591h
CHEMBL366911 128257 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 565 10 4 5 5.6 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)s1 10.1021/jm950591h
CHEMBL2369710 207898 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
10313743 95089 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3c(N)cccc3c2)c1C 10.1021/jm00004a012
CHEMBL25756 95089 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3c(N)cccc3c2)c1C 10.1021/jm00004a012
10813822 96509 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 460 5 2 5 4.5 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)Nc2ccccc2)cc1 10.1021/jm9505369
CHEMBL266336 96509 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 460 5 2 5 4.5 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)Nc2ccccc2)cc1 10.1021/jm9505369
9915028 9306 12 None 28183 2 Human 4.6 pIC50 = 4.6 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL111612 9306 12 None 28183 2 Human 4.6 pIC50 = 4.6 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL4761843 9306 12 None 28183 2 Human 4.6 pIC50 = 4.6 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
10218058 81243 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 523 12 2 10 3.1 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL2163695 81243 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 523 12 2 10 3.1 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL97470 214138 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10600668 5074 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1cc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc(OC)c1OC 10.1021/jm9606507
CHEMBL10589 5074 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 476 7 1 8 3.8 COc1cc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc(OC)c1OC 10.1021/jm9606507
10625269 14306 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)cc2C)cc1 10.1021/jm990170q
CHEMBL120106 14306 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)cc2C)cc1 10.1021/jm990170q
10792783 60042 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 551 10 3 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL174699 60042 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 551 10 3 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
10218058 81243 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 523 12 2 10 3.1 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1021/jm3009103
CHEMBL2163695 81243 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 523 12 2 10 3.1 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1021/jm3009103
10951918 110371 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 567 11 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2SCCOc2ncccn2)c1 10.1021/jm0102304
CHEMBL326105 110371 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 567 11 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2SCCOc2ncccn2)c1 10.1021/jm0102304
44327656 141245 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 977 25 9 8 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL386181 141245 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 977 25 9 8 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10862228 201263 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 398 7 1 6 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC)cc21 10.1021/jm010382z
CHEMBL63000 201263 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 398 7 1 6 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC)cc21 10.1021/jm010382z
CHEMBL405677 210817 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor
ChEMBL None None None CC(=O)[C@@H](Cc1c[nH]c2ccccc12)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00084-7
44266552 4431 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/s0960-894x(97)10151-2
CHEMBL10218 4431 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/s0960-894x(97)10151-2
56671734 62984 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)NCC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC 10.1021/jm970161m
CHEMBL1793932 62984 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)NCC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC 10.1021/jm970161m
44266552 4431 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1021/jm0300429
CHEMBL10218 4431 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1021/jm0300429
CHEMBL341443 209884 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](CCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44368824 96366 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL 1595 31 19 20 0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
77282142 96366 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL 1595 31 19 20 0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL265164 96366 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL 1595 31 19 20 0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL412460 211234 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
18617363 163997 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL421523 163997 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL37860 210505 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccn1)C(=O)O 10.1021/jm00087a001
44368905 161261 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL 1623 31 19 20 1.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
77282145 161261 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL 1623 31 19 20 1.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL414448 161261 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL 1623 31 19 20 1.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
10792784 59268 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 551 10 4 5 5.4 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)o1 10.1021/jm950591h
CHEMBL171910 59268 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 551 10 4 5 5.4 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)o1 10.1021/jm950591h
44309488 202302 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 471 7 1 8 5.1 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1 10.1016/s0960-894x(97)10151-2
CHEMBL69664 202302 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 471 7 1 8 5.1 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1 10.1016/s0960-894x(97)10151-2
44327726 206146 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 495 6 1 8 2.7 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc3c(cc2=O)CCC3)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL96644 206146 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 495 6 1 8 2.7 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc3c(cc2=O)CCC3)cc1 10.1016/S0960-894X(96)00617-8
44309488 202302 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 471 7 1 8 5.1 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1 10.1021/jm0300429
CHEMBL69664 202302 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 471 7 1 8 5.1 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1 10.1021/jm0300429
10038537 59643 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor
ChEMBL 266 3 2 5 0.8 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)CC1 10.1016/s0960-894x(00)00136-0
CHEMBL173336 59643 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor
ChEMBL 266 3 2 5 0.8 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)CC1 10.1016/s0960-894x(00)00136-0
44279479 98817 1 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined
ChEMBL 516 14 6 5 1.8 CC(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL281963 98817 1 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined
ChEMBL 516 14 6 5 1.8 CC(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)O 10.1016/0960-894X(95)00221-E
44279439 106881 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 534 3 2 3 6.2 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(C(F)(F)F)cc3C(F)(F)F)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL31781 106881 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 534 3 2 3 6.2 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(C(F)(F)F)cc3C(F)(F)F)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL137569 206993 0 None - 0 Pig 4.6 pIC50 = 4.6 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10787482 96500 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 405 4 1 4 3.9 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)nc3)cccc12 10.1021/jm9604585
CHEMBL266277 96500 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 405 4 1 4 3.9 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)nc3)cccc12 10.1021/jm9604585
10740139 201257 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 406 4 1 5 3.3 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)nn3)cccc12 10.1021/jm9604585
CHEMBL6297 201257 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 406 4 1 5 3.3 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)nn3)cccc12 10.1021/jm9604585
18617288 203426 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 316 3 1 4 2.5 Cc1noc(NS(=O)(=O)c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL78080 203426 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 316 3 1 4 2.5 Cc1noc(NS(=O)(=O)c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
10646522 201692 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 434 5 1 5 3.8 CCc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
CHEMBL6543 201692 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 434 5 1 5 3.8 CCc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
22998439 201398 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 392 5 1 7 3.7 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/S0960-894X(97)00367-3
CHEMBL63938 201398 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 392 5 1 7 3.7 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/S0960-894X(97)00367-3
10650368 60033 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 553 10 5 7 3.6 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(O)CC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL174635 60033 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 553 10 5 7 3.6 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(O)CC2)nc1C(=O)O 10.1021/jm950592+
10789715 112586 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 450 8 1 5 4.2 CCCN(C)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL331375 112586 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 450 8 1 5 4.2 CCCN(C)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10575552 110808 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 450 8 1 5 4.2 CCCN(C)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL326690 110808 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 450 8 1 5 4.2 CCCN(C)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
9871561 174218 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 527 10 2 8 4.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4562189 174218 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 527 10 2 8 4.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO 10.1016/j.bmcl.2016.06.014
44314657 102715 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 619 13 5 4 4.3 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1)C(=O)O 10.1021/jm9600914
CHEMBL308383 102715 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 619 13 5 4 4.3 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1)C(=O)O 10.1021/jm9600914
10288020 14445 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 430 7 1 6 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205067 14445 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 430 7 1 6 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL48881 14445 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 430 7 1 6 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
11796594 205636 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 424 10 1 5 5.8 CC(=O)c1ccc(OCc2ccsc2)cc1OC(CCC(=O)O)c1ccccc1C 10.1021/jm9707131
CHEMBL93776 205636 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 424 10 1 5 5.8 CC(=O)c1ccc(OCc2ccsc2)cc1OC(CCC(=O)O)c1ccccc1C 10.1021/jm9707131
10144334 130129 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 561 10 2 10 4.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL368211 130129 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 561 10 2 10 4.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
44385941 130141 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368286 130141 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O 10.1021/jm950592+
31771 96505 33 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 267 3 2 5 1.7 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00008a013
CHEMBL26630 96505 33 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 267 3 2 5 1.7 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00008a013
11755275 198316 0 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 489 9 1 7 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1cc(OC)ccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL59537 198316 0 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 489 9 1 7 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1cc(OC)ccc1OC 10.1016/S0960-894X(97)00319-3
31771 96505 33 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 267 3 2 5 1.7 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00004a012
CHEMBL26630 96505 33 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 267 3 2 5 1.7 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00004a012
56657875 62980 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC 10.1021/jm970161m
CHEMBL1793925 62980 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC 10.1021/jm970161m
56681798 62983 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@@H](C)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)CNC(=O)[C@H](NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)[C@H](C)CC 10.1021/jm970161m
CHEMBL1793929 62983 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@@H](C)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)CNC(=O)[C@H](NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)[C@H](C)CC 10.1021/jm970161m
44327252 205790 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 495 7 1 8 3.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C3CC3)ccc2=O)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL94654 205790 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 495 7 1 8 3.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C3CC3)ccc2=O)cc1 10.1016/S0960-894X(96)00617-8
44266592 5288 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 431 4 1 7 4.5 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10699 5288 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 431 4 1 7 4.5 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL137754 206997 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
CHEMBL436884 211932 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
44328019 155151 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 1000 26 9 8 5.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL405178 155151 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 1000 26 9 8 5.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44327348 161346 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 1076 28 9 8 7.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL415238 161346 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 1076 28 9 8 7.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10216862 194728 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 443 4 1 7 3.9 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n(Cc2ccc3c(c2)OCO3)c1=O 10.1016/S0960-894X(97)00319-3
CHEMBL56286 194728 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 443 4 1 7 3.9 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n(Cc2ccc3c(c2)OCO3)c1=O 10.1016/S0960-894X(97)00319-3
44327412 205837 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL94929 205837 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44327114 206063 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 533 7 1 7 4.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccccc3)CCC2=O)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL96234 206063 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 533 7 1 7 4.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccccc3)CCC2=O)cc1 10.1016/S0960-894X(96)00617-8
10244529 58955 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor
ChEMBL 264 3 1 5 1.0 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(=O)[C@]2(O)CC1 10.1016/s0960-894x(00)00136-0
CHEMBL170450 58955 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor
ChEMBL 264 3 1 5 1.0 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(=O)[C@]2(O)CC1 10.1016/s0960-894x(00)00136-0
44279371 99449 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 466 3 2 3 5.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cc(Cl)cc(Cl)c3)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL286214 99449 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 466 3 2 3 5.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cc(Cl)cc(Cl)c3)cc21 10.1016/0960-894X(95)00230-Q
6426756 150164 33 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 537 9 3 10 3.9 CC(C)(C)c1ccc(S(=O)(=O)Nc2nc(-c3ncccn3)nc(OCCO)c2Oc2ccccc2O)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL3956076 150164 33 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 537 9 3 10 3.9 CC(C)(C)c1ccc(S(=O)(=O)Nc2nc(-c3ncccn3)nc(OCCO)c2Oc2ccccc2O)cc1 10.1016/j.bmcl.2016.06.014
23445254 205416 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 412 5 1 5 4.2 Cc1noc(NS(=O)(=O)c2sccc2Cc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL92318 205416 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 412 5 1 5 4.2 Cc1noc(NS(=O)(=O)c2sccc2Cc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
9810571 61042 0 None - 2 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 731 18 2 13 5.0 CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL176997 61042 0 None - 2 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 731 18 2 13 5.0 CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
127034756 135817 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 679 12 2 7 7.5 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3734829 135817 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 679 12 2 7 7.5 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
176 394 63 None -7 31 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -7 31 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -7 31 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -7 31 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -7 31 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
18617393 203556 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 308 5 1 4 3.2 CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
CHEMBL79066 203556 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 308 5 1 4 3.2 CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
44314647 203366 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 647 13 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCCC1)C(=O)O 10.1021/jm9600914
CHEMBL77468 203366 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 647 13 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCCC1)C(=O)O 10.1021/jm9600914
CHEMBL2304016 207717 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](C(C)(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC1=O 10.1021/jm9600914
10502226 101045 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 420 6 1 8 3.3 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1C 10.1021/jm9700068
CHEMBL298203 101045 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 420 6 1 8 3.3 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1C 10.1021/jm9700068
10715441 175343 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 390 6 1 6 3.9 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm9700068
CHEMBL45875 175343 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 390 6 1 6 3.9 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm9700068
10575755 179227 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1021/jm9608366
CHEMBL47450 179227 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1021/jm9608366
10168195 61043 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 631 11 2 13 5.0 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176999 61043 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 631 11 2 13 5.0 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10744085 102384 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 503 9 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN(C)C)c2)cc1 10.1021/jm980504w
CHEMBL305777 102384 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 503 9 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN(C)C)c2)cc1 10.1021/jm980504w
10318748 99157 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 399 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCCC4=O)cccc23)c1C 10.1021/jm00008a013
CHEMBL284177 99157 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 399 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCCC4=O)cccc23)c1C 10.1021/jm00008a013
44316527 203759 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 280 3 1 4 2.7 Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
CHEMBL80532 203759 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 280 3 1 4 2.7 Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
44316831 203794 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 358 4 1 4 3.4 CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
CHEMBL80807 203794 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 358 4 1 4 3.4 CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
15296635 99081 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 488 11 5 5 2.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL283591 99081 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 488 11 5 5 2.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
23445224 201698 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 406 5 1 7 4.0 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1016/S0960-894X(97)00367-3
CHEMBL65488 201698 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 406 5 1 7 4.0 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1016/S0960-894X(97)00367-3
CHEMBL1791006 207159 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44371396 49238 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 471 6 1 6 5.9 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3SC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL156532 49238 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 471 6 1 6 5.9 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3SC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
44371532 51185 1 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 455 6 1 6 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL158239 51185 1 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 455 6 1 6 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
44371571 118971 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 425 5 1 5 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL345380 118971 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 425 5 1 5 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
10473627 101406 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc12 10.1021/jm00008a013
CHEMBL30077 101406 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc12 10.1021/jm00008a013
18617395 203551 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 361 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL79030 203551 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 361 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1Br 10.1016/0960-894X(96)00441-6
10473627 101406 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc12 10.1021/jm00004a012
CHEMBL30077 101406 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc12 10.1021/jm00004a012
56681797 62979 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC 10.1021/jm970161m
CHEMBL1793924 62979 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC 10.1021/jm970161m
44213924 205753 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 567 7 1 7 4.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccc(Cl)cc3)CCC2=O)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL94426 205753 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 567 7 1 7 4.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccc(Cl)cc3)CCC2=O)cc1 10.1016/S0960-894X(96)00617-8
44266537 4247 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 507 8 1 6 6.4 COc1ccc(Cn2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)ccc32)cc1 10.1016/0960-894X(96)00170-9
CHEMBL10092 4247 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 507 8 1 6 6.4 COc1ccc(Cn2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)ccc32)cc1 10.1016/0960-894X(96)00170-9
44368414 120761 0 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 459 9 1 5 4.2 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccccc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL357978 120761 0 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 459 9 1 5 4.2 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccccc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
10470588 99517 2 None - 0 Human 4.6 pIC50 = 4.6 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 309 6 2 5 2.9 CCCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00029a001
CHEMBL286682 99517 2 None - 0 Human 4.6 pIC50 = 4.6 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 309 6 2 5 2.9 CCCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00029a001
10470588 99517 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 309 6 2 5 2.9 CCCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00008a013
CHEMBL286682 99517 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 309 6 2 5 2.9 CCCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00008a013
127035068 135837 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 633 10 2 7 7.7 CCCc1nc2c(C)cc(C(=O)Nc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3735036 135837 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 633 10 2 7 7.7 CCCc1nc2c(C)cc(C(=O)Nc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
10604119 11337 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 636 12 2 7 5.8 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL1180361 11337 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 636 12 2 7 5.8 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL123654 11337 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 636 12 2 7 5.8 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
23445241 102162 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 442 5 1 7 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1Br 10.1016/S0960-894X(97)00367-3
CHEMBL304406 102162 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 442 5 1 7 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1Br 10.1016/S0960-894X(97)00367-3
10554724 61421 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL177195 61421 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O 10.1021/jm950592+
12146375 96388 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 322 3 1 5 2.6 Cc1noc(NS(=O)(=O)c2ccsc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL265290 96388 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 322 3 1 5 2.6 Cc1noc(NS(=O)(=O)c2ccsc2)c1Br 10.1016/S0960-894X(96)00496-9
9975719 95566 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc12 10.1021/jm00008a013
CHEMBL25977 95566 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc12 10.1021/jm00008a013
9975719 95566 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc12 10.1021/jm00004a012
CHEMBL25977 95566 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc12 10.1021/jm00004a012
127034919 135979 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 599 10 2 7 6.6 CCCc1nc2c(C)cc(C(=O)NC(C)C)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3736310 135979 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 599 10 2 7 6.6 CCCc1nc2c(C)cc(C(=O)NC(C)C)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
44384610 127936 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 743 16 2 14 4.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL366627 127936 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 743 16 2 14 4.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
137633653 156044 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 593 10 2 9 5.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4068786 156044 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 593 10 2 9 5.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
9868822 8490 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 459 6 1 7 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(N(C)C)cc2)cc1 10.1021/jm9606507
CHEMBL10948 8490 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 459 6 1 7 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(N(C)C)cc2)cc1 10.1021/jm9606507
CHEMBL2304013 207714 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](C(C)(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC1=O 10.1021/jm9600914
443289 702 40 None -2 3 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL None None None None 10.1007/s00044-013-0542-3
997 702 40 None -2 3 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL None None None None 10.1007/s00044-013-0542-3
CHEMBL314691 702 40 None -2 3 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL None None None None 10.1007/s00044-013-0542-3
DB12054 702 40 None -2 3 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL None None None None 10.1007/s00044-013-0542-3
CHEMBL336033 209818 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2015.01.003
44295224 14447 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 532 9 1 9 4.6 COc1cc(C/C(C(=O)c2ccc3c(c2)CCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1205077 14447 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 532 9 1 9 4.6 COc1cc(C/C(C(=O)c2ccc3c(c2)CCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL49675 14447 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 532 9 1 9 4.6 COc1cc(C/C(C(=O)c2ccc3c(c2)CCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
44294929 14610 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1206731 14610 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL301971 14610 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44320375 106648 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 506 8 1 7 5.3 COc1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc(OC)c1 10.1016/s0960-894x(00)00513-8
CHEMBL316187 106648 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 506 8 1 7 5.3 COc1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc(OC)c1 10.1016/s0960-894x(00)00513-8
10252787 98796 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 442 7 1 6 4.6 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL281865 98796 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 442 7 1 6 4.6 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00232-8
10839618 201871 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 517 10 1 8 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN(C)C)c2)cc1 10.1021/jm980504w
CHEMBL66762 201871 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 517 10 1 8 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN(C)C)c2)cc1 10.1021/jm980504w
17885919 204674 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 526 9 2 8 4.8 O=C(O)COc1ccccc1Cn1nc(-c2cccs2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
CHEMBL87801 204674 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 526 9 2 8 4.8 O=C(O)COc1ccccc1Cn1nc(-c2cccs2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
3795752 104710 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1C 10.1016/0960-894X(96)00441-6
CHEMBL311455 104710 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1C 10.1016/0960-894X(96)00441-6
44283453 138235 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)C(CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL37807 138235 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)C(CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
10721106 61062 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 536 9 4 5 4.3 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL177023 61062 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 536 9 4 5 4.3 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
10247887 97898 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 359 5 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(CN(C)C)cccc23)c1C 10.1021/jm00029a001
CHEMBL27525 97898 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 359 5 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(CN(C)C)cccc23)c1C 10.1021/jm00029a001
10247887 97898 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 5 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(CN(C)C)cccc23)c1C 10.1021/jm00008a013
CHEMBL27525 97898 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 5 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(CN(C)C)cccc23)c1C 10.1021/jm00008a013
CHEMBL86814 214105 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
CHEMBL408141 210946 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL86814 214105 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
CHEMBL344473 209949 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](C)NC1=O 10.1021/jm00021a021
10444974 99125 17 None - 0 Human 4.6 pIC50 = 4.6 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)on1 10.1021/jm00029a001
CHEMBL283941 99125 17 None - 0 Human 4.6 pIC50 = 4.6 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)on1 10.1021/jm00029a001
10444974 99125 17 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)on1 10.1021/jm00008a013
CHEMBL283941 99125 17 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)on1 10.1021/jm00008a013
127035084 135847 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 707 13 2 9 7.4 CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3735151 135847 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 707 13 2 9 7.4 CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
44298395 100206 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 308 3 1 4 3.4 Cc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1C 10.1016/s0960-894x(00)00366-8
CHEMBL292355 100206 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 308 3 1 4 3.4 Cc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1C 10.1016/s0960-894x(00)00366-8
44298342 101274 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 283 3 2 5 2.1 Cc1snc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/s0960-894x(00)00366-8
CHEMBL299831 101274 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 283 3 2 5 2.1 Cc1snc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/s0960-894x(00)00366-8
18184179 128487 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 654 13 2 12 4.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL367017 128487 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 654 13 2 12 4.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
52950137 18235 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 559 10 3 8 3.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(=O)O)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271863 18235 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 559 10 3 8 3.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(=O)O)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
10760657 59693 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 355 7 1 6 4.0 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccoc1 10.1021/jm990378b
CHEMBL173565 59693 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 355 7 1 6 4.0 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccoc1 10.1021/jm990378b
10717279 96587 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 425 9 1 5 4.8 CCCCCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL266996 96587 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 425 9 1 5 4.8 CCCCCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
18948954 167332 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 360 4 2 5 3.5 Cc1noc(NS(=O)(=O)c2cccc3c(C(C)(C)O)cccc23)c1C 10.1021/jm00008a013
CHEMBL431300 167332 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 360 4 2 5 3.5 Cc1noc(NS(=O)(=O)c2cccc3c(C(C)(C)O)cccc23)c1C 10.1021/jm00008a013
11783885 100407 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 382 7 1 5 4.6 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm031041j
CHEMBL293702 100407 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 382 7 1 5 4.6 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm031041j
18617340 104911 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 422 4 1 4 3.9 CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
CHEMBL311742 104911 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 422 4 1 4 3.9 CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
11783885 100407 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 382 7 1 5 4.6 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL293702 100407 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 382 7 1 5 4.6 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
155511294 168991 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 469 6 1 8 2.5 Cc1ccc(=O)n([C@@H](C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/j.bmcl.2016.06.014
CHEMBL4435789 168991 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 469 6 1 8 2.5 Cc1ccc(=O)n([C@@H](C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/j.bmcl.2016.06.014
44293805 100632 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 545 10 2 10 3.5 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCc1nn[nH]n1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL295140 100632 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 545 10 2 10 3.5 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCc1nn[nH]n1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10693679 205631 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 425 10 2 5 4.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(N)=O 10.1021/jm9707131
CHEMBL93749 205631 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 425 10 2 5 4.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(N)=O 10.1021/jm9707131
9848132 205833 0 None 1 2 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 483 6 1 8 2.8 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL94918 205833 0 None 1 2 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 483 6 1 8 2.8 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44387111 165618 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 548 10 5 5 4.2 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL426413 165618 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 548 10 5 5 4.2 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
10506505 128134 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 535 11 4 5 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H](CC(=O)NC2CCCCC2)CC(C)C)nc1C(=O)O 10.1021/jm9505932
CHEMBL366805 128134 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 535 11 4 5 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H](CC(=O)NC2CCCCC2)CC(C)C)nc1C(=O)O 10.1021/jm9505932
CHEMBL137716 206996 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None COC(=O)n1cc(C[C@@H]2NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@H]3CCCN3C(=O)[C@H](CC(=O)O)NC2=O)c2ccccc21 10.1021/jm00021a021
137655525 158433 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 525 7 3 9 3.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4096346 158433 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 525 7 3 9 3.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10383850 99295 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 5 1 5 3.6 CCc1c(C)noc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm00008a013
CHEMBL285122 99295 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 5 1 5 3.6 CCc1c(C)noc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm00008a013
10882352 201285 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 340 4 1 5 3.4 CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL63099 201285 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 340 4 1 5 3.4 CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
44279383 99519 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 398 3 2 3 4.2 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccccc3)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL286687 99519 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 398 3 2 3 4.2 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccccc3)cc21 10.1016/0960-894X(95)00230-Q
23445221 201397 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 470 5 1 7 4.4 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00367-3
CHEMBL63937 201397 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 470 5 1 7 4.4 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00367-3
44327237 206181 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 511 8 1 8 3.5 CCCc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL96847 206181 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 511 8 1 8 3.5 CCCc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
15453172 203267 4 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL76623 203267 4 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1Br 10.1016/0960-894X(96)00441-6
44213923 107782 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 563 8 1 8 4.1 COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL319743 107782 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 563 8 1 8 4.1 COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1 10.1016/S0960-894X(96)00617-8
10530457 61768 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 538 9 5 6 4.0 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)NO 10.1021/jm950592+
CHEMBL177602 61768 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 538 9 5 6 4.0 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)NO 10.1021/jm950592+
10168939 130833 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 695 11 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
CHEMBL368860 130833 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 695 11 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
CHEMBL170600 207092 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL None None None CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)O 10.1016/0960-894X(95)00144-I
CHEMBL1201469 14326 0 None -1 4 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL None None None None nan
23445227 120299 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2ccsc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
CHEMBL355800 120299 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2ccsc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
10789525 61426 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL177221 61426 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
10789524 5106 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2)cc1 10.1021/jm9606507
CHEMBL10607 5106 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2)cc1 10.1021/jm9606507
10896413 100128 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 504 9 1 7 5.4 COc1ccc(CCOC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL291841 100128 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 504 9 1 7 5.4 COc1ccc(CCOC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
11762291 100156 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL292041 100156 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 6 1 6 5.2 COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
11059249 102132 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 440 10 1 6 5.3 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCCC)cc21 10.1021/jm010382z
CHEMBL304202 102132 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 440 10 1 6 5.3 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCCC)cc21 10.1021/jm010382z
11144468 201759 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 430 5 1 5 5.2 CC(C)Oc1ccc2c(c1)C(c1ccccc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL65925 201759 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 430 5 1 5 5.2 CC(C)Oc1ccc2c(c1)C(c1ccccc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10184817 9468 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)CCC 10.1021/jm980217s
CHEMBL112417 9468 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)CCC 10.1021/jm980217s
44314904 102659 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL 585 12 5 5 3.6 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL307936 102659 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL 585 12 5 5 3.6 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
155564169 174751 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 545 11 1 12 2.0 COc1ccc(Cl)c(Oc2c(NS(C)(=O)=O)ncnc2OCCOc2ncc(S(C)(=O)=O)cn2)c1 10.1016/j.bmcl.2016.06.014
CHEMBL4574034 174751 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 545 11 1 12 2.0 COc1ccc(Cl)c(Oc2c(NS(C)(=O)=O)ncnc2OCCOc2ncc(S(C)(=O)=O)cn2)c1 10.1016/j.bmcl.2016.06.014
71455062 81253 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 669 14 1 12 5.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C(F)(F)F)cn1 10.1021/jm3009103
CHEMBL2163705 81253 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 669 14 1 12 5.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C(F)(F)F)cn1 10.1021/jm3009103
44295005 10109 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c(F)c1 10.1016/s0960-894x(98)00301-1
CHEMBL1160205 10109 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c(F)c1 10.1016/s0960-894x(98)00301-1
10226215 100949 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 8 3.8 Cc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
CHEMBL297473 100949 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 8 3.8 Cc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
44291255 172877 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 8 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C)OCO3)c1Cl 10.1021/jm9700068
CHEMBL45296 172877 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 8 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C)OCO3)c1Cl 10.1021/jm9700068
CHEMBL414165 211357 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
Inhibitory effect against porcine ET-A receptorInhibitory effect against porcine ET-A receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](c2cccs2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44311345 202507 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 663 13 3 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CCNCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70895 202507 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 663 13 3 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CCNCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL414165 211357 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](c2cccs2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
8260 527 46 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at ETA receptor (unknown origin) in presence of ET1Antagonist activity at ETA receptor (unknown origin) in presence of ET1
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
9912992 527 46 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at ETA receptor (unknown origin) in presence of ET1Antagonist activity at ETA receptor (unknown origin) in presence of ET1
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
CHEMBL3989834 527 46 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at ETA receptor (unknown origin) in presence of ET1Antagonist activity at ETA receptor (unknown origin) in presence of ET1
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
44458597 98322 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 535 7 3 8 2.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2C(=O)O)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL278349 98322 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 535 7 3 8 2.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2C(=O)O)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
11017071 9846 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 547 9 1 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3cccs3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL114683 9846 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 547 9 1 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3cccs3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
10994373 161892 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 5 1 7 5.0 CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL416675 161892 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 5 1 7 5.0 CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10122033 81251 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 631 15 1 13 4.0 COc1cnc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)nc1 10.1021/jm3009103
CHEMBL2163703 81251 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 631 15 1 13 4.0 COc1cnc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)nc1 10.1021/jm3009103
44334145 4569 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 460 6 1 6 4.6 COc1ccc([C@@H]2c3nc(N(C)C(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL103090 4569 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 460 6 1 6 4.6 COc1ccc([C@@H]2c3nc(N(C)C(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
44352026 116969 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 548 11 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C(F)(F)F)cc1 10.1021/jm010237l
CHEMBL339969 116969 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 548 11 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C(F)(F)F)cc1 10.1021/jm010237l
44339840 9183 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 486 13 1 5 5.1 C/C=C(\C)CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL110904 9183 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 486 13 1 5 5.1 C/C=C(\C)CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
10577829 9561 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 518 13 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCCO1 10.1021/jm980217s
CHEMBL112877 9561 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 518 13 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCCO1 10.1021/jm980217s
73669821 117111 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of PD156707 from rat ETA receptor after 1 hr by Lowry methodDisplacement of PD156707 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 448 10 1 6 5.2 CC(=O)c1ccc(OCc2ccc3c(c2)OCO3)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400988 117111 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of PD156707 from rat ETA receptor after 1 hr by Lowry methodDisplacement of PD156707 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 448 10 1 6 5.2 CC(=O)c1ccc(OCc2ccc3c(c2)OCO3)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
21041307 174387 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 482 10 2 9 2.6 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4566095 174387 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 482 10 2 9 2.6 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
10274552 73151 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 434 6 1 8 3.6 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2 10.1021/jm9700068
CHEMBL20168 73151 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 434 6 1 8 3.6 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2 10.1021/jm9700068
10274552 73151 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 434 6 1 8 3.6 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2 10.1021/jm000349x
CHEMBL20168 73151 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 434 6 1 8 3.6 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2 10.1021/jm000349x
16004692 2411 85 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
4809 2411 85 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
7352 2411 85 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
CHEMBL2103873 2411 85 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
DB08932 2411 85 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
10070 445 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1016/j.bmcl.2016.06.014
25099191 445 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1016/j.bmcl.2016.06.014
CHEMBL2165326 445 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1016/j.bmcl.2016.06.014
DB15059 445 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1016/j.bmcl.2016.06.014
10070 445 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1021/jm3009103
25099191 445 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1021/jm3009103
CHEMBL2165326 445 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1021/jm3009103
DB15059 445 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1021/jm3009103
71455065 81273 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 679 14 2 11 4.8 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ccncc2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163724 81273 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 679 14 2 11 4.8 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ccncc2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
17869373 14450 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205094 14450 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL51890 14450 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44295106 14558 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 472 7 1 7 4.6 COc1ccc(C(=O)/C(Cc2ccc3c(c2)CCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1206319 14558 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 472 7 1 7 4.6 COc1ccc(C(=O)/C(Cc2ccc3c(c2)CCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL262000 14558 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 472 7 1 7 4.6 COc1ccc(C(=O)/C(Cc2ccc3c(c2)CCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
17869279 14695 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2ccccc2OC)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1207701 14695 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2ccccc2OC)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL431160 14695 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2ccccc2OC)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44320171 106461 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 504 6 1 5 6.4 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC12CC3CC(CC(C3)C1)C2 10.1016/s0960-894x(00)00513-8
CHEMBL314974 106461 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 504 6 1 5 6.4 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC12CC3CC(CC(C3)C1)C2 10.1016/s0960-894x(00)00513-8
11135910 10100 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 624 10 1 10 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL116002 10100 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 624 10 1 10 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
10205245 71850 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm9608366
CHEMBL19808 71850 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm9608366
44291575 178845 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C#N)OCO3)c1Cl 10.1021/jm9700068
CHEMBL47404 178845 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C#N)OCO3)c1Cl 10.1021/jm9700068
10205245 71850 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm000349x
CHEMBL19808 71850 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm000349x
CHEMBL133257 206963 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory effect against Human ET-A receptorInhibitory effect against Human ET-A receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
11634755 61963 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 480 7 1 7 4.9 COc1cc(/C(C(=O)O)=C(\CC2CCCCC2)C(=O)c2ccc3c(c2)OCCO3)cc2c1OCO2 10.1021/jm031041j
CHEMBL177886 61963 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 480 7 1 7 4.9 COc1cc(/C(C(=O)O)=C(\CC2CCCCC2)C(=O)c2ccc3c(c2)OCCO3)cc2c1OCO2 10.1021/jm031041j
44304492 96099 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL262993 96099 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
18738878 193154 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 547 8 2 7 4.2 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL539420 193154 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 547 8 2 7 4.2 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
9958846 169599 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 537 13 1 10 3.7 COCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)CCc2ccccc2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL4444693 169599 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 537 13 1 10 3.7 COCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)CCc2ccccc2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
71455140 81582 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 598 12 2 8 4.7 CC(C)c1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL2165336 81582 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 598 12 2 8 4.7 CC(C)c1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
11123269 204567 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 452 6 1 5 5.8 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL87070 204567 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 452 6 1 5 5.8 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
10697520 11996 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 530 10 2 6 4.9 CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL1184086 11996 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 530 10 2 6 4.9 CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL331936 11996 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 530 10 2 6 4.9 CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
10530156 9451 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 526 14 1 6 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL112347 9451 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 526 14 1 6 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
44295206 14609 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 580 12 1 11 4.7 COc1cc(C/C(C(=O)c2cc(OC)c(OC)c(OC)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1206728 14609 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 580 12 1 11 4.7 COc1cc(C/C(C(=O)c2cc(OC)c(OC)c(OC)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL301577 14609 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 580 12 1 11 4.7 COc1cc(C/C(C(=O)c2cc(OC)c(OC)c(OC)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
11059349 201806 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 6 1 6 4.8 CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm031041j
CHEMBL66264 201806 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 6 1 6 4.8 CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm031041j
15453178 104261 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 348 4 1 4 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
CHEMBL310739 104261 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 348 4 1 4 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
11059349 201806 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 446 6 1 6 4.8 CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL66264 201806 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 446 6 1 6 4.8 CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
44314610 102370 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 671 12 6 5 3.9 CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
CHEMBL305650 102370 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 671 12 6 5 3.9 CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
44314619 202970 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 631 12 5 4 4.5 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL73925 202970 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 631 12 5 4 4.5 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
71451529 81267 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 632 14 2 12 3.4 CCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163719 81267 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 632 14 2 12 3.4 CCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
10504920 162548 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 480 6 2 9 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC#N)OCO3)c1Cl 10.1021/jm9608366
CHEMBL417719 162548 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 480 6 2 9 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC#N)OCO3)c1Cl 10.1021/jm9608366
CHEMBL284250 209105 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1016/0960-894X(95)00237-N
10579100 165777 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 578 10 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1 10.1021/jm031041j
CHEMBL122614 165777 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 578 10 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1 10.1021/jm031041j
CHEMBL427303 165777 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 578 10 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1 10.1021/jm031041j
10579100 165777 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 578 10 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL122614 165777 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 578 10 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL427303 165777 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 578 10 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
10695363 5168 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 462 6 1 7 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(SC)cc2)cc1 10.1021/jm9606507
CHEMBL10636 5168 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 462 6 1 7 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(SC)cc2)cc1 10.1021/jm9606507
73669820 117112 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 462 10 1 7 5.5 CC(=O)c1ccc(OCc2ccc3nsnc3c2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400989 117112 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 462 10 1 7 5.5 CC(=O)c1ccc(OCc2ccc3nsnc3c2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
44380952 27266 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 679 10 1 9 7.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(-c3cccs3)nc2OCCOc2ncc(Br)cn2)cc1 10.1016/s0960-894x(01)00682-5
CHEMBL136871 27266 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 679 10 1 9 7.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(-c3cccs3)nc2OCCOc2ncc(Br)cn2)cc1 10.1016/s0960-894x(01)00682-5
44291897 100810 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 482 7 2 9 3.6 COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
CHEMBL296456 100810 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 482 7 2 9 3.6 COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
9956918 170306 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 482 7 2 9 3.6 COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1OC 10.1021/jm9700068
CHEMBL44544 170306 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 482 7 2 9 3.6 COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1OC 10.1021/jm9700068
44279172 108152 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 532 10 2 6 4.6 CCCCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccccc1 10.1016/S0960-894X(97)00228-X
CHEMBL32075 108152 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 532 10 2 6 4.6 CCCCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccccc1 10.1016/S0960-894X(97)00228-X
10022121 101346 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 371 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCC4)cccc23)c1C 10.1021/jm00008a013
CHEMBL30032 101346 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 371 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCC4)cccc23)c1C 10.1021/jm00008a013
9957225 5178 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 490 8 0 8 4.7 COc1ccc(C2OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL10644 5178 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 490 8 0 8 4.7 COc1ccc(C2OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
18738880 167600 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 561 8 2 7 4.5 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)NC)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL433221 167600 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 561 8 2 7 4.5 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)NC)cc21 10.1016/s0960-894x(01)00660-6
10738157 58925 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1C(Oc1cc(OCc2cccnc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL170348 58925 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1C(Oc1cc(OCc2cccnc2)ccc1C#N)C(=O)O 10.1021/jm990378b
10714797 120192 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 380 7 1 6 4.1 Cc1ccccc1C(Oc1cc(OCc2cncs2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL354740 120192 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 380 7 1 6 4.1 Cc1ccccc1C(Oc1cc(OCc2cncs2)ccc1C#N)C(=O)O 10.1021/jm990378b
10622380 100972 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1cccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
CHEMBL297679 100972 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1cccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
CHEMBL2369736 207909 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N(C)[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
CHEMBL65559 214074 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00349-X
9850566 4115 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 551 8 1 8 6.1 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00170-9
CHEMBL10016 4115 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 551 8 1 8 6.1 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00170-9
CHEMBL342615 209919 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory effect against Human Endothelin A receptorInhibitory effect against Human Endothelin A receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CS(=O)(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44311527 202414 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 675 12 2 11 7.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2cccs2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70365 202414 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 675 12 2 11 7.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2cccs2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL148751 207032 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
The inhibitory constant was evaluated against Endothelin A receptorThe inhibitory constant was evaluated against Endothelin A receptor
ChEMBL None None None CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CN(Cc1ccccc1)C(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC 10.1016/S0960-894X(01)81219-1
10836474 61436 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 432 9 1 5 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc(OC)cc2OC)cc1 10.1021/jm031041j
CHEMBL177287 61436 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 432 9 1 5 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc(OC)cc2OC)cc1 10.1021/jm031041j
10788853 6018 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)cc3OC)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10808 6018 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)cc3OC)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10717504 98048 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 430 6 0 6 4.5 COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL276173 98048 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 430 6 0 6 4.5 COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10717504 98048 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 430 6 0 6 4.5 COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL276173 98048 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 430 6 0 6 4.5 COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1016/S0960-894X(97)00002-4
10522605 205041 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 361 6 1 4 5.0 Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1C#N)CO 10.1021/jm970847e
CHEMBL90191 205041 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 361 6 1 4 5.0 Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1C#N)CO 10.1021/jm970847e
10595639 205332 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 375 6 1 4 5.1 Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1C#N)C(=O)O 10.1021/jm970847e
CHEMBL91810 205332 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 375 6 1 4 5.1 Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1C#N)C(=O)O 10.1021/jm970847e
10697377 60746 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 523 10 4 6 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL176513 60746 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 523 10 4 6 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL3349461 209653 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00089a028
18617366 167262 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL430822 167262 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1Br 10.1016/0960-894X(96)00441-6
44314864 102549 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 566 11 5 5 3.4 CCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL307077 102549 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 566 11 5 5 3.4 CCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
10788691 205026 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 428 6 1 3 6.0 Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1Br)C(=O)O 10.1021/jm970847e
CHEMBL90094 205026 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 428 6 1 3 6.0 Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1Br)C(=O)O 10.1021/jm970847e
127035544 135824 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 721 14 2 9 7.4 CCCc1nc2c(C)cc(C(=O)NCCc3cc(OC)ccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3734870 135824 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 721 14 2 9 7.4 CCCc1nc2c(C)cc(C(=O)NCCc3cc(OC)ccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
10549875 59473 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2cccc3c2OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL172691 59473 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2cccc3c2OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL2367550 207829 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
10506524 60837 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 536 9 4 5 4.2 CNC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C 10.1021/jm950592+
CHEMBL176565 60837 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 536 9 4 5 4.2 CNC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C 10.1021/jm950592+
10743900 127272 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 497 11 4 5 4.0 CCN(CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C)o1 10.1021/jm950592+
CHEMBL366387 127272 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 497 11 4 5 4.0 CCN(CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C)o1 10.1021/jm950592+
CHEMBL432683 211876 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44368396 44325 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 506 8 2 5 4.9 COc1ccc(C(=O)N(Cc2cc3c(cc2Cl)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL152017 44325 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 506 8 2 5 4.9 COc1ccc(C(=O)N(Cc2cc3c(cc2Cl)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
95285 96811 33 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 256 3 2 5 1.7 O=S(=O)(Nc1nccs1)c1ccc(O)cc1 10.1021/jm00008a013
CHEMBL26894 96811 33 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 256 3 2 5 1.7 O=S(=O)(Nc1nccs1)c1ccc(O)cc1 10.1021/jm00008a013
CHEMBL1791272 207164 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
10027408 96684 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 463 10 2 5 6.1 Cc1noc(NS(=O)(=O)c2cccc3c(NCCCCCc4ccccc4)cccc23)c1C 10.1021/jm00008a013
CHEMBL26786 96684 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 463 10 2 5 6.1 Cc1noc(NS(=O)(=O)c2cccc3c(NCCCCCc4ccccc4)cccc23)c1C 10.1021/jm00008a013
23445410 105651 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 412 4 1 5 4.6 Cc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL313551 105651 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 412 4 1 5 4.6 Cc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
23445379 129564 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 456 6 1 6 4.8 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL367776 129564 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 456 6 1 6 4.8 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
44459299 89163 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 520 7 3 6 4.4 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2c[nH]c3cc(C(=O)O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL23752 89163 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 520 7 3 6 4.4 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2c[nH]c3cc(C(=O)O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
44293754 101482 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 531 9 2 10 3.5 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(c1nn[nH]n1)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL301371 101482 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 531 9 2 10 3.5 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(c1nn[nH]n1)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10552051 100689 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 463 6 2 9 3.3 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2 10.1021/jm9608366
CHEMBL295583 100689 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 463 6 2 9 3.3 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2 10.1021/jm9608366
18704821 99347 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 419 5 1 5 3.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1-c1ccccc1 10.1016/S0960-894X(97)00228-X
CHEMBL285512 99347 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 419 5 1 5 3.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1-c1ccccc1 10.1016/S0960-894X(97)00228-X
44279367 99280 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 485 11 5 4 2.0 CC(C)C[C@H](NC(=O)N1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL285031 99280 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 485 11 5 4 2.0 CC(C)C[C@H](NC(=O)N1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
10575356 9602 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 446 8 1 4 3.7 CCCN(C)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113184 9602 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 446 8 1 4 3.7 CCCN(C)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10551532 110082 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 450 8 1 4 3.9 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL325444 110082 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 450 8 1 4 3.9 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
127035219 135822 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 677 12 2 8 7.4 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3734849 135822 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 677 12 2 8 7.4 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
44293719 96195 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 581 12 2 10 3.9 CCOc1ccc2c(c1)[C@@H](c1cc(OC)c(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL263723 96195 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 581 12 2 10 3.9 CCOc1ccc2c(c1)[C@@H](c1cc(OC)c(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
11800505 61891 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 536 11 3 6 5.1 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H](CC(=O)NC2CCCCC2)CC(C)C)nc1C(=O)O 10.1021/jm9505932
CHEMBL177839 61891 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 536 11 3 6 5.1 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H](CC(=O)NC2CCCCC2)CC(C)C)nc1C(=O)O 10.1021/jm9505932
10570511 205370 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 360 6 1 4 4.2 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(N)=O)c1ccccc1 10.1021/jm970847e
CHEMBL92092 205370 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 360 6 1 4 4.2 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(N)=O)c1ccccc1 10.1021/jm970847e
44276577 106361 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 459 7 1 7 4.1 COc1cccc(Cn2[nH]c(-c3ccc([N+](=O)[O-])cc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144850 106361 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 459 7 1 7 4.1 COc1cccc(Cn2[nH]c(-c3ccc([N+](=O)[O-])cc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
10357554 97102 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1021/jm00004a012
CHEMBL27065 97102 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1021/jm00004a012
44368539 44904 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 475 9 2 6 3.9 COc1cccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)c1 10.1016/s0960-894x(01)00009-9
CHEMBL152552 44904 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 475 9 2 6 3.9 COc1cccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)c1 10.1016/s0960-894x(01)00009-9
10476286 95968 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 403 6 1 7 3.2 CCOC(=O)c1c(C)noc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm00008a013
CHEMBL26206 95968 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 403 6 1 7 3.2 CCOC(=O)c1c(C)noc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm00008a013
127037496 135867 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 613 12 2 7 6.9 CCCCNC(=O)c1cc(C)c2nc(CCC)n(Cc3ccc(-c4ccccc4S(=O)(=O)Nc4onc(C)c4C)cc3)c2c1 10.1039/C4MD00499J
CHEMBL3735311 135867 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 613 12 2 7 6.9 CCCCNC(=O)c1cc(C)c2nc(CCC)n(Cc3ccc(-c4ccccc4S(=O)(=O)Nc4onc(C)c4C)cc3)c2c1 10.1039/C4MD00499J
22998508 205195 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 412 4 1 5 4.6 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL91073 205195 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 412 4 1 5 4.6 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
10020445 100885 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2ccc3cccc(N(C)C)c3c2)c1C 10.1021/jm00008a013
CHEMBL29705 100885 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2ccc3cccc(N(C)C)c3c2)c1C 10.1021/jm00008a013
10020445 100885 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2ccc3cccc(N(C)C)c3c2)c1C 10.1021/jm00004a012
CHEMBL29705 100885 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2ccc3cccc(N(C)C)c3c2)c1C 10.1021/jm00004a012
10645779 96708 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 419 4 1 4 4.2 Cc1cc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
CHEMBL268116 96708 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 419 4 1 4 4.2 Cc1cc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
10832243 201800 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 358 5 1 6 2.5 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1 10.1021/jm9604585
CHEMBL6624 201800 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 358 5 1 6 2.5 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1 10.1021/jm9604585
10692649 201407 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 404 4 1 3 4.5 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)cc3)cccc12 10.1021/jm9604585
CHEMBL6400 201407 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 404 4 1 3 4.5 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Br)cc3)cccc12 10.1021/jm9604585
CHEMBL293874 209137 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)CN(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00089a028
18738879 89788 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 548 8 2 7 4.8 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL23833 89788 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 548 8 2 7 4.8 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21 10.1016/s0960-894x(01)00660-6
18738879 89788 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 548 8 2 7 4.8 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21 10.1007/s00044-004-0021-y
CHEMBL23833 89788 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 548 8 2 7 4.8 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21 10.1007/s00044-004-0021-y
10548486 173534 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 391 5 2 6 3.7 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm9608366
CHEMBL45456 173534 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 391 5 2 6 3.7 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm9608366
44327661 164027 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 483 5 1 8 2.7 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL421563 164027 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 483 5 1 8 2.7 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44327226 206168 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 7 1 8 3.1 CCc1cc(C)nn(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c1=O 10.1016/S0960-894X(96)00617-8
CHEMBL96762 206168 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 7 1 8 3.1 CCc1cc(C)nn(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c1=O 10.1016/S0960-894X(96)00617-8
CHEMBL132542 206951 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)CN(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10647372 205378 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 8 1 6 3.1 CCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9212 205378 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 8 1 6 3.1 CCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL329609 209562 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)CC 10.1021/jm00015a003
10665805 97713 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 354 4 1 6 3.0 CCC1=C(c2ccc3c(c2)OCO3)C(=O)OC1(O)c1ccc(OC)cc1 10.1021/jm9606507
CHEMBL273951 97713 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 354 4 1 6 3.0 CCC1=C(c2ccc3c(c2)OCO3)C(=O)OC1(O)c1ccc(OC)cc1 10.1021/jm9606507
44298381 194220 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 476 9 2 7 4.9 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL55909 194220 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 476 9 2 7 4.9 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCO)c1 10.1016/s0960-894x(00)00366-8
44279408 104169 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 521 13 6 4 2.7 CC(C)C[C@H](NC(=O)NCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31051 104169 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 521 13 6 4 2.7 CC(C)C[C@H](NC(=O)NCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
44327868 110943 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 906 24 9 8 3.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC12CC3CC(CC(C3)C1)C2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL327523 110943 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 906 24 9 8 3.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC12CC3CC(CC(C3)C1)C2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL2369713 207900 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
CHEMBL1793934 207179 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm970161m
44327399 160983 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 539 7 1 8 4.2 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3cccs3)CCC2=O)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL412865 160983 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 539 7 1 8 4.2 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3cccs3)CCC2=O)cc1 10.1016/S0960-894X(96)00617-8
44327734 206350 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 561 8 1 9 3.9 COc1ccc(-c2ccc(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL97851 206350 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 561 8 1 9 3.9 COc1ccc(-c2ccc(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL282340 209096 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](N)C(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)O 10.1016/0960-894X(95)00221-E
44284506 167385 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL 596 14 4 4 4.6 CC(C)C[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)[C@@H](CC(C)C)NC(=O)Cc1ccccc1Cl)C(=O)O 10.1021/jm00087a001
CHEMBL431699 167385 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL 596 14 4 4 4.6 CC(C)C[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)[C@@H](CC(C)C)NC(=O)Cc1ccccc1Cl)C(=O)O 10.1021/jm00087a001
10555806 12001 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 616 12 2 7 6.0 CC(C)OCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL1184095 12001 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 616 12 2 7 6.0 CC(C)OCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL332289 12001 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 616 12 2 7 6.0 CC(C)OCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
23445505 201854 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 412 5 1 7 4.0 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1016/S0960-894X(97)00367-3
CHEMBL66641 201854 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 412 5 1 7 4.0 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1016/S0960-894X(97)00367-3
44314676 102438 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 589 12 5 4 4.6 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL306171 102438 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 589 12 5 4 4.6 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
10577388 15388 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)ccc2C)cc1 10.1021/jm990170q
CHEMBL122111 15388 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)ccc2C)cc1 10.1021/jm990170q
10625270 112863 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C)cc1 10.1021/jm990170q
CHEMBL331767 112863 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C)cc1 10.1021/jm990170q
70240112 171027 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 626 10 2 11 5.0 CC#CCOc1nc(-c2ccnc(-c3nnn[nH]3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL4465332 171027 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 626 10 2 11 5.0 CC#CCOc1nc(-c2ccnc(-c3nnn[nH]3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
44310016 202133 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 489 6 1 9 4.8 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC 10.1016/s0960-894x(97)10151-2
CHEMBL68557 202133 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 489 6 1 9 4.8 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC 10.1016/s0960-894x(97)10151-2
44386143 130157 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 571 9 3 6 5.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL368360 130157 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 571 9 3 6 5.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
44310016 202133 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 489 6 1 9 4.8 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC 10.1021/jm0300429
CHEMBL68557 202133 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 489 6 1 9 4.8 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC 10.1021/jm0300429
CHEMBL422285 211527 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CCC[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44279312 106828 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 565 12 6 4 3.5 CC(C)C[C@H](NC(=O)NC12CC3CC(CC(C3)C1)C2)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31746 106828 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 565 12 6 4 3.5 CC(C)C[C@H](NC(=O)NC12CC3CC(CC(C3)C1)C2)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
44305079 101608 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL302189 101608 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
44293813 183517 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 581 12 2 10 3.9 CCOc1ccc2c(c1)[C@H](c1cc(OC)c(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL48261 183517 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 581 12 2 10 3.9 CCOc1ccc2c(c1)[C@H](c1cc(OC)c(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
44270523 48337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 724 14 1 9 8.0 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL15573 48337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 724 14 1 9 8.0 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL404763 210775 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44293716 100933 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 433 6 1 6 4.0 COc1ccc([C@@H]2c3cc(OC)ccc3[C@@H](c3ccc4c(c3)OCO4)N2CC(=O)O)cc1 10.1016/s0960-894x(01)00273-6
CHEMBL297353 100933 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 433 6 1 6 4.0 COc1ccc([C@@H]2c3cc(OC)ccc3[C@@H](c3ccc4c(c3)OCO4)N2CC(=O)O)cc1 10.1016/s0960-894x(01)00273-6
18936171 194821 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 489 7 1 8 4.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2c(OC)c(OC)ccc21 10.1016/S0960-894X(97)00319-3
CHEMBL56348 194821 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 489 7 1 8 4.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2c(OC)c(OC)ccc21 10.1016/S0960-894X(97)00319-3
44332546 106716 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 491 5 0 7 5.7 O=C(OCc1ccc2c(c1)OCO2)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
CHEMBL316648 106716 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 491 5 0 7 5.7 O=C(OCc1ccc2c(c1)OCO2)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
5329 168898 114 None - 0 Rat 3.5 pIC50 = 3.5 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1 10.1016/s0960-894x(00)00366-8
CHEMBL443 168898 114 None - 0 Rat 3.5 pIC50 = 3.5 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1 10.1016/s0960-894x(00)00366-8
44322947 204964 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 428 5 1 6 4.3 COc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL89689 204964 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 428 5 1 6 4.3 COc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
10067069 99013 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 360 4 1 6 3.0 COC(=O)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL283195 99013 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 360 4 1 6 3.0 COC(=O)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
44385805 60952 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 532 10 1 10 4.1 C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176698 60952 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 532 10 1 10 4.1 C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10230375 129114 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 534 9 2 11 2.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL367317 129114 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 534 9 2 11 2.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
44384557 130855 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 504 9 1 10 3.3 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL369003 130855 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 504 9 1 10 3.3 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
23445547 111837 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2cc(-c3ccccc3)cs2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL329375 111837 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2cc(-c3ccccc3)cs2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL303204 209163 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00089a028
22467219 84910 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 492 6 2 7 3.3 Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1 10.1007/s00044-004-0021-y
CHEMBL2261362 84910 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 492 6 2 7 3.3 Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1 10.1007/s00044-004-0021-y
44320461 105855 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 514 6 1 5 6.6 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00513-8
CHEMBL313920 105855 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 514 6 1 5 6.6 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00513-8
10457385 112178 0 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 469 6 1 8 2.5 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL330424 112178 0 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 469 6 1 8 2.5 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL263537 208818 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10670664 205576 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 438 8 2 6 2.6 C=CCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9342 205576 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 438 8 2 6 2.6 C=CCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10792636 167939 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 544 10 2 6 5.4 CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.1021/jm990170q
CHEMBL435385 167939 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 544 10 2 6 5.4 CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.1021/jm990170q
44327423 205797 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 483 6 1 8 2.8 Cc1cc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)nc1C 10.1016/S0960-894X(96)00617-8
CHEMBL94720 205797 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 483 6 1 8 2.8 Cc1cc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)nc1C 10.1016/S0960-894X(96)00617-8
9998563 96384 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c2ccccc12 10.1021/jm00008a013
CHEMBL26527 96384 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c2ccccc12 10.1021/jm00008a013
10895198 100473 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cccc(OCCC)c21 10.1021/jm010382z
CHEMBL294123 100473 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cccc(OCCC)c21 10.1021/jm010382z
44298612 193842 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 281 4 2 5 1.9 CCc1c(NS(=O)(=O)c2ccc(N)cc2)noc1C 10.1016/s0960-894x(00)00366-8
CHEMBL55405 193842 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 281 4 2 5 1.9 CCc1c(NS(=O)(=O)c2ccc(N)cc2)noc1C 10.1016/s0960-894x(00)00366-8
9998563 96384 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c2ccccc12 10.1021/jm00004a012
CHEMBL26527 96384 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c2ccccc12 10.1021/jm00004a012
44332638 4295 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 477 6 0 6 6.0 COc1ccc(COC(=O)C(c2ccc3c(c2)OCO3)c2c3ccccc3nc3ccccc23)cc1 10.1016/S0960-894X(96)00551-3
CHEMBL101239 4295 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 477 6 0 6 6.0 COc1ccc(COC(=O)C(c2ccc3c(c2)OCO3)c2c3ccccc3nc3ccccc23)cc1 10.1016/S0960-894X(96)00551-3
137643691 157701 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 569 10 2 7 5.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4088634 157701 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 569 10 2 7 5.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
23445538 59741 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 456 6 1 6 4.8 Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL173805 59741 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 456 6 1 6 4.8 Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
23445272 127215 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 440 6 1 5 4.7 Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
CHEMBL366364 127215 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 440 6 1 5 4.7 Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
10615322 201718 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 316 4 1 7 1.9 COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C 10.1016/S0960-894X(97)00367-3
CHEMBL65639 201718 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 316 4 1 7 1.9 COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C 10.1016/S0960-894X(97)00367-3
11762081 201619 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 7 1 5 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm031041j
CHEMBL64851 201619 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 7 1 5 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm031041j
CHEMBL307324 209223 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
ChEMBL None None None CC(C)C[C@H]1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(=O)O)C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(C)C)C(=O)N1C 10.1021/jm00089a028
CHEMBL319719 209465 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10503067 8071 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 436 5 1 6 4.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCCC2)cc1 10.1021/jm9606507
CHEMBL10919 8071 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 436 5 1 6 4.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCCC2)cc1 10.1021/jm9606507
11762081 201619 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 446 7 1 5 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL64851 201619 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 446 7 1 5 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
155519245 169765 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 592 10 2 10 4.2 COc1ccc(Cl)c(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(N3CCOCC3)nc2OCCO)c1 10.1016/j.bmcl.2016.06.014
CHEMBL4447261 169765 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 592 10 2 10 4.2 COc1ccc(Cl)c(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(N3CCOCC3)nc2OCCO)c1 10.1016/j.bmcl.2016.06.014
22467240 98717 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 558 7 2 9 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(-c4nn[nH]n4)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL281378 98717 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 558 7 2 9 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(-c4nn[nH]n4)ccc23)cc1 10.1016/s0960-894x(01)00660-6
10305334 128512 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 680 12 2 11 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL367036 128512 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 680 12 2 11 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL138120 206999 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@@H]1C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(=O)O)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C(C)C)C(=O)N1C 10.1021/jm00021a021
11133491 101686 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 416 3 1 6 4.2 O=C(O)C1=C(c2ccc3c(c2)OCO3)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
CHEMBL302659 101686 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 416 3 1 6 4.2 O=C(O)C1=C(c2ccc3c(c2)OCO3)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
10950843 201254 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cccc(OC)c1)O2 10.1021/jm010382z
CHEMBL62951 201254 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cccc(OC)c1)O2 10.1021/jm010382z
44279370 106709 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 426 4 2 3 4.7 CCc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
CHEMBL31662 106709 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 426 4 2 3 4.7 CCc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
CHEMBL1790451 207136 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C)[C@H](C)O)C1c2ccccc2CCc2ccccc21 10.1016/0960-894X(95)00349-X
10790376 166345 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 466 6 1 6 3.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N2CCCCC2)cc1 10.1021/jm9505369
CHEMBL428644 166345 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 466 6 1 6 3.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N2CCCCC2)cc1 10.1021/jm9505369
44266655 4959 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 445 5 1 7 4.5 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10523 4959 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 445 5 1 7 4.5 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
44371420 50622 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL157763 50622 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
10425958 99478 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc(N)c3ccccc23)c1C 10.1021/jm00008a013
CHEMBL286406 99478 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc(N)c3ccccc23)c1C 10.1021/jm00008a013
CHEMBL438194 211995 7 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
44327881 161114 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 1044 26 9 8 6.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL413179 161114 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 1044 26 9 8 6.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44298613 193844 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 287 3 2 5 2.0 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Cl 10.1016/s0960-894x(00)00366-8
CHEMBL55406 193844 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 287 3 2 5 2.0 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Cl 10.1016/s0960-894x(00)00366-8
CHEMBL438768 212038 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
44277387 106354 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 450 7 2 6 3.0 O=C(O)COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144800 106354 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 450 7 2 6 3.0 O=C(O)COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
10425958 99478 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc(N)c3ccccc23)c1C 10.1021/jm00004a012
CHEMBL286406 99478 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc(N)c3ccccc23)c1C 10.1021/jm00004a012
44266645 206013 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 417 5 1 6 4.7 COc1ccc(-n2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OC)ccc32)cc1 10.1016/0960-894X(96)00170-9
CHEMBL9588 206013 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 417 5 1 6 4.7 COc1ccc(-n2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OC)ccc32)cc1 10.1016/0960-894X(96)00170-9
127034918 135922 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 599 11 2 7 6.6 CCCNC(=O)c1cc(C)c2nc(CCC)n(Cc3ccc(-c4ccccc4S(=O)(=O)Nc4onc(C)c4C)cc3)c2c1 10.1039/C4MD00499J
CHEMBL3735797 135922 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 599 11 2 7 6.6 CCCNC(=O)c1cc(C)c2nc(CCC)n(Cc3ccc(-c4ccccc4S(=O)(=O)Nc4onc(C)c4C)cc3)c2c1 10.1039/C4MD00499J
CHEMBL263025 208803 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)CNC(=O)[C@@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44386523 132048 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 621 10 4 6 5.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2c(F)c(F)c(F)c(F)c2F)nc1C(=O)O 10.1021/jm950592+
CHEMBL369874 132048 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 621 10 4 6 5.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2c(F)c(F)c(F)c(F)c2F)nc1C(=O)O 10.1021/jm950592+
CHEMBL421190 211511 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL2304009 207710 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
CHEMBL87243 214106 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
44327347 96302 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 1102 26 9 8 7.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL264579 96302 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 1102 26 9 8 7.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44368516 44543 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 451 11 2 6 4.1 COc1ccc(CN(Cc2cc(OC)cc(OC)c2)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL152203 44543 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 451 11 2 6 4.1 COc1ccc(CN(Cc2cc(OC)cc(OC)c2)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
10816835 61041 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 567 11 4 5 5.7 CCCc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
CHEMBL176992 61041 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 567 11 4 5 5.7 CCCc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
137652304 156672 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 544 10 3 8 3.7 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCN)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4076290 156672 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 544 10 3 8 3.7 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCN)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
22998446 106137 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL314320 106137 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)c1Br 10.1016/S0960-894X(96)00496-9
443289 702 40 None 2 3 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at Homo sapiens (human) ETA receptorAntagonist activity at Homo sapiens (human) ETA receptor
ChEMBL None None None None 10.1007/s00044-013-0542-3
997 702 40 None 2 3 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at Homo sapiens (human) ETA receptorAntagonist activity at Homo sapiens (human) ETA receptor
ChEMBL None None None None 10.1007/s00044-013-0542-3
CHEMBL314691 702 40 None 2 3 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at Homo sapiens (human) ETA receptorAntagonist activity at Homo sapiens (human) ETA receptor
ChEMBL None None None None 10.1007/s00044-013-0542-3
DB12054 702 40 None 2 3 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at Homo sapiens (human) ETA receptorAntagonist activity at Homo sapiens (human) ETA receptor
ChEMBL None None None None 10.1007/s00044-013-0542-3
11798762 204887 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 475 9 1 7 3.1 CCCS(=O)(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8911 204887 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 475 9 1 7 3.1 CCCS(=O)(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10768346 131008 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 522 10 5 5 4.0 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL369202 131008 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 522 10 5 5 4.0 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O 10.1021/jm950592+
24997097 18272 2 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 501 7 3 7 4.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1272137 18272 2 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 501 7 3 7 4.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
44309445 102213 4 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 370 4 1 5 3.4 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4c(c3)OCO4)cccc12 10.1016/s0960-894x(97)10151-2
CHEMBL304761 102213 4 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 370 4 1 5 3.4 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc4c(c3)OCO4)cccc12 10.1016/s0960-894x(97)10151-2
10816963 112817 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 574 12 2 7 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1 10.1021/jm990170q
CHEMBL331625 112817 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 574 12 2 7 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1 10.1021/jm990170q
CHEMBL289687 209120 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
10602726 165222 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 549 10 4 5 5.1 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)o1 10.1021/jm950591h
CHEMBL424764 165222 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 549 10 4 5 5.1 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)o1 10.1021/jm950591h
44332623 4683 1 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 320 3 1 4 2.9 Cc1cc(C(C(N)=O)c2ccc3c(c2)OCO3)c2ccccc2n1 10.1016/S0960-894X(96)00551-3
CHEMBL103886 4683 1 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 320 3 1 4 2.9 Cc1cc(C(C(N)=O)c2ccc3c(c2)OCO3)c2ccccc2n1 10.1016/S0960-894X(96)00551-3
137655285 158419 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 568 10 3 10 3.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCCN)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4096211 158419 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 568 10 3 10 3.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCCN)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
44177614 129116 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 547 10 1 9 5.4 C=CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL367339 129116 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 547 10 1 9 5.4 C=CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
22467229 98487 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 519 7 2 7 4.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CN)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL279703 98487 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 519 7 2 7 4.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CN)ccc23)cc1 10.1016/s0960-894x(01)00660-6
44385008 130826 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 574 10 2 9 4.9 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368829 130826 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 574 10 2 9 4.9 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
19010493 97891 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 543 11 1 7 6.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL275179 97891 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 543 11 1 7 6.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
42630532 18200 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 541 10 2 7 4.9 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271479 18200 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 541 10 2 7 4.9 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
42630532 18200 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 541 10 2 7 4.9 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271479 18200 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 541 10 2 7 4.9 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
24997097 18272 2 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 501 7 3 7 4.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1272137 18272 2 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 501 7 3 7 4.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
10173807 50594 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 455 6 1 6 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL157742 50594 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 455 6 1 6 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
18995990 98884 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 507 7 1 9 5.0 COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)c1 10.1016/0960-894X(96)00232-6
CHEMBL282426 98884 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 507 7 1 9 5.0 COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)c1 10.1016/0960-894X(96)00232-6
10160887 99673 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 447 5 1 7 5.0 O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00232-6
CHEMBL28779 99673 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 447 5 1 7 5.0 O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00232-6
CHEMBL411797 211200 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44298277 193319 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 474 9 1 7 5.1 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54773 193319 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 474 9 1 7 5.1 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC=O)c1 10.1016/s0960-894x(00)00366-8
10288713 101560 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 473 7 1 7 4.6 CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL301840 101560 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
ChEMBL 473 7 1 7 4.6 CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL62514 214057 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C)C1c2ccccc2CCc2ccccc21 10.1016/0960-894X(95)00349-X
10383832 167605 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc2c1 10.1021/jm00008a013
CHEMBL433234 167605 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc2c1 10.1021/jm00008a013
10540843 85398 8 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 282 4 1 3 4.0 Cc1c(C(=O)O)oc2cccc(OCc3ccccc3)c12 10.1007/s00044-013-0542-3
CHEMBL2296889 85398 8 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 282 4 1 3 4.0 Cc1c(C(=O)O)oc2cccc(OCc3ccccc3)c12 10.1007/s00044-013-0542-3
CHEMBL408141 210946 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
18617407 203262 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL76576 203262 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
44276886 106337 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 410 4 1 4 4.2 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1Cl 10.1016/s0960-894x(00)00232-8
CHEMBL3144600 106337 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 410 4 1 4 4.2 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1Cl 10.1016/s0960-894x(00)00232-8
44277368 106349 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 480 8 2 7 3.0 COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144733 106349 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 480 8 2 7 3.0 COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
10070783 96596 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL267094 96596 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
10383832 167605 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc2c1 10.1021/jm00004a012
CHEMBL433234 167605 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2cc(S(=O)(=O)Nc3onc(C)c3C)ccc2c1 10.1021/jm00004a012
44368482 44417 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 523 8 2 7 4.2 O=C(O)C(Cc1ccc(O)cc1)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
CHEMBL152091 44417 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 523 8 2 7 4.2 O=C(O)C(Cc1ccc(O)cc1)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
4550514 96744 6 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 386 5 3 5 3.7 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)c1C 10.1021/jm00008a013
CHEMBL26842 96744 6 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 386 5 3 5 3.7 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)c1C 10.1021/jm00008a013
127035083 135820 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 677 12 2 8 7.4 CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)cc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3734835 135820 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 677 12 2 8 7.4 CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)cc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
76320429 85400 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL 324 4 1 6 3.6 Cc1c(C(=O)O)oc2cccc(OCc3ccc4nonc4c3)c12 10.1007/s00044-013-0542-3
CHEMBL2296900 85400 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL 324 4 1 6 3.6 Cc1c(C(=O)O)oc2cccc(OCc3ccc4nonc4c3)c12 10.1007/s00044-013-0542-3
10875450 9716 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 565 11 1 10 4.9 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2nccc(C)n2)c1 10.1021/jm0102304
CHEMBL113927 9716 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 565 11 1 10 4.9 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2nccc(C)n2)c1 10.1021/jm0102304
18704814 99647 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 475 7 1 5 4.9 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
CHEMBL287581 99647 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 475 7 1 5 4.9 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1016/S0960-894X(97)00228-X
44279173 106766 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 476 6 2 6 3.1 CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccccc1 10.1016/S0960-894X(97)00228-X
CHEMBL31696 106766 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 476 6 2 6 3.1 CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccccc1 10.1016/S0960-894X(97)00228-X
44279237 110030 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 462 6 2 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccccc1 10.1016/S0960-894X(97)00228-X
CHEMBL32512 110030 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
ChEMBL 462 6 2 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccccc1 10.1016/S0960-894X(97)00228-X
44309996 202055 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 483 5 1 8 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4nsnc4c3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(97)10151-2
CHEMBL67971 202055 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 483 5 1 8 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4nsnc4c3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(97)10151-2
CHEMBL342913 209939 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None COC(=O)C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm00021a021
44279300 106038 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined
ChEMBL 472 13 5 4 2.4 CC(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31405 106038 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membrane was determinedBinding affinity against ETA receptor in porcine aortic smooth muscle membrane was determined
ChEMBL 472 13 5 4 2.4 CC(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
44279350 167602 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 428 4 2 4 4.2 COc1cccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)c1 10.1016/0960-894X(95)00230-Q
CHEMBL433229 167602 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 428 4 2 4 4.2 COc1cccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)c1 10.1016/0960-894X(95)00230-Q
10390467 96667 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 481 6 1 5 6.4 Cc1noc(NS(=O)(=O)c2cccc3c(N=C(c4ccccc4)c4ccccc4)cccc23)c1C 10.1021/jm00008a013
CHEMBL26776 96667 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 481 6 1 5 6.4 Cc1noc(NS(=O)(=O)c2cccc3c(N=C(c4ccccc4)c4ccccc4)cccc23)c1C 10.1021/jm00008a013
10373814 14715 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Displacement of [125]ET1 from ETA receptor in pig thoracic aortaDisplacement of [125]ET1 from ETA receptor in pig thoracic aorta
ChEMBL 1016 2 6 12 7.0 O=C1NCCc2ccc(c(Br)c2)Oc2cc(ccc2O)CCNC(=O)/C(=N/O)Cc2cc(Br)c(OS(=O)(=O)O)c(c2)Oc2c(Br)cc(cc2Br)C/C1=N\O 10.1021/np50099a026
CHEMBL1207961 14715 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Displacement of [125]ET1 from ETA receptor in pig thoracic aortaDisplacement of [125]ET1 from ETA receptor in pig thoracic aorta
ChEMBL 1016 2 6 12 7.0 O=C1NCCc2ccc(c(Br)c2)Oc2cc(ccc2O)CCNC(=O)/C(=N/O)Cc2cc(Br)c(OS(=O)(=O)O)c(c2)Oc2c(Br)cc(cc2Br)C/C1=N\O 10.1021/np50099a026
CHEMBL465400 14715 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Displacement of [125]ET1 from ETA receptor in pig thoracic aortaDisplacement of [125]ET1 from ETA receptor in pig thoracic aorta
ChEMBL 1016 2 6 12 7.0 O=C1NCCc2ccc(c(Br)c2)Oc2cc(ccc2O)CCNC(=O)/C(=N/O)Cc2cc(Br)c(OS(=O)(=O)O)c(c2)Oc2c(Br)cc(cc2Br)C/C1=N\O 10.1021/np50099a026
10793886 59490 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 615 11 4 5 6.3 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)s1 10.1021/jm950591h
CHEMBL172760 59490 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 615 11 4 5 6.3 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)s1 10.1021/jm950591h
10625083 204910 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 10 1 5 5.3 CCCCN(CCCC)C(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8925 204910 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 10 1 5 5.3 CCCCN(CCCC)C(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10833400 161333 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 376 4 1 5 3.5 Cc1cc(Cl)nnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
CHEMBL415106 161333 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 376 4 1 5 3.5 Cc1cc(Cl)nnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
11793650 96862 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 372 6 1 6 2.9 CCOc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1 10.1021/jm9604585
CHEMBL269237 96862 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 372 6 1 6 2.9 CCOc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nn1 10.1021/jm9604585
25211074 18284 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in membranes by radioligand assayAntagonist activity at ETA receptor (unknown origin) expressed in membranes by radioligand assay
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1272244 18284 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in membranes by radioligand assayAntagonist activity at ETA receptor (unknown origin) expressed in membranes by radioligand assay
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL405599 210811 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10767505 5213 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 494 6 1 8 3.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm9606507
CHEMBL10661 5213 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 494 6 1 8 3.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm9606507
10673715 9445 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 528 14 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(F)(F)F 10.1021/jm980217s
CHEMBL112314 9445 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 528 14 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(F)(F)F 10.1021/jm980217s
10650210 102300 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 545 9 1 9 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN3CCOCC3)c2)cc1 10.1021/jm980504w
CHEMBL305267 102300 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 545 9 1 9 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN3CCOCC3)c2)cc1 10.1021/jm980504w
10361993 99092 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 373 5 1 5 4.1 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C(C)C)cccc23)c1C 10.1021/jm00004a012
CHEMBL283652 99092 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 373 5 1 5 4.1 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C(C)C)cccc23)c1C 10.1021/jm00004a012
44304492 96099 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
CHEMBL262993 96099 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
CHEMBL133257 206963 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Inhibitory effect against porcine ET-A receptorInhibitory effect against porcine ET-A receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44311232 202399 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 658 13 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70293 202399 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 658 13 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44311233 202400 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 630 12 2 13 4.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70303 202400 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 630 12 2 13 4.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL133257 206963 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10961277 100535 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 446 5 2 6 4.9 CC(C)Oc1ccc2c(c1)C(c1ccc(O)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL294496 100535 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 446 5 2 6 4.9 CC(C)Oc1ccc2c(c1)C(c1ccc(O)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10391968 187840 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL50232 187840 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
25211074 18284 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1272244 18284 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
11058717 201119 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 412 8 1 6 4.6 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCC)cc21 10.1021/jm010382z
CHEMBL62348 201119 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 412 8 1 6 4.6 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCC)cc21 10.1021/jm010382z
9807200 84907 0 None 346 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261359 84907 0 None 346 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
71451528 81263 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 631 14 1 12 4.3 CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL2163715 81263 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 631 14 1 12 4.3 CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
21041249 81236 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 648 11 1 8 4.7 CN(Cc1ccccc1)S(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2163688 81236 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 648 11 1 8 4.7 CN(Cc1ccccc1)S(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
71451525 81245 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 629 12 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
CHEMBL2163697 81245 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 629 12 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
71451528 81263 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 631 14 1 12 4.3 CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163715 81263 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 631 14 1 12 4.3 CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
11059576 201593 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL64726 201593 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
21041266 81586 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 584 10 2 8 3.3 O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)NC1CC1 10.1021/jm3009103
CHEMBL2165340 81586 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 584 10 2 8 3.3 O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)NC1CC1 10.1021/jm3009103
10625633 205400 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 514 12 1 8 2.4 COCCN(CCOC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9223 205400 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 514 12 1 8 2.4 COCCN(CCOC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10697636 167246 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 536 13 1 7 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1SCCS1 10.1021/jm980217s
CHEMBL430683 167246 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 536 13 1 7 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1SCCS1 10.1021/jm980217s
10279940 100868 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 527 8 2 10 3.6 CC(=O)OCCc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
CHEMBL296927 100868 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 527 8 2 10 3.6 CC(=O)OCCc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
44333578 4522 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 417 5 1 5 4.4 CCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL102773 4522 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 417 5 1 5 4.4 CCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
44439111 96715 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 979 31 2 15 7.0 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL268201 96715 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 979 31 2 15 7.0 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1 10.1016/j.bmcl.2006.10.009
44295032 14606 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 520 10 1 9 4.7 COc1cccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c1 10.1016/s0960-894x(98)00301-1
CHEMBL1206717 14606 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 520 10 1 9 4.7 COc1cccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c1 10.1016/s0960-894x(98)00301-1
CHEMBL299572 14606 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 520 10 1 9 4.7 COc1cccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c1 10.1016/s0960-894x(98)00301-1
9959298 60176 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 552 10 2 7 5.4 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL175698 60176 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 552 10 2 7 5.4 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
10625530 205301 3 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm031041j
CHEMBL9162 205301 3 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm031041j
10625530 205301 3 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9162 205301 3 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10917653 201677 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 468 11 1 6 6.1 CCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL65292 201677 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 468 11 1 6 6.1 CCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
104865 697 94 None 1 4 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human ETA receptorBinding affinity to human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
3494 697 94 None 1 4 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human ETA receptorBinding affinity to human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
392 697 94 None 1 4 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human ETA receptorBinding affinity to human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
CHEMBL957 697 94 None 1 4 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human ETA receptorBinding affinity to human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
DB00559 697 94 None 1 4 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human ETA receptorBinding affinity to human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
104865 697 94 None -1 4 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
3494 697 94 None -1 4 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
392 697 94 None -1 4 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
CHEMBL957 697 94 None -1 4 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
DB00559 697 94 None -1 4 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
17885921 106305 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccn2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL314454 106305 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccn2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
11798504 96662 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 468 9 1 6 3.5 CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267695 96662 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 468 9 1 6 3.5 CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10648135 9237 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 472 13 1 5 4.7 C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL111218 9237 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 472 13 1 5 4.7 C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
44314581 104385 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 591 11 6 5 2.8 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
CHEMBL311134 104385 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 591 11 6 5 2.8 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
11798504 96662 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 468 9 1 6 3.5 CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267695 96662 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 468 9 1 6 3.5 CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
11113473 201669 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 472 6 1 5 6.3 CC(C)Oc1ccc2c(c1)C(c1ccc(C(C)C)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL65201 201669 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 472 6 1 5 6.3 CC(C)Oc1ccc2c(c1)C(c1ccc(C(C)C)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL2304006 207707 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None O=C(O)C[C@H]1NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm9600914
44320419 106578 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 496 7 2 6 5.1 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCC(C(=O)O)CC1 10.1016/s0960-894x(00)00513-8
CHEMBL315805 106578 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 496 7 2 6 5.1 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCC(C(=O)O)CC1 10.1016/s0960-894x(00)00513-8
10576428 14403 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 473 8 2 6 4.3 COc1ccc(C(=O)/C(Cc2ccc(NC(C)=O)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL10905 14403 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 473 8 2 6 4.3 COc1ccc(C(=O)/C(Cc2ccc(NC(C)=O)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL1204673 14403 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 473 8 2 6 4.3 COc1ccc(C(=O)/C(Cc2ccc(NC(C)=O)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL328942 209560 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
18617318 105121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2ccccc2Br)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL312266 105121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2ccccc2Br)c1Br 10.1016/0960-894X(96)00441-6
10526002 7953 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 417 5 1 7 3.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccnc2)cc1 10.1021/jm9606507
CHEMBL10910 7953 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 417 5 1 7 3.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccnc2)cc1 10.1021/jm9606507
CHEMBL2304018 207719 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
18004820 16261 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 527 9 2 7 4.7 CCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL12333 16261 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 527 9 2 7 4.7 CCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
71456865 81276 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 632 14 2 11 3.7 COc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1021/jm3009103
CHEMBL2163727 81276 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 632 14 2 11 3.7 COc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1021/jm3009103
10504148 205518 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 459 10 1 5 6.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ccccn1 10.1021/jm9707131
CHEMBL92965 205518 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 459 10 1 5 6.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ccccn1 10.1021/jm9707131
104865 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
3494 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
392 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
CHEMBL957 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
DB00559 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
CHEMBL2369709 207897 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
CHEMBL405100 210786 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00349-X
CHEMBL438820 212042 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00349-X
10002033 100530 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 417 7 2 7 3.6 CCOC(=O)C(C)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL29448 100530 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 417 7 2 7 3.6 CCOC(=O)C(C)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
10718141 5137 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 444 5 1 7 3.6 COC(=O)c1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10622 5137 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 444 5 1 7 3.6 COC(=O)c1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10027018 98024 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 454 4 1 5 5.1 O=C1OC(O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL275991 98024 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 454 4 1 5 5.1 O=C1OC(O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
44279413 99477 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 400 2 2 3 3.3 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL286395 99477 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 400 2 2 3 3.3 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21 10.1016/0960-894X(95)00230-Q
10716071 205575 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 401 7 1 5 5.4 O=[N+]([O-])c1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1Cl 10.1021/jm970847e
CHEMBL93411 205575 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 401 7 1 5 5.4 O=[N+]([O-])c1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1Cl 10.1021/jm970847e
44298330 101065 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 518 10 1 8 5.4 COC(=O)CCCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1 10.1016/s0960-894x(00)00366-8
CHEMBL298340 101065 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 518 10 1 8 5.4 COC(=O)CCCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1 10.1016/s0960-894x(00)00366-8
CHEMBL85341 214101 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
10792782 130829 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368847 130829 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL147510 207026 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
The inhibitory constant was evaluated against Endothelin A receptorThe inhibitory constant was evaluated against Endothelin A receptor
ChEMBL None None None CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC 10.1016/S0960-894X(01)81219-1
10087191 101354 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C 10.1021/jm00029a001
CHEMBL30039 101354 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C 10.1021/jm00029a001
10087191 101354 1 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C 10.1021/jm00008a013
CHEMBL30039 101354 1 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2cccc3c(N)cccc23)c1C 10.1021/jm00008a013
5329 168898 114 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1 10.1021/jm00008a013
CHEMBL443 168898 114 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1 10.1021/jm00008a013
CHEMBL405709 210819 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
5329 168898 114 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1 10.1021/jm00004a012
CHEMBL443 168898 114 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1 10.1021/jm00004a012
44327619 205695 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 511 6 1 8 3.5 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C(C)(C)C)ccc2=O)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL94102 205695 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 511 6 1 8 3.5 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C(C)(C)C)ccc2=O)cc1 10.1016/S0960-894X(96)00617-8
44327714 206191 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 575 8 1 9 4.2 COc1ccc(-c2cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL96935 206191 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 575 8 1 9 4.2 COc1ccc(-c2cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1 10.1016/S0960-894X(96)00617-8
182140 188498 27 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cellsDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells
ChEMBL 430 8 0 7 3.7 COC[C@@H]1Cc2cc(OC)c3c(c2[C@H](c2ccc(OC)c(OC)c2)[C@H]1COC)OCO3 10.1021/np50124a006
CHEMBL510130 188498 27 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cellsDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells
ChEMBL 430 8 0 7 3.7 COC[C@@H]1Cc2cc(OC)c3c(c2[C@H](c2ccc(OC)c(OC)c2)[C@H]1COC)OCO3 10.1021/np50124a006
44277130 98982 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 450 8 1 7 3.6 COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCCO)c1 10.1016/s0960-894x(00)00232-8
CHEMBL283037 98982 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 450 8 1 7 3.6 COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCCO)c1 10.1016/s0960-894x(00)00232-8
44277131 106339 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 380 5 1 3 4.0 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(F)cc3)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144603 106339 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 380 5 1 3 4.0 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(F)cc3)c2=O)c1 10.1016/s0960-894x(00)00232-8
44357135 115734 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL 642 10 6 8 -0.1 CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)c2ccccc2NC=O)NC1=O 10.1021/jm00021a021
CHEMBL335863 115734 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL 642 10 6 8 -0.1 CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)c2ccccc2NC=O)NC1=O 10.1021/jm00021a021
10814222 9446 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 470 10 1 6 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL112325 9446 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 470 10 1 6 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
18995992 99364 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 507 7 1 9 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL28563 99364 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 507 7 1 9 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
44339755 9672 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 551 12 1 7 2.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CN1CCCCS1(=O)=O 10.1021/jm980217s
CHEMBL113589 9672 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 551 12 1 7 2.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CN1CCCCS1(=O)=O 10.1021/jm980217s
10763680 120256 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 403 7 1 6 4.1 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1 10.1021/jm990378b
CHEMBL355413 120256 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 403 7 1 6 4.1 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1 10.1021/jm990378b
9894460 204972 6 None -24 3 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/S0960-894X(96)00617-8
CHEMBL313871 204972 6 None -24 3 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/S0960-894X(96)00617-8
CHEMBL8978 204972 6 None -24 3 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/S0960-894X(96)00617-8
10554410 119863 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 538 10 3 7 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)OC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL353320 119863 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 538 10 3 7 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)OC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
10916597 201615 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm031041j
CHEMBL64832 201615 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm031041j
CHEMBL304756 209219 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00089a028
11058658 201548 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 409 7 1 5 4.8 CCCCC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL64558 201548 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 409 7 1 5 4.8 CCCCC1=C(C(N)=O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL337897 209844 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
4642915 97475 1 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 402 5 3 5 4.1 Cc1noc(NS(=O)(=O)c2ccc(N/C(S)=N/c3ccccc3)cc2)c1C 10.1021/jm00008a013
CHEMBL27256 97475 1 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 402 5 3 5 4.1 Cc1noc(NS(=O)(=O)c2ccc(N/C(S)=N/c3ccccc3)cc2)c1C 10.1021/jm00008a013
44213925 111200 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 593 9 1 9 4.1 COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1OC 10.1016/S0960-894X(96)00617-8
CHEMBL328683 111200 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 593 9 1 9 4.1 COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1OC 10.1016/S0960-894X(96)00617-8
44266532 4419 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 401 3 1 6 4.5 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10211 4419 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 401 3 1 6 4.5 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
10816264 59599 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 539 9 4 5 5.0 Cc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
CHEMBL173181 59599 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 539 9 4 5 5.0 Cc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
10840476 131306 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 553 10 4 5 5.3 CCc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
CHEMBL369420 131306 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 553 10 4 5 5.3 CCc1sc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
23445345 201362 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 378 5 1 7 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1C 10.1016/S0960-894X(97)00367-3
CHEMBL63611 201362 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 378 5 1 7 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1C 10.1016/S0960-894X(97)00367-3
10280531 162369 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 541 10 2 7 5.1 CCCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL417429 162369 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 541 10 2 7 5.1 CCCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
10366742 106611 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 454 6 1 5 5.5 CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(96)00496-9
CHEMBL316012 106611 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 454 6 1 5 5.5 CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(96)00496-9
44371410 49141 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 439 5 1 5 5.5 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL156453 49141 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 439 5 1 5 5.5 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL406279 210845 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
44383187 59834 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 617 13 4 5 4.5 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCc1cccc(CCC(=O)O)c1 10.1016/0960-894X(95)00144-I
CHEMBL173974 59834 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 617 13 4 5 4.5 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCc1cccc(CCC(=O)O)c1 10.1016/0960-894X(95)00144-I
15296635 99081 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 488 11 5 5 2.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL283591 99081 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 488 11 5 5 2.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
44279516 99376 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 512 13 5 5 2.6 CC(C)C[C@H](NC(=O)Cc1cccs1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL285729 99376 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 512 13 5 5 2.6 CC(C)C[C@H](NC(=O)Cc1cccs1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
15340613 106348 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 414 6 1 5 4.2 COc1cccc(Cn2[nH]c(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144732 106348 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 414 6 1 5 4.2 COc1cccc(Cn2[nH]c(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
44317215 203542 2 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 266 3 1 4 2.4 Cc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/0960-894X(96)00441-6
CHEMBL78952 203542 2 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 266 3 1 4 2.4 Cc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/0960-894X(96)00441-6
10816963 112817 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 574 12 2 7 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1 10.1021/jm990170q
CHEMBL331625 112817 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 574 12 2 7 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1 10.1021/jm990170q
CHEMBL1791015 207162 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44368417 44382 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 504 12 2 6 4.9 COc1ccc(CN(Cc2cc(OC)c(OC)c(OC)c2)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL152065 44382 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 504 12 2 6 4.9 COc1ccc(CN(Cc2cc(OC)c(OC)c(OC)c2)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
10383833 99633 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc2c1 10.1021/jm00008a013
CHEMBL28751 99633 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc2c1 10.1021/jm00008a013
10383833 99633 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc2c1 10.1021/jm00004a012
CHEMBL28751 99633 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2ccc(S(=O)(=O)Nc3onc(C)c3C)cc2c1 10.1021/jm00004a012
CHEMBL265066 96354 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Tested for its inhibitory activity against Endothelin A receptorTested for its inhibitory activity against Endothelin A receptor
ChEMBL 646 8 2 13 5.8 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC(=O)C2=C(C)N=C(C)/C(=C(/O)OC)[C@@H]2c2cccc([N+](=O)[O-])c2)[C@H]1c1cccc([N+](=O)[O-])c1 10.1016/S0960-894X(01)81025-8
9913198 5233 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 484 5 1 6 4.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(C(F)(F)F)c2)cc1 10.1021/jm9606507
CHEMBL10676 5233 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 484 5 1 6 4.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(C(F)(F)F)c2)cc1 10.1021/jm9606507
11733450 201720 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 6 1 7 5.0 CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL65658 201720 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 6 1 7 5.0 CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10502577 12283 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
CHEMBL1185771 12283 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
CHEMBL432109 12283 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
10599829 96668 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 9 2 6 3.2 CCCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267761 96668 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 9 2 6 3.2 CCCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44266575 4560 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 459 6 1 7 5.2 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10302 4560 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 459 6 1 7 5.2 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
44317005 203307 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL76949 203307 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
10070783 96596 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL267094 96596 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
44298305 192980 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 504 10 2 7 5.3 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(=O)O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL53097 192980 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 504 10 2 7 5.3 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(=O)O)c1 10.1016/s0960-894x(00)00366-8
44276948 106340 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 396 5 1 3 4.5 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)cc3)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144604 106340 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 396 5 1 3 4.5 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)cc3)c2=O)c1 10.1016/s0960-894x(00)00232-8
9820754 108062 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 371 3 0 5 4.4 COC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
CHEMBL320236 108062 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 371 3 0 5 4.4 COC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
10604167 12296 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 640 10 2 6 6.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1185826 12296 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 640 10 2 6 6.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL434986 12296 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 640 10 2 6 6.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
10647172 205029 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 449 6 1 5 4.6 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2Cc2ccc(F)cc2)cc1 10.1021/jm9505369
CHEMBL9012 205029 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 449 6 1 5 4.6 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2Cc2ccc(F)cc2)cc1 10.1021/jm9505369
44265906 96807 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 441 9 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOCC(C)C)cc1 10.1021/jm9505369
CHEMBL268902 96807 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 441 9 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOCC(C)C)cc1 10.1021/jm9505369
18617377 203753 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 344 3 1 4 3.2 Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
CHEMBL80484 203753 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 344 3 1 4 3.2 Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
10668427 164781 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 395 7 1 6 3.8 N#Cc1ccc(OCc2ccnnc2)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
CHEMBL423608 164781 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 395 7 1 6 3.8 N#Cc1ccc(OCc2ccnnc2)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
10765750 162597 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 445 8 1 6 3.0 CC[S+]([O-])CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL417972 162597 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 445 8 1 6 3.0 CC[S+]([O-])CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44383753 59736 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 466 5 1 5 5.7 Cc1cc(C)c(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL173761 59736 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 466 5 1 5 5.7 Cc1cc(C)c(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
44439105 168134 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 848 26 2 12 6.5 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOc2ccc(-c3ccccc3S(=O)(=O)Nc3ccno3)c(CN(C)C(=O)CC(C)(C)C)c2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL436821 168134 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 848 26 2 12 6.5 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOc2ccc(-c3ccccc3S(=O)(=O)Nc3ccno3)c(CN(C)C(=O)CC(C)(C)C)c2)cc1 10.1016/j.bmcl.2006.10.009
10357554 97102 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1016/0960-894X(96)00441-6
CHEMBL27065 97102 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1016/0960-894X(96)00441-6
10972369 167494 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 448 6 3 6 4.9 COc1ccc(C2=C(C(=O)O)C(c3ccc(O)c(O)c3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL432489 167494 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 448 6 3 6 4.9 COc1ccc(C2=C(C(=O)O)C(c3ccc(O)c(O)c3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
11801544 61433 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 589 10 4 6 5.1 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2C3CC4CC(C3)CC2C4)nc1C(=O)O 10.1021/jm950592+
CHEMBL177261 61433 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 589 10 4 6 5.1 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2C3CC4CC(C3)CC2C4)nc1C(=O)O 10.1021/jm950592+
CHEMBL135907 206983 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O 10.1021/jm00021a021
23445562 100136 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 398 5 1 7 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1Cl 10.1016/S0960-894X(97)00367-3
CHEMBL291891 100136 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 398 5 1 7 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccccc2)c1Cl 10.1016/S0960-894X(97)00367-3
CHEMBL438194 211995 7 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
CHEMBL34540 209951 13 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.
ChEMBL None None None None 10.1021/jm00087a001
104865 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
3494 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
392 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
CHEMBL957 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
DB00559 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
10839947 116786 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 530 9 2 6 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL339657 116786 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 530 9 2 6 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
104865 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
3494 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
392 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
CHEMBL957 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
DB00559 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-ET1 from human smooth muscle ETA receptorDisplacement of 125I-ET1 from human smooth muscle ETA receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
104865 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
3494 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
392 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
CHEMBL957 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
DB00559 697 94 None 1 4 Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
10741025 181089 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1cc(C)cc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
CHEMBL47765 181089 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1cc(C)cc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
18184234 61865 0 None - 2 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 605 15 2 10 4.2 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL177802 61865 0 None - 2 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 605 15 2 10 4.2 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
10599230 205257 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm031041j
CHEMBL9141 205257 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm031041j
10599230 205257 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9141 205257 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
11767189 9849 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 601 11 1 10 5.8 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cnc3ccccc3n2)c1 10.1021/jm0102304
CHEMBL114704 9849 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 601 11 1 10 5.8 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cnc3ccccc3n2)c1 10.1021/jm0102304
10793053 11338 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 564 9 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1180363 11338 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 564 9 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL123994 11338 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 564 9 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
15340617 98767 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 464 8 1 7 3.7 COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL281677 98767 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 464 8 1 7 3.7 COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
44386621 60933 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL176653 60933 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
10650331 132038 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 551 10 3 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)N(C)C(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL369821 132038 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 551 10 3 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)N(C)C(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
56678451 62981 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 25 8 8 4.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(c1ccccc1)c1ccccc1)N(C)C(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
CHEMBL1793927 62981 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 25 8 8 4.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(c1ccccc1)c1ccccc1)N(C)C(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
10205429 61262 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 470 8 2 9 2.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL177111 61262 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 470 8 2 9 2.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
71458717 81244 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 433 9 2 10 1.5 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCO 10.1021/jm3009103
CHEMBL2163696 81244 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 433 9 2 10 1.5 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCO 10.1021/jm3009103
10598840 60156 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 432 9 1 5 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)cc(OC)c2)cc1 10.1021/jm031041j
CHEMBL175545 60156 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 432 9 1 5 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)cc(OC)c2)cc1 10.1021/jm031041j
10670372 96785 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)cc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL268754 96785 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)cc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44314664 202980 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 615 12 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CCCC1)C(=O)O 10.1021/jm9600914
CHEMBL74000 202980 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 615 12 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CCCC1)C(=O)O 10.1021/jm9600914
76330201 84911 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 526 6 1 7 4.5 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(Cl)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261363 84911 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 526 6 1 7 4.5 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(Cl)ccc12 10.1007/s00044-004-0021-y
10479787 59288 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 6 1 5 5.3 Cc1cc(C)c(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL171972 59288 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 6 1 5 5.3 Cc1cc(C)c(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
18995988 99860 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 389 6 1 4 5.5 COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3ccccc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL28948 99860 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 389 6 1 4 5.5 COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3ccccc23)c1 10.1016/0960-894X(96)00232-6
10029811 97494 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 525 8 2 5 6.4 Cc1noc(NS(=O)(=O)c2cccc3c(NC(=O)CC(c4ccccc4)c4ccccc4)cccc23)c1C 10.1021/jm00008a013
CHEMBL27262 97494 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 525 8 2 5 6.4 Cc1noc(NS(=O)(=O)c2cccc3c(NC(=O)CC(c4ccccc4)c4ccccc4)cccc23)c1C 10.1021/jm00008a013
44279127 99015 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 432 3 2 3 4.8 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL283200 99015 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 432 3 2 3 4.8 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3)cc21 10.1016/0960-894X(95)00230-Q
10815168 167577 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 5 2 6 5.2 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)(C)C)cc2)c1Br 10.1021/jm9608366
CHEMBL433074 167577 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 5 2 6 5.2 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)(C)C)cc2)c1Br 10.1021/jm9608366
9869444 96784 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1 10.1016/0960-894X(96)00170-9
CHEMBL268751 96784 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1 10.1016/0960-894X(96)00170-9
CHEMBL342440 209918 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CCC[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O 10.1021/jm00021a021
23445250 167532 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 468 6 1 5 5.8 Cc1cc(CC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL432815 167532 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 468 6 1 5 5.8 Cc1cc(CC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
44316515 203285 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 360 4 1 5 2.9 COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL76779 203285 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 360 4 1 5 2.9 COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
44314472 103308 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 594 13 5 5 4.2 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL309003 103308 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 594 13 5 5 4.2 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
10626177 60057 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 535 11 4 5 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)CC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL174871 60057 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 535 11 4 5 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)CC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
44283420 161231 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 594 13 5 5 4.2 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL414175 161231 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 594 13 5 5 4.2 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
23548251 81255 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 661 16 1 14 4.0 COc1cc(OC)nc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)n1 10.1021/jm3009103
CHEMBL2163707 81255 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 661 16 1 14 4.0 COc1cc(OC)nc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)n1 10.1021/jm3009103
11801523 8157 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 588 16 1 7 5.3 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCC)cc1 10.1021/jm970101g
CHEMBL109242 8157 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 588 16 1 7 5.3 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCC)cc1 10.1021/jm970101g
10961960 201178 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 487 8 1 7 4.4 CCCCC1=C(C(=O)NS(C)(=O)=O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL62633 201178 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 487 8 1 7 4.4 CCCCC1=C(C(=O)NS(C)(=O)=O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL304260 209217 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00349-X
9830495 130614 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 618 14 2 9 5.0 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL368617 130614 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 618 14 2 9 5.0 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
137661460 158816 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 565 10 2 9 4.4 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4100579 158816 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 565 10 2 9 4.4 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL2370255 208064 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10645550 96890 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 416 5 1 6 3.8 COc1ccccc1C1(O)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1ccccc1 10.1021/jm9606507
CHEMBL269461 96890 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 416 5 1 6 3.8 COc1ccccc1C1(O)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1ccccc1 10.1021/jm9606507
11145841 100474 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 528 9 1 6 6.9 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC3CCCC3)cc1)O2 10.1021/jm010382z
CHEMBL294127 100474 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 528 9 1 6 6.9 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC3CCCC3)cc1)O2 10.1021/jm010382z
44279129 106499 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 428 4 2 4 4.2 COc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21 10.1016/0960-894X(95)00230-Q
CHEMBL31524 106499 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 428 4 2 4 4.2 COc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21 10.1016/0960-894X(95)00230-Q
44277245 106351 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 392 6 1 4 3.9 COc1ccc(Cc2c(C(F)(F)F)[nH]n(Cc3cccc(OC)c3)c2=O)cc1 10.1016/s0960-894x(00)00232-8
CHEMBL3144736 106351 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 392 6 1 4 3.9 COc1ccc(Cc2c(C(F)(F)F)[nH]n(Cc3cccc(OC)c3)c2=O)cc1 10.1016/s0960-894x(00)00232-8
44385522 59299 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 642 13 2 11 4.2 CCS(=O)(=O)NCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL172029 59299 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 642 13 2 11 4.2 CCS(=O)(=O)NCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9808545 11332 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 588 11 2 7 5.2 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL1180353 11332 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 588 11 2 7 5.2 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL123408 11332 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 588 11 2 7 5.2 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
10571380 59746 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 373 7 1 4 4.7 Cc1ccccc1C(Oc1cc(OCc2ccccc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL173838 59746 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 373 7 1 4 4.7 Cc1ccccc1C(Oc1cc(OCc2ccccc2)ccc1C#N)C(=O)O 10.1021/jm990378b
9845967 10974 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL10801 10974 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL1178000 10974 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL51530 10974 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL433853 211889 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)(C)S)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44371450 48585 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(OC)c(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1 10.1016/s0960-894x(99)00040-2
CHEMBL155937 48585 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(OC)c(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1 10.1016/s0960-894x(99)00040-2
15453210 203525 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 376 5 1 6 2.6 COc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1OC 10.1016/0960-894X(96)00441-6
CHEMBL78853 203525 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 376 5 1 6 2.6 COc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1OC 10.1016/0960-894X(96)00441-6
44316458 203720 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 408 3 1 4 3.6 Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1C 10.1016/0960-894X(96)00441-6
CHEMBL80317 203720 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 408 3 1 4 3.6 Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1C 10.1016/0960-894X(96)00441-6
10404449 99031 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 331 4 1 5 3.0 Cc1cnoc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm00008a013
CHEMBL283300 99031 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 331 4 1 5 3.0 Cc1cnoc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm00008a013
9865706 97669 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 400 4 1 5 4.1 Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL273613 97669 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 400 4 1 5 4.1 Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44385523 60723 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 666 13 2 9 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL176418 60723 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 666 13 2 9 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL409777 211027 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
9957883 98191 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 507 7 1 9 5.0 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL27732 98191 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 507 7 1 9 5.0 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
10626031 109197 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 529 13 1 7 2.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1C(=O)CCC1=O 10.1021/jm980217s
CHEMBL322799 109197 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 529 13 1 7 2.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1C(=O)CCC1=O 10.1021/jm980217s
10767210 110814 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL326719 110814 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
9871837 15019 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 535 10 2 7 4.9 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1039/C4MD00499J
CHEMBL12106 15019 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 535 10 2 7 4.9 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1039/C4MD00499J
44458650 84465 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 521 7 2 8 2.7 COc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
CHEMBL22367 84465 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 521 7 2 8 2.7 COc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
10619391 59907 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL173251 59907 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL174092 59907 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O 10.1021/jm990378b
10547407 77947 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1[C@H](Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL2110232 77947 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1[C@H](Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O 10.1021/jm990378b
10453733 111806 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cccnc2)ccc1C#N 10.1021/jm9707131
CHEMBL329181 111806 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cccnc2)ccc1C#N 10.1021/jm9707131
9953204 205689 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
CHEMBL94071 205689 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
10210086 60937 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 571 10 2 12 3.0 C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176664 60937 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 571 10 2 12 3.0 C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10361107 161487 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 5 2 5 4.1 Cc1noc(NS(=O)(=O)c2cccc3c(NC(C)C)cccc23)c1C 10.1021/jm00004a012
CHEMBL416026 161487 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 5 2 5 4.1 Cc1noc(NS(=O)(=O)c2cccc3c(NC(C)C)cccc23)c1C 10.1021/jm00004a012
CHEMBL64271 214066 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00349-X
10281929 9288 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 588 16 1 7 5.3 CCCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL111517 9288 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 588 16 1 7 5.3 CCCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
10553490 180524 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 501 8 3 10 2.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2OCCO)OCO3)c1Cl 10.1021/jm9608366
CHEMBL47604 180524 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 501 8 3 10 2.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2OCCO)OCO3)c1Cl 10.1021/jm9608366
44386921 60936 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)[C@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm031041j
CHEMBL176661 60936 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)[C@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm031041j
10721344 7444 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 548 13 1 8 3.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCOC 10.1021/jm970101g
CHEMBL108748 7444 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 548 13 1 8 3.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCOC 10.1021/jm970101g
10918390 19110 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 522 12 1 5 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
CHEMBL129060 19110 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 522 12 1 5 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
9807178 201293 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63121 201293 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10767280 108168 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 486 14 1 5 5.1 C=C(C)CCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL320763 108168 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 486 14 1 5 5.1 C=C(C)CCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
44458669 84236 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 505 6 2 7 3.0 Cc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
CHEMBL22249 84236 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 505 6 2 7 3.0 Cc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
107810 1646 25 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 604 12 4 6 3.4 CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C 10.1016/0960-894X(95)00144-I
998 1646 25 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 604 12 4 6 3.4 CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C 10.1016/0960-894X(95)00144-I
CHEMBL352396 1646 25 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 604 12 4 6 3.4 CC(C[C@@H](C(=O)N[C@@H](C(=O)N[C@@H](C(=O)O)Cc1ccccn1)Cc1cn(c2c1cccc2)C)NC(=O)N1CCCCCC1)C 10.1016/0960-894X(95)00144-I
22009947 84906 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261358 84906 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
9984193 100675 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1021/jm031041j
CHEMBL295440 100675 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1021/jm031041j
9984193 100675 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL295440 100675 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10649119 11318 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 502 8 2 6 4.1 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1180318 11318 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 502 8 2 6 4.1 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL121761 11318 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 502 8 2 6 4.1 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2)cc1 10.1021/jm990171i
73669994 117114 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 429 9 1 7 4.7 N#Cc1ccc(OCc2ccc3nonc3c2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400996 117114 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
ChEMBL 429 9 1 7 4.7 N#Cc1ccc(OCc2ccc3nonc3c2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
44314750 165089 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 647 13 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL424422 165089 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 647 13 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
10140965 100690 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 7 3 9 3.0 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCO)OCO3)c1Cl 10.1021/jm9608366
CHEMBL295588 100690 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 7 3 9 3.0 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCO)OCO3)c1Cl 10.1021/jm9608366
44283419 99840 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 647 13 5 4 5.1 CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL289349 99840 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 647 13 5 4 5.1 CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
44314905 203328 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 567 12 5 4 4.0 CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL77083 203328 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 567 12 5 4 4.0 CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
44333867 4559 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 403 4 1 5 4.1 COc1ccc([C@@H]2c3nc(C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL103001 4559 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 403 4 1 5 4.1 COc1ccc([C@@H]2c3nc(C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
10415822 129284 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 579 9 3 7 4.7 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCOC23CCCCC3)nc1C(=O)O 10.1021/jm950592+
CHEMBL367551 129284 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 579 9 3 7 4.7 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCOC23CCCCC3)nc1C(=O)O 10.1021/jm950592+
11798998 205098 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 482 10 1 6 3.9 CCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9050 205098 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 482 10 1 6 3.9 CCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
122272 96637 23 None 1 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1016/0960-894X(96)00441-6
CHEMBL267458 96637 23 None 1 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1016/0960-894X(96)00441-6
10415348 60747 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 557 9 3 6 4.8 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL176514 60747 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 557 9 3 6 4.8 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL438733 212033 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]2CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N2)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00077a013
10647642 8001 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 460 6 2 7 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(C(=O)O)c2)cc1 10.1021/jm9606507
CHEMBL10915 8001 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 460 6 2 7 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(C(=O)O)c2)cc1 10.1021/jm9606507
11799625 113286 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)c(C)c2)cc1 10.1021/jm990170q
CHEMBL332431 113286 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)c(C)c2)cc1 10.1021/jm990170q
9871561 174218 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 527 10 2 8 4.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4562189 174218 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
ChEMBL 527 10 2 8 4.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO 10.1016/j.bmcl.2016.06.014
9873255 59307 0 None - 2 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 591 14 2 10 3.8 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL172071 59307 0 None - 2 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 591 14 2 10 3.8 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
122272 96637 23 None 1 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm9604585
CHEMBL267458 96637 23 None 1 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm9604585
10553017 97643 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 488 7 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)c2ccccc2)cc1 10.1021/jm9505369
CHEMBL273476 97643 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 488 7 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)c2ccccc2)cc1 10.1021/jm9505369
10502023 121864 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 416 7 1 5 4.4 COc1cccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)c1 10.1021/jm031041j
CHEMBL360066 121864 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 416 7 1 5 4.4 COc1cccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)c1 10.1021/jm031041j
CHEMBL384728 210577 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
3370402 105298 4 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 252 3 1 4 2.1 Cc1noc(NS(=O)(=O)c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL312670 105298 4 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 252 3 1 4 2.1 Cc1noc(NS(=O)(=O)c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
10740614 97843 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 416 5 1 6 3.8 COc1cccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c1 10.1021/jm9606507
CHEMBL274857 97843 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 416 5 1 6 3.8 COc1cccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c1 10.1021/jm9606507
10714851 111420 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 381 7 1 5 4.9 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1 10.1021/jm970847e
CHEMBL328786 111420 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 381 7 1 5 4.9 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1 10.1021/jm970847e
44211959 55133 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 620 12 1 9 5.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(C)(=O)=O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL16197 55133 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 620 12 1 9 5.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(C)(=O)=O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
44368480 44341 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 495 13 1 7 4.4 COc1ccc(CC(C(=O)O)N(Cc2ccc(OC)cc2)Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL152034 44341 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 495 13 1 7 4.4 COc1ccc(CC(C(=O)O)N(Cc2ccc(OC)cc2)Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(01)00009-9
10017402 101409 2 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 295 5 2 5 2.5 CCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00008a013
CHEMBL30078 101409 2 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 295 5 2 5 2.5 CCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00008a013
44328057 96433 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 986 26 9 9 4.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1cccnc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL265734 96433 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 986 26 9 9 4.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1cccnc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL2370253 208062 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44279351 99469 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 412 3 2 3 4.5 Cc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21 10.1016/0960-894X(95)00230-Q
CHEMBL286333 99469 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 412 3 2 3 4.5 Cc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21 10.1016/0960-894X(95)00230-Q
31771 96505 33 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 267 3 2 5 1.7 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/s0960-894x(00)00366-8
CHEMBL26630 96505 33 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 267 3 2 5 1.7 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/s0960-894x(00)00366-8
10017402 101409 2 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 295 5 2 5 2.5 CCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00004a012
CHEMBL30078 101409 2 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 295 5 2 5 2.5 CCNc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm00004a012
10454873 95962 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 421 6 1 5 4.6 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Cc1ccccc1 10.1021/jm00008a013
CHEMBL26203 95962 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 421 6 1 5 4.6 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Cc1ccccc1 10.1021/jm00008a013
44383536 119878 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Tested for binding affinity towards rabbit Endothelin A receptorTested for binding affinity towards rabbit Endothelin A receptor
ChEMBL 362 3 2 5 2.9 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
CHEMBL353502 119878 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Tested for binding affinity towards rabbit Endothelin A receptorTested for binding affinity towards rabbit Endothelin A receptor
ChEMBL 362 3 2 5 2.9 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
10671298 201751 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 450 6 1 6 3.7 CCOc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
CHEMBL6588 201751 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 450 6 1 6 3.7 CCOc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
10789830 96557 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 453 4 1 4 3.7 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(I)cn3)cccc12 10.1021/jm9604585
CHEMBL266684 96557 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 453 4 1 4 3.7 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(I)cn3)cccc12 10.1021/jm9604585
10740942 201838 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 422 4 2 6 3.0 CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3O)cccc12 10.1021/jm9604585
CHEMBL6647 201838 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 422 4 2 6 3.0 CN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3O)cccc12 10.1021/jm9604585
10595728 201847 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 376 4 1 5 3.5 Cc1cc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nnc1Cl 10.1021/jm9604585
CHEMBL6660 201847 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 376 4 1 5 3.5 Cc1cc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)nnc1Cl 10.1021/jm9604585
10644647 119981 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 399 7 1 5 5.1 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccc(Cl)cc1 10.1021/jm990378b
CHEMBL354428 119981 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 399 7 1 5 5.1 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccc(Cl)cc1 10.1021/jm990378b
9845562 4658 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1 10.1021/jm9606507
CHEMBL10374 4658 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1 10.1021/jm9606507
44279535 103646 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 527 11 5 4 3.2 CC(C)C[C@H](NC(=O)N1C(C)CCCC1C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL30944 103646 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 527 11 5 4 3.2 CC(C)C[C@H](NC(=O)N1C(C)CCCC1C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
44314675 97663 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 603 13 5 4 5.0 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)CC)C(=O)O 10.1021/jm9600914
CHEMBL273583 97663 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 603 13 5 4 5.0 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)CC)C(=O)O 10.1021/jm9600914
CHEMBL2304005 207706 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
9955093 165732 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 443 7 1 5 5.2 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1Br 10.1021/jm990378b
CHEMBL427117 165732 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 443 7 1 5 5.2 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1Br 10.1021/jm990378b
10281606 129137 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 575 9 2 10 4.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL367382 129137 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 575 9 2 10 4.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
9809270 130805 0 None - 2 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 622 14 2 12 2.3 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL368738 130805 0 None - 2 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 622 14 2 12 2.3 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
10896930 9714 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cccnn2)c1 10.1021/jm0102304
CHEMBL113888 9714 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2cccnn2)c1 10.1021/jm0102304
44373550 119332 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 331 3 2 5 2.1 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Br 10.1021/jm00004a012
CHEMBL348641 119332 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 331 3 2 5 2.1 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Br 10.1021/jm00004a012
10647182 109221 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 449 8 2 4 3.9 CCCN(C)C(=O)CN1C[C@H](c2ccc3cc[nH]c3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL322935 109221 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 449 8 2 4 3.9 CCCN(C)C(=O)CN1C[C@H](c2ccc3cc[nH]c3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10579195 130804 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 584 10 5 4 5.7 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)[nH]1 10.1021/jm950591h
CHEMBL368711 130804 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 584 10 5 4 5.7 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)[nH]1 10.1021/jm950591h
10531664 167966 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 601 10 4 5 6.4 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)s1 10.1021/jm950591h
CHEMBL435537 167966 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 601 10 4 5 6.4 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)s1 10.1021/jm950591h
9897092 59606 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 779 17 2 13 6.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL173201 59606 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 779 17 2 13 6.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
23445523 59691 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2sccc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
CHEMBL173557 59691 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2sccc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
9961347 11842 1 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL1182945 11842 1 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL273642 11842 1 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
10764220 205345 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 413 8 1 6 3.3 CCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9189 205345 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 413 8 1 6 3.3 CCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10907399 201258 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 516 11 1 6 6.8 CCCCOc1ccc(C2Oc3ccc(OCCCC)cc3C(c3ccc4c(c3)OCO4)=C2C(=O)O)cc1 10.1021/jm010382z
CHEMBL62976 201258 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 516 11 1 6 6.8 CCCCOc1ccc(C2Oc3ccc(OCCCC)cc3C(c3ccc4c(c3)OCO4)=C2C(=O)O)cc1 10.1021/jm010382z
10745212 131012 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 548 10 5 4 4.9 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)[nH]1 10.1021/jm950591h
CHEMBL369257 131012 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 548 10 5 4 4.9 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)[nH]1 10.1021/jm950591h
10550844 96847 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 435 5 1 6 3.7 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)c2ccco2)cc1 10.1021/jm9505369
CHEMBL269140 96847 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 435 5 1 6 3.7 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)c2ccco2)cc1 10.1021/jm9505369
10548721 59331 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 395 8 1 6 4.4 COc1ccccc1C(Oc1cc(OCc2ccsc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL172164 59331 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 395 8 1 6 4.4 COc1ccccc1C(Oc1cc(OCc2ccsc2)ccc1C#N)C(=O)O 10.1021/jm990378b
44316768 203522 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 358 4 1 4 3.4 CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL78830 203522 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 358 4 1 4 3.4 CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
44279458 99244 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 531 13 6 5 2.0 CC(C)C[C@H](NC(=O)N(CCO)C(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL284785 99244 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 531 13 6 5 2.0 CC(C)C[C@H](NC(=O)N(CCO)C(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
9910709 59021 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 433 7 1 5 5.4 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1C(F)(F)F 10.1021/jm990378b
CHEMBL170715 59021 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 433 7 1 5 5.4 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1C(F)(F)F 10.1021/jm990378b
10144372 165490 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 562 10 2 11 3.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL425682 165490 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 562 10 2 11 3.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
10344511 59356 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 466 5 1 5 5.7 Cc1cc(C)c(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL172248 59356 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 466 5 1 5 5.7 Cc1cc(C)c(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
44279290 106532 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 547 11 5 4 3.0 CC(C)C[C@H](NC(=O)N1CCc2ccccc2C1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31546 106532 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 547 11 5 4 3.0 CC(C)C[C@H](NC(=O)N1CCc2ccccc2C1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
10971076 201166 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 386 3 1 4 4.7 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
CHEMBL62585 201166 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 386 3 1 4 4.7 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
44279128 106416 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 428 4 2 4 4.2 COc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
CHEMBL31469 106416 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 428 4 2 4 4.2 COc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
44298393 198139 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 432 6 1 6 5.2 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2C)c1 10.1016/s0960-894x(00)00366-8
CHEMBL59425 198139 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 432 6 1 6 5.2 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2C)c1 10.1016/s0960-894x(00)00366-8
CHEMBL136583 206987 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10546317 205427 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 358 8 1 2 5.7 O=C(O)CC/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
CHEMBL92402 205427 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 358 8 1 2 5.7 O=C(O)CC/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
10106336 97444 8 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 254 3 2 5 1.5 Cc1cc(NS(=O)(=O)c2ccc(O)cc2)no1 10.1021/jm00008a013
CHEMBL27248 97444 8 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 254 3 2 5 1.5 Cc1cc(NS(=O)(=O)c2ccc(O)cc2)no1 10.1021/jm00008a013
18617394 105137 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 294 3 1 4 3.0 Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1016/0960-894X(96)00441-6
CHEMBL312372 105137 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 294 3 1 4 3.0 Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1016/0960-894X(96)00441-6
10106336 97444 8 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 254 3 2 5 1.5 Cc1cc(NS(=O)(=O)c2ccc(O)cc2)no1 10.1021/jm00004a012
CHEMBL27248 97444 8 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 254 3 2 5 1.5 Cc1cc(NS(=O)(=O)c2ccc(O)cc2)no1 10.1021/jm00004a012
10815167 100710 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 7 2 6 5.4 CCC(C)c1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL295697 100710 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 7 2 6 5.4 CCC(C)c1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
23445313 165074 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL424371 165074 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
44279516 99376 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 512 13 5 5 2.6 CC(C)C[C@H](NC(=O)Cc1cccs1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL285729 99376 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 512 13 5 5 2.6 CC(C)C[C@H](NC(=O)Cc1cccs1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL96822 214133 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NS(C)(=O)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10426645 162513 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C 10.1021/jm00008a013
CHEMBL417651 162513 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C 10.1021/jm00008a013
44291602 100697 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 515 8 2 10 3.6 COC(=O)c1cc(OC)cc(OC)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm9608366
CHEMBL295632 100697 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 515 8 2 10 3.6 COC(=O)c1cc(OC)cc(OC)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl 10.1021/jm9608366
44279409 99384 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 555 11 5 4 4.0 CC(C)C[C@H](NC(=O)N1CCCCCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL285782 99384 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 555 11 5 4 4.0 CC(C)C[C@H](NC(=O)N1CCCCCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
23445533 60076 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 454 6 1 5 5.0 Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL175045 60076 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 454 6 1 5 5.0 Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
18617354 203756 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80507 203756 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
23445445 102174 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 377 5 2 6 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1C 10.1016/S0960-894X(97)00367-3
CHEMBL304481 102174 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 377 5 2 6 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1C 10.1016/S0960-894X(97)00367-3
127034917 135999 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 654 12 2 8 6.2 CCCc1nc2c(C)cc(C(=O)NCCN3CCCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3736507 135999 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 654 12 2 8 6.2 CCCc1nc2c(C)cc(C(=O)NCCN3CCCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
44266628 4682 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 417 5 1 6 4.7 COc1cccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OC)cc23)c1 10.1016/0960-894X(96)00170-9
CHEMBL10388 4682 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 417 5 1 6 4.7 COc1cccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OC)cc23)c1 10.1016/0960-894X(96)00170-9
127035545 135833 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 721 14 2 9 7.4 CCCc1nc2c(C)cc(C(=O)NCCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3734955 135833 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 721 14 2 9 7.4 CCCc1nc2c(C)cc(C(=O)NCCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
11797486 11923 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 442 6 2 8 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL1183448 11923 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 442 6 2 8 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL297557 11923 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 442 6 2 8 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
44279325 111122 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 501 12 6 4 2.5 CC(C)C[C@H](NC(=O)NCC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL32845 111122 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 501 12 6 4 2.5 CC(C)C[C@H](NC(=O)NCC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
76326542 84904 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 504 7 1 6 5.2 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccccc21 10.1007/s00044-004-0021-y
CHEMBL2261356 84904 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 504 7 1 6 5.2 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccccc21 10.1007/s00044-004-0021-y
10337624 99623 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3ccc(N(C)C)cc23)c1C 10.1021/jm00008a013
CHEMBL287451 99623 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3ccc(N(C)C)cc23)c1C 10.1021/jm00008a013
15340616 106338 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 420 4 1 6 3.3 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccc2c(c1)OCO2 10.1016/s0960-894x(00)00232-8
CHEMBL3144602 106338 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 420 4 1 6 3.3 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccc2c(c1)OCO2 10.1016/s0960-894x(00)00232-8
10337624 99623 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3ccc(N(C)C)cc23)c1C 10.1021/jm00004a012
CHEMBL287451 99623 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3ccc(N(C)C)cc23)c1C 10.1021/jm00004a012
CHEMBL137011 206991 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC1=O 10.1021/jm00021a021
127034757 135859 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 679 12 2 7 7.5 CCCc1nc2c(C)cc(C(=O)NCCc3ccc(F)cc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3735265 135859 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 679 12 2 7 7.5 CCCc1nc2c(C)cc(C(=O)NCCc3ccc(F)cc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
10185233 59732 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 497 8 2 8 3.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL173721 59732 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 497 8 2 8 3.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCC#CCO 10.1016/s0960-894x(02)01084-3
44279145 110042 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 515 13 5 4 3.0 CC(C)C[C@H](NC(=O)N(C(C)C)C(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL32518 110042 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 515 13 5 4 3.0 CC(C)C[C@H](NC(=O)N(C(C)C)C(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
44295097 14579 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 604 13 1 9 7.0 COc1ccc(C(=O)/C(Cc2cc(OC(C)C)c(OC(C)C)c(OC(C)C)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1206461 14579 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 604 13 1 9 7.0 COc1ccc(C(=O)/C(Cc2cc(OC(C)C)c(OC(C)C)c(OC(C)C)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL276362 14579 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 604 13 1 9 7.0 COc1ccc(C(=O)/C(Cc2cc(OC(C)C)c(OC(C)C)c(OC(C)C)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
10621170 11121 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 402 5 2 8 3.0 Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1 10.1021/jm9608366
CHEMBL1178890 11121 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 402 5 2 8 3.0 Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1 10.1021/jm9608366
CHEMBL48120 11121 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 402 5 2 8 3.0 Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1 10.1021/jm9608366
10549815 61270 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 416 8 1 4 5.0 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc(C)cc2)cc1 10.1021/jm031041j
CHEMBL177123 61270 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 416 8 1 4 5.0 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc(C)cc2)cc1 10.1021/jm031041j
10047521 8528 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 416 6 1 5 4.4 COc1ccc(CC2=C(c3ccc(C)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL10951 8528 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 416 6 1 5 4.4 COc1ccc(CC2=C(c3ccc(C)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
10815883 59257 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 522 9 5 4 4.3 Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
CHEMBL171855 59257 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 522 9 5 4 4.3 Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
10815883 59257 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 522 9 5 4 4.3 Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL171855 59257 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 522 9 5 4 4.3 Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
10043017 98811 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 342 4 1 4 4.3 C=C(C)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00029a001
CHEMBL281942 98811 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 342 4 1 4 4.3 C=C(C)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00029a001
10043017 98811 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 342 4 1 4 4.3 C=C(C)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL281942 98811 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 342 4 1 4 4.3 C=C(C)c1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
234762 99528 26 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 256 3 2 6 0.9 Nc1ccc(S(=O)(=O)Nc2nncs2)cc1 10.1021/jm00008a013
CHEMBL286737 99528 26 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 256 3 2 6 0.9 Nc1ccc(S(=O)(=O)Nc2nncs2)cc1 10.1021/jm00008a013
44332807 106738 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 447 5 0 5 6.0 O=C(OCc1ccccc1)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
CHEMBL316792 106738 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 447 5 0 5 6.0 O=C(OCc1ccccc1)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
10649086 174671 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 500 5 3 8 4.0 Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL45723 174671 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 500 5 3 8 4.0 Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
18995998 161829 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 523 9 1 9 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL416570 161829 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 523 9 1 9 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
44293631 167229 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 463 7 2 7 4.1 CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL430572 167229 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 463 7 2 7 4.1 CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL328942 209560 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
44265858 167020 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 509 12 1 6 4.1 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(N)=O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL430084 167020 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 509 12 1 6 4.1 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(N)=O)C1c1ccc(OC)cc1 10.1021/jm9505369
44386144 61640 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 555 9 3 7 5.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)n2ccc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL177431 61640 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 555 9 3 7 5.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)n2ccc3ccccc32)nc1C(=O)O 10.1021/jm950592+
23445336 59845 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 6 1 5 5.3 Cc1cc(C)c(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL173977 59845 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 6 1 5 5.3 Cc1cc(C)c(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL2370070 208024 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL216082 207562 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10426645 162513 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL417651 162513 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C 10.1016/0960-894X(96)00441-6
44279333 105726 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 513 11 5 4 2.6 CC(C)C[C@H](NC(=O)N1CCC(C)CC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31388 105726 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 513 11 5 4 2.6 CC(C)C[C@H](NC(=O)N1CCC(C)CC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
44294580 14451 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 502 8 1 7 5.8 COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205104 14451 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 502 8 1 7 5.8 COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL52338 14451 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 502 8 1 7 5.8 COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
127034916 135864 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 668 12 2 8 6.6 CCCc1nc2c(C)cc(C(=O)NCCN3CCCCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3735302 135864 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 668 12 2 8 6.6 CCCc1nc2c(C)cc(C(=O)NCCN3CCCCC3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL432091 211874 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
44384723 130352 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 563 13 2 10 3.0 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL368528 130352 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 563 13 2 10 3.0 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9853025 59489 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 690 14 2 13 3.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL172759 59489 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 690 14 2 13 3.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
44320212 106504 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 520 9 2 7 4.7 O=C(O)COc1ccccc1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
CHEMBL315280 106504 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 520 9 2 7 4.7 O=C(O)COc1ccccc1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
44386161 60932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 573 9 1 9 5.6 CCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176650 60932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 573 9 1 9 5.6 CCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
18996000 98880 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 491 9 1 7 6.1 CCCOc1ccc2c(Sc3cccc(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1 10.1016/0960-894X(96)00232-6
CHEMBL282398 98880 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 491 9 1 7 6.1 CCCOc1ccc2c(Sc3cccc(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1 10.1016/0960-894X(96)00232-6
10476492 168615 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 407 6 2 5 4.9 Cc1noc(NS(=O)(=O)c2cccc3c(NCc4ccccc4)cccc23)c1C 10.1021/jm00008a013
CHEMBL440653 168615 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 407 6 2 5 4.9 Cc1noc(NS(=O)(=O)c2cccc3c(NCc4ccccc4)cccc23)c1C 10.1021/jm00008a013
CHEMBL343379 209943 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory effect against Human Endothelin A receptorInhibitory effect against Human Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O 10.1021/jm00021a021
15453209 203411 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 358 3 1 4 3.5 Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/0960-894X(96)00441-6
CHEMBL77962 203411 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 358 3 1 4 3.5 Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/0960-894X(96)00441-6
19347988 98414 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor
ChEMBL 316 4 1 4 4.8 COc1cccc(Sc2c(C(=O)O)sc3ccccc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL27911 98414 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor
ChEMBL 316 4 1 4 4.8 COc1cccc(Sc2c(C(=O)O)sc3ccccc23)c1 10.1016/0960-894X(96)00232-6
10289348 9208 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 516 16 1 5 5.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(CCC)CCC 10.1021/jm980217s
CHEMBL111023 9208 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 516 16 1 5 5.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(CCC)CCC 10.1021/jm980217s
44215416 174498 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 649 11 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccnc(-c3noc(=S)[nH]3)c2)nc1OCC1CCCO1 10.1016/j.bmcl.2016.06.014
CHEMBL4568468 174498 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 649 11 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccnc(-c3noc(=S)[nH]3)c2)nc1OCC1CCCO1 10.1016/j.bmcl.2016.06.014
44212539 202385 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 671 12 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL70203 202385 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 671 12 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
10739431 59253 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 394 7 1 5 4.4 N#Cc1ccc(OCc2ccncc2)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
CHEMBL171844 59253 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 394 7 1 5 4.4 N#Cc1ccc(OCc2ccncc2)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
10740501 59951 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 414 7 1 6 4.8 Cc1ccccc1C(Oc1cc(OCc2ccc3ncoc3c2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL174235 59951 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 414 7 1 6 4.8 Cc1ccccc1C(Oc1cc(OCc2ccc3ncoc3c2)ccc1C#N)C(=O)O 10.1021/jm990378b
11799541 180677 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 499 8 3 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCCO)OCO3)c1Cl 10.1021/jm9608366
CHEMBL47620 180677 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 499 8 3 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCCO)OCO3)c1Cl 10.1021/jm9608366
44212539 202385 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 671 12 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70203 202385 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 671 12 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44311135 202480 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70800 202480 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44293720 181894 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 551 11 2 9 3.9 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL47868 181894 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 551 11 2 9 3.9 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10554539 100760 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 543 9 2 11 3.4 CC(=O)OCCOc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
CHEMBL296129 100760 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 543 9 2 11 3.4 CC(=O)OCCOc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
137647152 157096 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 581 10 2 9 4.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4081426 157096 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 581 10 2 9 4.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10429404 104386 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 372 5 1 4 3.7 CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
CHEMBL311138 104386 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 372 5 1 4 3.7 CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
44320315 106561 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 496 7 2 7 5.0 O=C(O)c1cccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL315638 106561 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 496 7 2 7 5.0 O=C(O)c1cccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00513-8
11006147 12307 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 550 11 2 10 4.7 COc1cccc(Oc2c(NCCOc3ncccn3)ncnc2NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1 10.1021/jm0102304
CHEMBL1185931 12307 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 550 11 2 10 4.7 COc1cccc(Oc2c(NCCOc3ncccn3)ncnc2NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1 10.1021/jm0102304
CHEMBL442031 12307 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 550 11 2 10 4.7 COc1cccc(Oc2c(NCCOc3ncccn3)ncnc2NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1 10.1021/jm0102304
2809510 128771 5 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cellsInhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cells
ChEMBL 362 5 1 7 2.8 COC(=O)c1cc(S(=O)(=O)Nc2cccc(-c3cnco3)c2)oc1C 10.1021/jm031041j
CHEMBL367093 128771 5 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cellsInhibition of [125]ET-1 binding to human Endothelin A receptor expressed in vero cells
ChEMBL 362 5 1 7 2.8 COC(=O)c1cc(S(=O)(=O)Nc2cccc(-c3cnco3)c2)oc1C 10.1021/jm031041j
10531650 167687 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 600 11 1 7 5.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm970101g
CHEMBL433842 167687 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 600 11 1 7 5.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm970101g
10918533 102357 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 536 8 1 6 6.8 CC(C)Oc1ccc2c(c1)C(c1ccc(OCc3ccccc3)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL305577 102357 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 536 8 1 6 6.8 CC(C)Oc1ccc2c(c1)C(c1ccc(OCc3ccccc3)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
52949155 18212 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 557 10 2 7 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271640 18212 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 557 10 2 7 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
44315008 102345 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL 665 13 5 5 4.7 CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL305524 102345 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL 665 13 5 5 4.7 CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44458604 98148 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 559 6 2 7 3.7 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL276982 98148 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 559 6 2 7 3.7 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
10239569 14604 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 534 9 1 10 4.4 COc1cc(C/C(C(=O)c2ccc3c(c2)OCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1206715 14604 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 534 9 1 10 4.4 COc1cc(C/C(C(=O)c2ccc3c(c2)OCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL299328 14604 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 534 9 1 10 4.4 COc1cc(C/C(C(=O)c2ccc3c(c2)OCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
52943105 18278 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 529 9 2 7 4.7 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1272190 18278 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 529 9 2 7 4.7 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
52943105 18278 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 529 9 2 7 4.7 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1272190 18278 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 529 9 2 7 4.7 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
10137382 181592 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 427 5 3 7 3.8 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(O)c1 10.1021/jm9608366
CHEMBL47827 181592 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 427 5 3 7 3.8 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(O)c1 10.1021/jm9608366
10527706 96540 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 8 1 6 3.1 CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL266594 96540 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 8 1 6 3.1 CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10671037 130909 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL273660 130909 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL369085 130909 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm031041j
10503525 5775 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10794 5775 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44314609 203030 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 720 12 6 4 5.6 CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm9600914
CHEMBL74471 203030 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 720 12 6 4 5.6 CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm9600914
71460535 81259 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 693 15 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)CCCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163711 81259 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 693 15 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)CCCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
11826259 201207 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 437 8 1 7 4.5 CC(C)Oc1ccc2c(c1)C(OCCCC#N)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL62759 201207 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 437 8 1 7 4.5 CC(C)Oc1ccc2c(c1)C(OCCCC#N)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
71455139 81577 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 556 11 2 8 3.6 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccccc1 10.1021/jm3009103
CHEMBL2165331 81577 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 556 11 2 8 3.6 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccccc1 10.1021/jm3009103
10697883 11120 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 548 8 3 10 2.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CNS(C)(=O)=O)OCO3)c1Cl 10.1021/jm9608366
CHEMBL1178885 11120 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 548 8 3 10 2.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CNS(C)(=O)=O)OCO3)c1Cl 10.1021/jm9608366
CHEMBL47828 11120 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 548 8 3 10 2.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CNS(C)(=O)=O)OCO3)c1Cl 10.1021/jm9608366
21979601 81574 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 602 13 2 10 3.7 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL2165328 81574 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 602 13 2 10 3.7 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
71462248 81277 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 676 17 2 12 3.8 COCCOc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1021/jm3009103
CHEMBL2163728 81277 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 676 17 2 12 3.8 COCCOc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1021/jm3009103
21979601 81574 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 602 13 2 10 3.7 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2165328 81574 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 602 13 2 10 3.7 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
10360201 95229 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1onc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00008a013
CHEMBL25816 95229 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1onc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00008a013
9974857 96931 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 5 2 5 3.7 CCNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL26978 96931 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 5 2 5 3.7 CCNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL1788127 209360 8 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL313760 209360 8 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
10506868 62912 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 10 5 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL179138 62912 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 10 5 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
44266594 4122 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 491 8 1 8 4.8 COc1ccc(-c2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)cc1OC 10.1016/0960-894X(96)00170-9
CHEMBL10019 4122 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 491 8 1 8 4.8 COc1ccc(-c2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)cc1OC 10.1016/0960-894X(96)00170-9
44266646 98100 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00170-9
CHEMBL276638 98100 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00170-9
10577879 9164 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 520 9 0 9 4.5 COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL11082 9164 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 520 9 0 9 4.5 COc1ccc(C2(OC)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
345351 9254 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL11131 9254 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
10763444 111143 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 399 7 1 5 5.0 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1F 10.1021/jm970847e
CHEMBL328580 111143 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 399 7 1 5 5.0 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1F 10.1021/jm970847e
10597928 112255 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 414 6 1 3 5.9 Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1Br)CO 10.1021/jm970847e
CHEMBL330543 112255 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 414 6 1 3 5.9 Cc1ccccc1/C(=C\c1cc(OCc2ccsc2)ccc1Br)CO 10.1021/jm970847e
10690863 205126 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 375 7 1 4 4.8 O=C(O)/C(=C/c1cc(OCc2ccccc2)ccc1[N+](=O)[O-])c1ccccc1 10.1021/jm970847e
CHEMBL90666 205126 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 375 7 1 4 4.8 O=C(O)/C(=C/c1cc(OCc2ccccc2)ccc1[N+](=O)[O-])c1ccccc1 10.1021/jm970847e
44277263 106341 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 440 5 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc4c(cc3Cl)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144605 106341 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 440 5 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc4c(cc3Cl)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
10403526 101402 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3cc(N)ccc3c2)c1C 10.1021/jm00004a012
CHEMBL30075 101402 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3cc(N)ccc3c2)c1C 10.1021/jm00004a012
44270522 45533 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 744 15 1 10 8.2 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL15310 45533 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 744 15 1 10 8.2 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
44368390 45036 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 475 9 2 6 3.9 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL152654 45036 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 475 9 2 6 3.9 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
14673588 4326 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Compound was evaluated for binding affinity against rabbit Endothelin A receptorCompound was evaluated for binding affinity against rabbit Endothelin A receptor
ChEMBL 342 6 1 4 5.0 CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12 10.1016/0960-894X(96)00170-9
CHEMBL10143 4326 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Compound was evaluated for binding affinity against rabbit Endothelin A receptorCompound was evaluated for binding affinity against rabbit Endothelin A receptor
ChEMBL 342 6 1 4 5.0 CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12 10.1016/0960-894X(96)00170-9
14673588 4326 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor
ChEMBL 342 6 1 4 5.0 CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12 10.1016/0960-894X(96)00232-6
CHEMBL10143 4326 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptorCompound was evaluated for the receptor binding activity in rabbit artery vascular smooth muscle cells expressing Endothelin A receptor
ChEMBL 342 6 1 4 5.0 CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12 10.1016/0960-894X(96)00232-6
10735178 205462 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 330 6 1 2 4.9 O=C(O)/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
CHEMBL92607 205462 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 330 6 1 2 4.9 O=C(O)/C(=C/c1cccc(OCc2ccccc2)c1)c1ccccc1 10.1021/jm970847e
22998396 100334 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL293232 100334 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
22998396 100334 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br 10.1016/S0960-894X(97)00367-3
CHEMBL293232 100334 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br 10.1016/S0960-894X(97)00367-3
10685758 201411 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 302 4 2 6 1.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1C 10.1016/S0960-894X(97)00367-3
CHEMBL64006 201411 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 302 4 2 6 1.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1C 10.1016/S0960-894X(97)00367-3
192311 106777 3 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 513 11 5 4 2.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31702 106777 3 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 513 11 5 4 2.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
10627805 16387 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 630 7 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(Br)cccc2Br)cc1 10.1021/jm990170q
CHEMBL123926 16387 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 630 7 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(Br)cccc2Br)cc1 10.1021/jm990170q
22467231 97826 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 515 6 1 7 4.5 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C#N)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL274758 97826 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 515 6 1 7 4.5 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C#N)ccc23)cc1 10.1016/s0960-894x(01)00660-6
52943235 17918 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 571 12 2 7 5.9 CCCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1269101 17918 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 571 12 2 7 5.9 CCCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
44332803 4624 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 335 3 0 5 3.6 COC(=O)C(c1ccc2c(c1)OCO2)c1cc(C)nc2ccccc12 10.1016/S0960-894X(96)00551-3
CHEMBL103497 4624 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 335 3 0 5 3.6 COC(=O)C(c1ccc2c(c1)OCO2)c1cc(C)nc2ccccc12 10.1016/S0960-894X(96)00551-3
22998414 201318 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 422 5 1 9 3.1 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1C 10.1016/S0960-894X(97)00367-3
CHEMBL63290 201318 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 422 5 1 9 3.1 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1C 10.1016/S0960-894X(97)00367-3
9984393 59742 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 527 11 4 5 2.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00144-I
CHEMBL173808 59742 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL 527 11 4 5 2.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00144-I
18617345 104712 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL311461 104712 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
10918216 201145 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 508 7 1 6 6.0 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OCc4ccccc4)cc32)cc1 10.1021/jm010382z
CHEMBL62450 201145 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 508 7 1 6 6.0 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OCc4ccccc4)cc32)cc1 10.1021/jm010382z
10576889 11117 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 6 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(C(=O)O)c2)c1Br 10.1021/jm9608366
CHEMBL1178864 11117 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 6 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(C(=O)O)c2)c1Br 10.1021/jm9608366
CHEMBL47008 11117 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 6 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(C(=O)O)c2)c1Br 10.1021/jm9608366
23445457 128489 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL367024 128489 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
23445304 130811 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 484 6 1 7 4.4 Cc1cc2c(cc1CCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL368780 130811 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 484 6 1 7 4.4 Cc1cc2c(cc1CCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL407771 210925 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CCCC[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
18995989 100076 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 583 9 1 9 6.6 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00232-6
CHEMBL29147 100076 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 583 9 1 9 6.6 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00232-6
10711546 203755 6 None - 1 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2ccccc2Br)c1C 10.1016/0960-894X(96)00441-6
CHEMBL80506 203755 6 None - 1 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2ccccc2Br)c1C 10.1016/0960-894X(96)00441-6
44279360 106095 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 498 13 5 4 2.9 CC(C)C[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31426 106095 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 498 13 5 4 2.9 CC(C)C[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
10602475 60036 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 537 9 3 6 4.6 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL174658 60036 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 537 9 3 6 4.6 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
44327585 161222 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 992 26 9 8 5.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL414082 161222 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 992 26 9 8 5.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL2304017 207718 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL None None None CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(C#N)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
44298324 194186 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 448 7 2 7 4.4 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL55876 194186 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 448 7 2 7 4.4 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CO)c1 10.1016/s0960-894x(00)00366-8
23445457 128489 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL367024 128489 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
44383537 58922 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor
ChEMBL 388 4 2 5 3.4 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
CHEMBL170335 58922 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor
ChEMBL 388 4 2 5 3.4 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
127036867 136844 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 614 11 3 8 5.7 CCCc1nc2c(C)cc(C(=O)NCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3753134 136844 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 614 11 3 8 5.7 CCCc1nc2c(C)cc(C(=O)NCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
9896468 170092 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 703 13 2 10 6.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCC(=O)Nc1ccccc1C(C)C 10.1016/j.bmcl.2016.06.014
CHEMBL4451582 170092 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
ChEMBL 703 13 2 10 6.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCC(=O)Nc1ccccc1C(C)C 10.1016/j.bmcl.2016.06.014
10646616 202061 3 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 436 5 1 6 3.3 COc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
CHEMBL6800 202061 3 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 436 5 1 6 3.3 COc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
10555208 12284 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 578 9 2 6 5.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL1185774 12284 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 578 9 2 6 5.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL432227 12284 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 578 9 2 6 5.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2C)cc1 10.1021/jm990171i
10740507 128509 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 414 7 1 4 4.9 CCc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL367032 128509 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 414 7 1 4 4.9 CCc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
10693110 97833 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 414 5 1 5 4.4 CCc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL274805 97833 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 414 5 1 5 4.4 CCc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
11733215 201437 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 459 6 1 6 4.6 COc1ccc(C2=C(C(N)=O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL64127 201437 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 459 6 1 6 4.6 COc1ccc(C2=C(C(N)=O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
44298409 193318 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 490 10 2 7 5.2 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54770 193318 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 490 10 2 7 5.2 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCO)c1 10.1016/s0960-894x(00)00366-8
44383771 59520 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 371 7 1 6 4.5 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccsc1 10.1021/jm990378b
CHEMBL172879 59520 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 371 7 1 6 4.5 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccsc1 10.1021/jm990378b
10717923 98227 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL277595 98227 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00133-9
10550094 201383 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 420 4 1 5 3.6 Cc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
CHEMBL6382 201383 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 420 4 1 5 3.6 Cc1nc(Br)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
10740138 202382 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 406 4 1 5 3.3 CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Br)nc3)cccc12 10.1021/jm9604585
CHEMBL7019 202382 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 406 4 1 5 3.3 CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Br)nc3)cccc12 10.1021/jm9604585
44327890 140868 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 985 26 9 8 5.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL384052 140868 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL 985 26 9 8 5.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44298304 101072 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 503 10 2 7 4.7 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(N)=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL298395 101072 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 503 10 2 7 4.7 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(N)=O)c1 10.1016/s0960-894x(00)00366-8
10496523 201581 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 328 4 1 5 2.5 CN(C)c1cccc2c(S(=O)(=O)Nc3ncccn3)cccc12 10.1021/jm9604585
CHEMBL6468 201581 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 328 4 1 5 2.5 CN(C)c1cccc2c(S(=O)(=O)Nc3ncccn3)cccc12 10.1021/jm9604585
17869231 14442 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 548 11 1 9 5.5 COc1cc(C/C(C(=O)c2ccc(OC(C)C)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1205061 14442 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 548 11 1 9 5.5 COc1cc(C/C(C(=O)c2ccc(OC(C)C)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL48315 14442 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 548 11 1 9 5.5 COc1cc(C/C(C(=O)c2ccc(OC(C)C)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
9853077 59300 0 None - 2 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 696 13 2 12 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL172030 59300 0 None - 2 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 696 13 2 12 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL1791008 207161 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC[C@@H](C)[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O 10.1021/jm00021a021
44327238 106910 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 8 1 8 3.1 CCCc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL318017 106910 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to the endothelin A receptor of rat aorta membranes
ChEMBL 497 8 1 8 3.1 CCCc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44277036 169639 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 492 10 1 7 4.5 COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCCCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL444545 169639 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 492 10 1 7 4.5 COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCCCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
44294712 14608 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 566 11 1 9 5.6 COc1cc(C/C(C(=O)c2ccc(OC(C)C)c(F)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1206722 14608 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 566 11 1 9 5.6 COc1cc(C/C(C(=O)c2ccc(OC(C)C)c(F)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL300201 14608 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 566 11 1 9 5.6 COc1cc(C/C(C(=O)c2ccc(OC(C)C)c(F)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
11071689 9355 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 549 11 1 8 5.8 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccccc2)c1 10.1021/jm0102304
CHEMBL111876 9355 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 549 11 1 8 5.8 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccccc2)c1 10.1021/jm0102304
23445468 11113 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 459 5 3 9 2.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(O)nn2)c1Br 10.1021/jm9608366
CHEMBL1178818 11113 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 459 5 3 9 2.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(O)nn2)c1Br 10.1021/jm9608366
CHEMBL44615 11113 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 459 5 3 9 2.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(O)nn2)c1Br 10.1021/jm9608366
CHEMBL263295 208810 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
44279677 101743 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 478 2 2 3 4.0 O=C1c2cc(Br)ccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL30297 101743 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 478 2 2 3 4.0 O=C1c2cc(Br)ccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL147908 207029 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
23445412 101779 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 426 5 1 7 4.3 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00367-3
CHEMBL303203 101779 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 426 5 1 7 4.3 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00367-3
44385942 61032 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O 10.1021/jm950592+
CHEMBL176913 61032 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O 10.1021/jm950592+
10449431 99559 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 332 4 1 5 3.3 COc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00029a001
CHEMBL28692 99559 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 332 4 1 5 3.3 COc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00029a001
44276828 96311 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 324 5 3 6 1.0 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2)c1C 10.1021/jm00008a013
CHEMBL26470 96311 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 324 5 3 6 1.0 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2)c1C 10.1021/jm00008a013
10449431 99559 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 332 4 1 5 3.3 COc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL28692 99559 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 332 4 1 5 3.3 COc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL436884 211932 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
44383537 58922 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Tested for binding affinity towards rabbit Endothelin A receptorTested for binding affinity towards rabbit Endothelin A receptor
ChEMBL 388 4 2 5 3.4 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
CHEMBL170335 58922 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Tested for binding affinity towards rabbit Endothelin A receptorTested for binding affinity towards rabbit Endothelin A receptor
ChEMBL 388 4 2 5 3.4 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
6450144 122033 7 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonist activity at endothelin A receptor in Wistar rat thoracic aorta strips assessed as inhibition of ET1-induced vasoconstriction preincubated for 5 mins followed by ET1 additionAntagonist activity at endothelin A receptor in Wistar rat thoracic aorta strips assessed as inhibition of ET1-induced vasoconstriction preincubated for 5 mins followed by ET1 addition
ChEMBL 632 5 3 6 8.1 CC1(C)CC[C@]2(C(=O)O)CC[C@]3(COC(=O)/C=C/c4ccc(O)c(O)c4)C(=CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]2C1 10.1016/j.bmc.2015.06.055
CHEMBL3601500 122033 7 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Antagonist activity at endothelin A receptor in Wistar rat thoracic aorta strips assessed as inhibition of ET1-induced vasoconstriction preincubated for 5 mins followed by ET1 additionAntagonist activity at endothelin A receptor in Wistar rat thoracic aorta strips assessed as inhibition of ET1-induced vasoconstriction preincubated for 5 mins followed by ET1 addition
ChEMBL 632 5 3 6 8.1 CC1(C)CC[C@]2(C(=O)O)CC[C@]3(COC(=O)/C=C/c4ccc(O)c(O)c4)C(=CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]2C1 10.1016/j.bmc.2015.06.055
11728313 162712 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 368 6 1 5 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL418667 162712 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 368 6 1 5 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL2304008 207709 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
19363918 14452 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 474 7 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc3c(c2)OCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205106 14452 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 474 7 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc3c(c2)OCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL52535 14452 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 474 7 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc3c(c2)OCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44293927 101535 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 507 9 1 8 4.4 CCOc1ccc2c(c1)[C@@H](c1cc(OC)c(OC)c(OC)c1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL301723 101535 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 507 9 1 8 4.4 CCOc1ccc2c(c1)[C@@H](c1cc(OC)c(OC)c(OC)c1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
135884434 130030 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 628 10 2 12 5.2 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368117 130030 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 628 10 2 12 5.2 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
44386535 130830 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccc(F)c2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368853 130830 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccc(F)c2)nc1C(=O)O 10.1021/jm950592+
10403526 101402 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3cc(N)ccc3c2)c1C 10.1021/jm00008a013
CHEMBL30075 101402 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3cc(N)ccc3c2)c1C 10.1021/jm00008a013
10815902 165647 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 523 10 5 5 4.6 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL426589 165647 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 523 10 5 5 4.6 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
44332578 4235 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 413 3 0 5 5.6 CC(C)(C)OC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
CHEMBL100874 4235 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 413 3 0 5 5.6 CC(C)(C)OC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
CHEMBL431874 211870 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
44279251 99586 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 486 12 5 4 2.8 CC(C)C[C@H](NC(=O)CC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL287141 99586 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 486 12 5 4 2.8 CC(C)C[C@H](NC(=O)CC(C)(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
10265127 96375 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL26522 96375 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL3301647 209573 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10880982 102280 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 296 2 1 4 3.0 O=C(O)C1=Cc2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm031041j
CHEMBL305149 102280 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 296 2 1 4 3.0 O=C(O)C1=Cc2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm031041j
10880982 102280 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 296 2 1 4 3.0 O=C(O)C1=Cc2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
CHEMBL305149 102280 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 296 2 1 4 3.0 O=C(O)C1=Cc2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
CHEMBL385492 210595 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
10737416 59397 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 363 7 1 5 4.2 Cc1ccccc1C(Oc1cc(OCc2ccoc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL172412 59397 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 363 7 1 5 4.2 Cc1ccccc1C(Oc1cc(OCc2ccoc2)ccc1C#N)C(=O)O 10.1021/jm990378b
44293526 100874 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 563 11 2 8 4.9 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(C)(C)C(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL296974 100874 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 563 11 2 8 4.9 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(C)(C)C(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10336018 101625 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 318 3 2 5 3.0 Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C 10.1021/jm00004a012
CHEMBL30228 101625 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 318 3 2 5 3.0 Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C 10.1021/jm00004a012
22998438 201381 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 456 5 1 7 4.1 Cc1ccccc1OC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(97)00367-3
CHEMBL63805 201381 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 456 5 1 7 4.1 Cc1ccccc1OC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(97)00367-3
10602451 61409 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 536 11 3 6 5.1 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)CC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL177179 61409 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 536 11 3 6 5.1 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)CC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
1011 3288 24 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 609 12 3 10 4.8 OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O 10.1016/j.bmcl.2016.06.014
5312146 3288 24 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 609 12 3 10 4.8 OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O 10.1016/j.bmcl.2016.06.014
CHEMBL1628620 3288 24 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 609 12 3 10 4.8 OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O 10.1016/j.bmcl.2016.06.014
10531851 59425 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 614 11 3 7 5.3 CC(C)C[C@H](NC(=O)N1CCCCCC1)c1nc(C(=O)N[C@H](Cc2ccccn2)C(=O)O)c(Cc2cn(C)c3ccccc23)o1 10.1021/jm950591h
CHEMBL172506 59425 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 614 11 3 7 5.3 CC(C)C[C@H](NC(=O)N1CCCCCC1)c1nc(C(=O)N[C@H](Cc2ccccn2)C(=O)O)c(Cc2cn(C)c3ccccc23)o1 10.1021/jm950591h
10529715 205411 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)CC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9228 205411 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)CC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10694547 205336 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 443 10 1 7 2.9 COCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9183 205336 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 443 10 1 7 2.9 COCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10836835 96641 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 440 7 2 5 3.8 CCCCNC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267483 96641 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 440 7 2 5 3.8 CCCCNC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10599453 205531 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 445 9 1 6 5.2 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N 10.1021/jm9707131
CHEMBL93097 205531 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 445 9 1 6 5.2 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N 10.1021/jm9707131
5340 168154 104 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 255 3 2 5 1.5 Nc1ccc(S(=O)(=O)Nc2nccs2)cc1 10.1021/jm00008a013
CHEMBL437 168154 104 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 255 3 2 5 1.5 Nc1ccc(S(=O)(=O)Nc2nccs2)cc1 10.1021/jm00008a013
5340 168154 104 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 255 3 2 5 1.5 Nc1ccc(S(=O)(=O)Nc2nccs2)cc1 10.1021/jm030480f
CHEMBL437 168154 104 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 255 3 2 5 1.5 Nc1ccc(S(=O)(=O)Nc2nccs2)cc1 10.1021/jm030480f
18995991 99823 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 537 8 1 10 5.0 COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC 10.1016/0960-894X(96)00232-6
CHEMBL28920 99823 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 537 8 1 10 5.0 COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC 10.1016/0960-894X(96)00232-6
10649585 109272 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 518 14 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC1OCCO1 10.1021/jm980217s
CHEMBL323175 109272 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 518 14 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC1OCCO1 10.1021/jm980217s
22574723 15747 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 549 11 2 7 5.2 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CC)c1 10.1039/C4MD00499J
CHEMBL12233 15747 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 549 11 2 7 5.2 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CC)c1 10.1039/C4MD00499J
20747575 97959 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 579 12 2 8 5.0 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1 10.1039/C4MD00499J
CHEMBL275545 97959 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 579 12 2 8 5.0 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1 10.1039/C4MD00499J
71455064 81270 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 694 14 1 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)N(C)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163721 81270 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 694 14 1 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)N(C)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
10693270 59739 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL172144 59739 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL173792 59739 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
10601191 112294 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 492 11 3 6 5.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc(C(=O)O)[nH]n1 10.1021/jm9707131
CHEMBL330679 112294 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 492 11 3 6 5.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc(C(=O)O)[nH]n1 10.1021/jm9707131
22010244 205064 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
CHEMBL90320 205064 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
10740214 205563 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 408 9 1 6 4.9 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cnsc2)ccc1C#N 10.1021/jm9707131
CHEMBL93331 205563 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 408 9 1 6 4.9 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cnsc2)ccc1C#N 10.1021/jm9707131
10190108 130163 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 681 12 2 12 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
CHEMBL368386 130163 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 681 12 2 12 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
44333887 108125 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 446 7 2 6 3.9 CCNCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL320631 108125 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 446 7 2 6 3.9 CCNCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
44311528 202432 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 633 12 2 10 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70487 202432 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 633 12 2 10 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44311284 202534 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 635 12 2 10 6.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL71070 202534 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 635 12 2 10 6.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
137642741 157682 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 553 9 2 9 4.2 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4088349 157682 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 553 9 2 9 4.2 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
10224228 179022 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1ccc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
CHEMBL47424 179022 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1ccc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
101039204 158369 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 610 7 6 6 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2017.04.049
CHEMBL4095638 158369 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 610 7 6 6 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2017.04.049
11742628 97770 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL274383 97770 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
9845967 10974 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL10801 10974 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL1178000 10974 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL51530 10974 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/S0960-894X(97)00002-4
52944276 18230 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 559 11 3 8 4.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCCO)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271807 18230 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 559 11 3 8 4.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCCO)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
9845967 10974 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL10801 10974 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1178000 10974 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL51530 10974 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(98)00301-1
104865 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
3494 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
392 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
CHEMBL957 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
DB00559 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
10790686 5164 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 474 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCCO3)cc1 10.1021/jm9606507
CHEMBL10635 5164 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 474 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCCO3)cc1 10.1021/jm9606507
44458999 167654 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 525 6 2 7 3.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL433619 167654 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 525 6 2 7 3.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
104865 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(01)00682-5
3494 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(01)00682-5
392 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(01)00682-5
CHEMBL957 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(01)00682-5
DB00559 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(01)00682-5
104865 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
3494 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
392 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
CHEMBL957 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
DB00559 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
44385593 128939 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 530 10 5 5 4.5 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL367208 128939 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 530 10 5 5 4.5 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O 10.1021/jm950592+
10553316 96616 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 11 1 6 4.3 CCCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267279 96616 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 11 1 6 4.3 CCCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44439108 166550 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 1267 53 3 22 5.7 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL429019 166550 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 1267 53 3 22 5.7 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
71451527 81254 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 641 15 1 12 4.8 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C2CC2)cn1 10.1021/jm3009103
CHEMBL2163706 81254 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 641 15 1 12 4.8 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C2CC2)cn1 10.1021/jm3009103
71462246 81265 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 604 12 2 12 2.6 CNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163717 81265 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 604 12 2 12 2.6 CNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
10667000 96711 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 372 5 1 6 2.8 COc1nc(C)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
CHEMBL268174 96711 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 372 5 1 6 2.8 COc1nc(C)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12 10.1021/jm9604585
10765171 7798 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)c(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10901 7798 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)c(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
11798228 98031 2 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 461 6 1 8 3.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc([N+](=O)[O-])c2)cc1 10.1021/jm9606507
CHEMBL276018 98031 2 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 461 6 1 8 3.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc([N+](=O)[O-])c2)cc1 10.1021/jm9606507
9863916 59950 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 365 7 1 5 4.4 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1 10.1021/jm990378b
CHEMBL174229 59950 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 365 7 1 5 4.4 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1ccccc1 10.1021/jm990378b
44320432 204522 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 442 6 1 7 3.6 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1OCCO1 10.1016/s0960-894x(00)00513-8
CHEMBL86821 204522 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 442 6 1 7 3.6 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1OCCO1 10.1016/s0960-894x(00)00513-8
9980487 5183 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 436 6 1 5 4.8 COc1ccc(CC2=C(c3ccc(Cl)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL10648 5183 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 436 6 1 5 4.8 COc1ccc(CC2=C(c3ccc(Cl)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
10692351 9289 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 400 5 0 5 4.7 COc1ccc(C2OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL11152 9289 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 400 5 0 5 4.7 COc1ccc(C2OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10894688 201803 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 402 4 1 5 4.4 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)c1 10.1021/jm010382z
CHEMBL66246 201803 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 402 4 1 5 4.4 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)c1 10.1021/jm010382z
10835638 111055 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 414 6 1 3 5.7 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1Br)c1ccccc1 10.1021/jm970847e
CHEMBL328057 111055 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 414 6 1 3 5.7 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1Br)c1ccccc1 10.1021/jm970847e
10739089 111125 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 389 8 1 4 5.6 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/CCC(=O)O)c1ccccc1 10.1021/jm970847e
CHEMBL328464 111125 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 389 8 1 4 5.6 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/CCC(=O)O)c1ccccc1 10.1021/jm970847e
CHEMBL1793933 207178 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H]([C@@H](C)CC)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm970161m
19010490 53238 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 648 13 1 9 6.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)C(C)C)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL16018 53238 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 648 13 1 9 6.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)C(C)C)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL85341 214101 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
127029203 136889 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 628 12 3 8 5.8 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3753458 136889 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 628 12 3 8 5.8 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
18617322 203739 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80438 203739 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1Br 10.1016/0960-894X(96)00441-6
44371531 164302 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 467 6 1 5 6.3 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C(C)C)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL422002 164302 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 467 6 1 5 6.3 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C(C)C)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL438768 212038 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)Binding affinity against Endothelin A receptor in rabbit renal artery vascular smooth muscle membrane (ET-A)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL2370247 208058 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm00015a003
127026040 136941 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 591 11 3 8 4.6 CCCc1nc2c(C)cc(C(=O)NCCN3CCCC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3753888 136941 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 591 11 3 8 4.6 CCCc1nc2c(C)cc(C(=O)NCCN3CCCC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
44298597 100357 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 343 5 2 5 3.0 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Cc1ccccc1 10.1016/s0960-894x(00)00366-8
CHEMBL293376 100357 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 343 5 2 5 3.0 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1Cc1ccccc1 10.1016/s0960-894x(00)00366-8
18617333 105035 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 424 4 1 5 3.3 COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL312187 105035 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 424 4 1 5 3.3 COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
44459247 87581 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 575 8 1 7 4.9 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)N(C)C)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL23444 87581 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
ChEMBL 575 8 1 7 4.9 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)N(C)C)cc21 10.1016/s0960-894x(01)00660-6
44385127 61024 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Tested for the inhibitory activity of cloned human ETA receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for the inhibitory activity of cloned human ETA receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 482 5 1 7 4.8 Cc1cc2c(cc1/C=C/c1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL176854 61024 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Tested for the inhibitory activity of cloned human ETA receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for the inhibitory activity of cloned human ETA receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 482 5 1 7 4.8 Cc1cc2c(cc1/C=C/c1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
44316994 203232 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 266 3 1 4 2.4 Cc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
CHEMBL76420 203232 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 266 3 1 4 2.4 Cc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
127036866 136732 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 614 11 3 8 5.7 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3752117 136732 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 614 11 3 8 5.7 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
18184256 128948 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 662 13 2 13 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL367275 128948 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 662 13 2 13 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
71458720 81258 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 665 13 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163710 81258 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 665 13 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
44384652 60941 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 582 8 1 9 5.2 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2COC2CCOCC2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL176675 60941 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 582 8 1 9 5.2 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2COC2CCOCC2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL353605 209970 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL None None None CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NC(C)(C)C(=O)O 10.1016/0960-894X(95)00144-I
10672060 9155 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 470 10 1 6 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)c(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL110794 9155 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 470 10 1 6 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)c(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10626501 127988 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 550 10 5 4 5.1 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)[nH]1 10.1021/jm950591h
CHEMBL366745 127988 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 550 10 5 4 5.1 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)[nH]1 10.1021/jm950591h
10721386 60041 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 11 5 5 4.8 CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)[nH]2)c2ccccc21 10.1021/jm950592+
CHEMBL174686 60041 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 550 11 5 5 4.8 CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)[nH]2)c2ccccc21 10.1021/jm950592+
10603414 60724 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 585 10 4 5 5.9 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)o1 10.1021/jm950591h
CHEMBL176420 60724 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 585 10 4 5 5.9 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(-c2ccccc2)o1 10.1021/jm950591h
71455061 81247 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 511 11 1 12 2.4 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
CHEMBL2163699 81247 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 511 11 1 12 2.4 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
11826173 201123 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1 10.1021/jm031041j
CHEMBL62363 201123 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1 10.1021/jm031041j
11826173 201123 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1 10.1021/jm010382z
CHEMBL62363 201123 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1 10.1021/jm010382z
44385490 131273 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 532 10 4 7 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccn2)nc1C(=O)O 10.1021/jm950592+
CHEMBL369386 131273 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 532 10 4 7 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccn2)nc1C(=O)O 10.1021/jm950592+
10833686 201705 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 380 4 1 7 2.4 COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(97)00367-3
CHEMBL65531 201705 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 380 4 1 7 2.4 COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(97)00367-3
44266621 98097 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 387 4 1 5 4.7 COc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccccc3)c2c1 10.1016/0960-894X(96)00170-9
CHEMBL276615 98097 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 387 4 1 5 4.7 COc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccccc3)c2c1 10.1016/0960-894X(96)00170-9
10722389 12004 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 606 10 2 6 6.0 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL1184099 12004 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 606 10 2 6 6.0 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL332424 12004 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 606 10 2 6 6.0 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1C 10.1021/jm990171i
10621704 59663 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 414 7 1 6 4.8 Cc1ccccc1C(Oc1cc(OCc2ccc3ocnc3c2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL173444 59663 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 414 7 1 6 4.8 Cc1ccccc1C(Oc1cc(OCc2ccc3ocnc3c2)ccc1C#N)C(=O)O 10.1021/jm990378b
44270498 98454 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 702 13 1 10 7.2 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL279419 98454 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 702 13 1 10 7.2 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
10577941 61014 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 522 10 6 4 4.3 Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL176794 61014 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 522 10 6 4 4.3 Cc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL2370070 208024 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
44276596 106346 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 458 8 1 6 4.2 COc1ccc(Cc2[nH]n(Cc3cccc(OC)c3)c(=O)c2Cc2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(00)00232-8
CHEMBL3144728 106346 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 458 8 1 6 4.2 COc1ccc(Cc2[nH]n(Cc3cccc(OC)c3)c(=O)c2Cc2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(00)00232-8
10477792 173222 1 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cellsDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells
ChEMBL 430 8 0 7 3.7 COC[C@@H]1Cc2cc3c(c(OC)c2[C@H](c2ccc(OC)c(OC)c2)[C@H]1COC)OCO3 10.1021/np50124a006
CHEMBL453822 173222 1 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cellsDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells
ChEMBL 430 8 0 7 3.7 COC[C@@H]1Cc2cc3c(c(OC)c2[C@H](c2ccc(OC)c(OC)c2)[C@H]1COC)OCO3 10.1021/np50124a006
10305181 60113 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 666 11 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)NC1CCCCC1 10.1016/s0960-894x(02)01084-3
CHEMBL175278 60113 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 666 11 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)NC1CCCCC1 10.1016/s0960-894x(02)01084-3
10578300 129455 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 537 10 4 6 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)OC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL367645 129455 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 537 10 4 6 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)OC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
44279126 100247 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 466 3 2 3 5.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3Cl)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL29265 100247 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 466 3 2 3 5.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3Cl)cc21 10.1016/0960-894X(95)00230-Q
44284490 99749 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL 616 13 3 5 3.9 CNC(=O)[C@H](Cc1ccccn1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)N(C)C(=O)[C@@H](CC(=O)N1CCCCCC1)CC(C)C 10.1021/jm00087a001
CHEMBL288514 99749 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL 616 13 3 5 3.9 CNC(=O)[C@H](Cc1ccccn1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)N(C)C(=O)[C@@H](CC(=O)N1CCCCCC1)CC(C)C 10.1021/jm00087a001
CHEMBL1206620 206855 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL None None None CC(C)C[C@@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)N(C)CC(=O)O 10.1021/jm00087a001
CHEMBL287980 206855 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranesCompound was evaluated for the binding affinity towards Endothelin A receptor in porcine aortic membranes
ChEMBL None None None CC(C)C[C@@H](NC(=O)N1CCCCCC1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccn1)C(=O)N(C)CC(=O)O 10.1021/jm00087a001
44332641 4657 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 384 4 0 4 5.2 COC(=O)C(Cc1c2ccccc2cc2ccccc12)c1ccc2c(c1)OCO2 10.1016/S0960-894X(96)00551-3
CHEMBL103731 4657 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 384 4 0 4 5.2 COC(=O)C(Cc1c2ccccc2cc2ccccc12)c1ccc2c(c1)OCO2 10.1016/S0960-894X(96)00551-3
10598270 96483 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 421 6 1 5 4.1 CCCC#CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL266144 96483 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 421 6 1 5 4.1 CCCC#CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10744041 96840 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 502 8 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)Cc2ccccc2)cc1 10.1021/jm9505369
CHEMBL269108 96840 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 502 8 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)Cc2ccccc2)cc1 10.1021/jm9505369
11101703 167344 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 412 7 1 5 5.3 CCCC[C@@H]1c2cc(OC(C)C)ccc2O[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1021/jm031041j
CHEMBL431372 167344 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 412 7 1 5 5.3 CCCC[C@@H]1c2cc(OC(C)C)ccc2O[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1021/jm031041j
11101703 167344 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 412 7 1 5 5.3 CCCC[C@@H]1c2cc(OC(C)C)ccc2O[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1021/jm010382z
CHEMBL431372 167344 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 412 7 1 5 5.3 CCCC[C@@H]1c2cc(OC(C)C)ccc2O[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1021/jm010382z
44293736 187558 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 463 7 2 7 4.1 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL49850 187558 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 463 7 2 7 4.1 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
9874557 129203 0 None - 2 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 667 15 2 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL367443 129203 0 None - 2 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 667 15 2 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
10516176 203479 3 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccccc2F)c1C 10.1016/0960-894X(96)00441-6
CHEMBL78499 203479 3 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccccc2F)c1C 10.1016/0960-894X(96)00441-6
44298278 192991 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 462 8 2 7 4.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL53168 192991 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 462 8 2 7 4.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCO)c1 10.1016/s0960-894x(00)00366-8
10626522 129748 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 551 11 4 5 5.2 CCCc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
CHEMBL367989 129748 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 551 11 4 5 5.2 CCCc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
9961347 11842 1 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL1182945 11842 1 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL273642 11842 1 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
137638953 156293 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 579 10 2 9 4.6 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4071505 156293 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 579 10 2 9 4.6 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
11728411 201183 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 372 3 1 4 4.4 O=C(O)C1=C(c2ccccc2)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm031041j
CHEMBL62659 201183 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 372 3 1 4 4.4 O=C(O)C1=C(c2ccccc2)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm031041j
5344 172891 98 None - 1 Human 6.1 pIC50 = 6.1 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00029a001
CHEMBL453 172891 98 None - 1 Human 6.1 pIC50 = 6.1 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00029a001
5344 172891 98 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00008a013
CHEMBL453 172891 98 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00008a013
11728411 201183 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 372 3 1 4 4.4 O=C(O)C1=C(c2ccccc2)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
CHEMBL62659 201183 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 372 3 1 4 4.4 O=C(O)C1=C(c2ccccc2)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
5344 172891 98 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm030480f
CHEMBL453 172891 98 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm030480f
10334781 95551 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1C 10.1021/jm00008a013
CHEMBL25970 95551 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1C 10.1021/jm00008a013
9983872 101240 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 511 9 2 5 6.9 Cc1noc(NS(=O)(=O)c2cccc3c(NCCC(c4ccccc4)c4ccccc4)cccc23)c1C 10.1021/jm00008a013
CHEMBL29954 101240 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 511 9 2 5 6.9 Cc1noc(NS(=O)(=O)c2cccc3c(NCCC(c4ccccc4)c4ccccc4)cccc23)c1C 10.1021/jm00008a013
10336018 101625 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 318 3 2 5 3.0 Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C 10.1021/jm00008a013
CHEMBL30228 101625 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 318 3 2 5 3.0 Cc1noc(NS(=O)(=O)c2cccc3c(O)cccc23)c1C 10.1021/jm00008a013
CHEMBL413825 211329 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(95)00084-7
10840422 130831 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 550 11 5 4 4.9 CCCc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
CHEMBL368854 130831 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 550 11 5 4 4.9 CCCc1[nH]c([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1C(=O)O 10.1021/jm950591h
10624915 204500 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 490 6 2 6 4.5 COc1ccc(NC(=O)N2C[C@@H](c3ccc4c(c3)OCO4)[C@H](C(=O)O)[C@H]2c2ccc(OC)cc2)cc1 10.1021/jm9505369
CHEMBL8671 204500 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 490 6 2 6 4.5 COc1ccc(NC(=O)N2C[C@@H](c3ccc4c(c3)OCO4)[C@H](C(=O)O)[C@H]2c2ccc(OC)cc2)cc1 10.1021/jm9505369
18617288 203426 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 316 3 1 4 2.5 Cc1noc(NS(=O)(=O)c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78080 203426 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 316 3 1 4 2.5 Cc1noc(NS(=O)(=O)c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
44320444 204707 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 481 7 2 8 4.0 O=C(O)c1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)on1 10.1016/s0960-894x(00)00513-8
CHEMBL88019 204707 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 481 7 2 8 4.0 O=C(O)c1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)on1 10.1016/s0960-894x(00)00513-8
44384651 127964 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 498 6 2 8 4.0 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2CO)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL366680 127964 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 498 6 2 8 4.0 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2CO)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
44332624 4102 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 356 3 1 4 3.7 NC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
CHEMBL100120 4102 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 356 3 1 4 3.7 NC(=O)C(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
10743872 96746 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 13 1 6 5.2 CCCCN(CCCC)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL268432 96746 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 496 13 1 6 5.2 CCCCN(CCCC)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
3847484 202029 2 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 360 4 1 3 4.4 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)cc3)cccc12 10.1021/jm9604585
CHEMBL6778 202029 2 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
ChEMBL 360 4 1 3 4.4 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)cc3)cccc12 10.1021/jm9604585
10145418 81246 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 601 14 1 12 4.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1016/j.bmcl.2016.06.014
CHEMBL2163698 81246 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
ChEMBL 601 14 1 12 4.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1016/j.bmcl.2016.06.014
CHEMBL354082 209972 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL None None None CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)N[C@H](CO)C(=O)O 10.1016/0960-894X(95)00144-I
CHEMBL354152 209973 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
ChEMBL None None None CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)O 10.1016/0960-894X(95)00144-I
10646372 5364 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 5 2 7 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(O)cc2)cc1 10.1021/jm9606507
CHEMBL10744 5364 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 432 5 2 7 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(O)cc2)cc1 10.1021/jm9606507
10950392 201256 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 448 5 1 5 5.4 CC(C)Oc1ccc2c(c1)C(c1ccc(F)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL62966 201256 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 448 5 1 5 5.4 CC(C)Oc1ccc2c(c1)C(c1ccc(F)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
11113542 201511 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 476 8 1 6 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3OC)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL64398 201511 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 476 8 1 6 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3OC)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
44314575 103084 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 601 13 5 5 4.2 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL308584 103084 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 601 13 5 5 4.2 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
22010244 205064 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm970847e
CHEMBL90320 205064 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm970847e
44439106 153061 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 1005 37 2 17 5.8 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL398070 153061 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
ChEMBL 1005 37 2 17 5.8 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
10145418 81246 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 601 14 1 12 4.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
CHEMBL2163698 81246 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 601 14 1 12 4.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
44304492 96099 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(95)00349-X
CHEMBL262993 96099 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(95)00349-X
CHEMBL265614 208901 13 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(95)00349-X
104865 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
3494 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
392 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
CHEMBL957 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
DB00559 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
10230835 109731 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 546 12 1 7 4.0 CCCS(=O)(=O)N(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)CC(C)C 10.1021/jm970101g
CHEMBL323789 109731 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 546 12 1 7 4.0 CCCS(=O)(=O)N(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)CC(C)C 10.1021/jm970101g
10383884 203488 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 359 4 2 5 2.9 CNc1ccc(C)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78563 203488 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 359 4 2 5 2.9 CNc1ccc(C)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
44314660 103873 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 633 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1C)C(=O)O 10.1021/jm9600914
CHEMBL310111 103873 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 633 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1C)C(=O)O 10.1021/jm9600914
CHEMBL2304011 207712 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
10766385 97963 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 460 6 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
CHEMBL275559 97963 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 460 6 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
44333889 4999 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 463 7 1 6 5.3 CCCSc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL105494 4999 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
ChEMBL 463 7 1 6 5.3 CCCSc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
10647373 96510 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 8 2 6 3.0 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(C)C)cc1 10.1021/jm9505369
CHEMBL266337 96510 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 454 8 2 6 3.0 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(C)C)cc1 10.1021/jm9505369
10817057 9587 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 580 11 1 7 4.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(C)cc1 10.1021/jm970101g
CHEMBL113087 9587 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
ChEMBL 580 11 1 7 4.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(C)cc1 10.1021/jm970101g
9840391 104047 6 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL310427 104047 6 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
9803428 101721 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 442 5 1 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Cl 10.1016/S0960-894X(97)00367-3
CHEMBL302872 101721 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 442 5 1 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Cl 10.1016/S0960-894X(97)00367-3
CHEMBL336033 209818 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory effect against Human Endothelin A receptorInhibitory effect against Human Endothelin A receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
104865 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1039/C5MD00169B
3494 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1039/C5MD00169B
392 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1039/C5MD00169B
CHEMBL957 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1039/C5MD00169B
DB00559 697 94 None 1 4 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1039/C5MD00169B
10504689 9335 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 474 6 1 8 3.6 COC(=O)c1cccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)c1 10.1021/jm9606507
CHEMBL11176 9335 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 474 6 1 8 3.6 COC(=O)c1cccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)c1 10.1021/jm9606507
10840410 202353 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 550 10 2 10 3.3 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCC(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL70017 202353 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
ChEMBL 550 10 2 10 3.3 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCC(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL2304006 207707 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
ChEMBL None None None O=C(O)C[C@H]1NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm9600914
CHEMBL411171 211110 0 None - 1 Pig 8.1 pIC50 = 8.1 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00077a013
22467266 84908 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261360 84908 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
10626362 11331 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 544 8 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL1180351 11331 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 544 8 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL123316 11331 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
ChEMBL 544 8 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
22467230 84917 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 536 8 1 8 4.0 COCc1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1007/s00044-004-0021-y
CHEMBL2261601 84917 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 536 8 1 8 4.0 COCc1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1007/s00044-004-0021-y
11038925 9750 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 550 11 1 9 5.2 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccccn2)c1 10.1021/jm0102304
CHEMBL114105 9750 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 550 11 1 9 5.2 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccccn2)c1 10.1021/jm0102304
9826741 100277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00367-3
CHEMBL292802 100277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00367-3
9826741 100277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
CHEMBL292802 100277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
10068813 97565 4 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 387 8 2 5 4.8 CCCCCNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL27299 97565 4 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 387 8 2 5 4.8 CCCCCNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
10406285 111148 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 361 6 1 4 4.8 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccccc1 10.1021/jm970847e
CHEMBL328600 111148 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 361 6 1 4 4.8 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/C(=O)O)c1ccccc1 10.1021/jm970847e
104865 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
3494 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
392 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
CHEMBL957 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
DB00559 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
18184229 59281 0 None - 2 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 605 15 2 10 4.2 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL171950 59281 0 None - 2 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 605 15 2 10 4.2 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
44266552 4431 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10218 4431 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
44266567 97768 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 461 5 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00170-9
CHEMBL274368 97768 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 461 5 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00170-9
104865 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
3494 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
392 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
CHEMBL957 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
DB00559 697 94 None 1 4 Human 7.1 pIC50 = 7.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
19432672 202511 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 606 11 3 9 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCNC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70924 202511 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 606 11 3 9 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCNC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
10623877 8388 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 461 6 1 8 3.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm9606507
CHEMBL10940 8388 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 461 6 1 8 3.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm9606507
11015023 102234 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 406 3 1 4 5.1 O=C(O)C1=C(c2ccc(Cl)cc2)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
CHEMBL304875 102234 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 406 3 1 4 5.1 O=C(O)C1=C(c2ccc(Cl)cc2)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
14041110 99539 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 322 2 2 3 2.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccccc21 10.1016/0960-894X(95)00230-Q
CHEMBL286808 99539 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human ETA receptorBinding affinity towards cloned human ETA receptor
ChEMBL 322 2 2 3 2.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccccc21 10.1016/0960-894X(95)00230-Q
10497859 162862 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 347 6 1 4 4.7 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1 10.1021/jm970847e
CHEMBL419694 162862 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 347 6 1 4 4.7 N#Cc1ccc(OCc2ccsc2)cc1/C=C(/CO)c1ccccc1 10.1021/jm970847e
44298325 193994 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 446 7 1 6 5.5 CCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1 10.1016/s0960-894x(00)00366-8
CHEMBL55664 193994 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 446 7 1 6 5.5 CCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1 10.1016/s0960-894x(00)00366-8
19095644 169134 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 549 10 2 8 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4438132 169134 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
ChEMBL 549 10 2 8 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO 10.1016/j.bmcl.2016.06.014
5344 172891 98 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00004a012
CHEMBL453 172891 98 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1021/jm00004a012
44386621 60933 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL176653 60933 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 549 10 4 6 4.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
44266542 162248 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 521 7 1 7 6.1 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL417246 162248 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
ChEMBL 521 7 1 7 6.1 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
44368428 44309 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 521 9 2 5 5.5 O=C(O)C(Cc1ccc(O)cc1)N(Cc1ccccc1-c1ccccc1)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
CHEMBL152001 44309 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 521 9 2 5 5.5 O=C(O)C(Cc1ccc(O)cc1)N(Cc1ccccc1-c1ccccc1)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
CHEMBL330489 209576 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
CHEMBL86737 214103 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
CHEMBL330489 209576 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/S0960-894X(01)81215-4
10627378 60087 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 598 11 5 4 5.6 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)[nH]1 10.1021/jm950591h
CHEMBL175103 60087 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
ChEMBL 598 11 5 4 5.6 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)[nH]1 10.1021/jm950591h
18995996 98732 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 569 10 1 8 6.9 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OCc4ccccc4)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL281451 98732 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 569 10 1 8 6.9 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OCc4ccccc4)cc23)c1 10.1016/0960-894X(96)00232-6
44279366 99187 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 499 11 5 4 2.4 CC(C)C[C@H](NC(=O)N1CCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL284392 99187 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity determined against ETA receptor in porcine aortic smooth muscle membraneBinding affinity determined against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 499 11 5 4 2.4 CC(C)C[C@H](NC(=O)N1CCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
44384757 165584 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 482 5 1 7 4.8 Cc1cc2c(cc1/C=C/c1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL426218 165584 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 482 5 1 7 4.8 Cc1cc2c(cc1/C=C/c1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
11103152 162677 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)c(OC)c1)O2 10.1021/jm010382z
CHEMBL418473 162677 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)c(OC)c1)O2 10.1021/jm010382z
44314580 203417 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 608 13 5 5 4.5 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL78023 203417 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 608 13 5 5 4.5 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL441006 212117 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor
ChEMBL None None None CC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00084-7
23445388 204788 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2sccc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL88506 204788 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2sccc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
9917072 61759 0 None - 2 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 619 16 2 10 4.6 CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL177538 61759 0 None - 2 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 619 16 2 10 4.6 CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
23445408 111132 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 454 6 1 5 5.5 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CC(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL328517 111132 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 454 6 1 5 5.5 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CC(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
44270602 98389 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 688 13 1 10 7.0 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1cccs1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL278930 98389 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 688 13 1 10 7.0 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1cccs1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
1009 192 20 None - 1 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
5310991 192 20 None - 1 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
CHEMBL332794 192 20 None - 1 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
44383535 58953 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor
ChEMBL 280 4 1 5 1.5 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(OC)[C@]2(O)CC1 10.1016/s0960-894x(00)00136-0
CHEMBL170446 58953 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Tested for binding affinity towards human Endothelin A receptorTested for binding affinity towards human Endothelin A receptor
ChEMBL 280 4 1 5 1.5 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(OC)[C@]2(O)CC1 10.1016/s0960-894x(00)00136-0
10960638 100586 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 414 4 1 4 5.6 CC(C)c1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
CHEMBL294793 100586 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 414 4 1 4 5.6 CC(C)c1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
23445358 111062 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 412 4 1 5 4.6 Cc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
CHEMBL328089 111062 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 412 4 1 5 4.6 Cc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
10546830 100892 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 365 4 2 6 1.7 Cc1noc(NS(=O)(=O)c2ccsc2C(N)=O)c1Br 10.1021/jm9608366
CHEMBL297107 100892 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 365 4 2 6 1.7 Cc1noc(NS(=O)(=O)c2ccsc2C(N)=O)c1Br 10.1021/jm9608366
44386069 59408 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 704 13 2 11 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL172441 59408 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 704 13 2 11 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
18995999 98047 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 477 6 1 8 5.0 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)c1 10.1016/0960-894X(96)00232-6
CHEMBL27617 98047 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 477 6 1 8 5.0 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)c1 10.1016/0960-894X(96)00232-6
44384611 128119 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 644 10 2 12 5.8 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL366797 128119 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 644 10 2 12 5.8 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10405292 97114 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3cc(N(C)C)ccc23)c1C 10.1021/jm00008a013
CHEMBL27073 97114 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3cc(N(C)C)ccc23)c1C 10.1021/jm00008a013
44316526 203700 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 344 3 1 4 3.2 Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL80180 203700 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 344 3 1 4 3.2 Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
10674642 112858 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 574 10 3 7 4.7 CCc1cc(C(=O)O)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL331758 112858 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 574 10 3 7 4.7 CCc1cc(C(=O)O)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
10405292 97114 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3cc(N(C)C)ccc23)c1C 10.1021/jm00004a012
CHEMBL27073 97114 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3cc(N(C)C)ccc23)c1C 10.1021/jm00004a012
19010508 56036 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 501 9 1 7 5.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL16306 56036 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
ChEMBL 501 9 1 7 5.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
14973488 113295 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 295 4 1 5 2.2 Cc1noc(NS(=O)(=O)c2ccc(N(C)C)cc2)c1C 10.1021/jm00029a001
CHEMBL332471 113295 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 295 4 1 5 2.2 Cc1noc(NS(=O)(=O)c2ccc(N(C)C)cc2)c1C 10.1021/jm00029a001
14973488 113295 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 295 4 1 5 2.2 Cc1noc(NS(=O)(=O)c2ccc(N(C)C)cc2)c1C 10.1021/jm00004a012
CHEMBL332471 113295 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 295 4 1 5 2.2 Cc1noc(NS(=O)(=O)c2ccc(N(C)C)cc2)c1C 10.1021/jm00004a012
44293685 101297 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL300000 101297 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 521 10 2 8 3.9 CCOc1ccc2c(c1)[C@@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10576377 11887 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL1183291 11887 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL288967 11887 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
44384715 60028 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 559 9 1 9 5.2 CC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL174607 60028 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 559 9 1 9 5.2 CC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
44265861 96747 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 481 11 1 6 5.1 CCCC(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL268433 96747 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 481 11 1 6 5.1 CCCC(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL433406 211882 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)NC)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
5344 172891 98 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL453 172891 98 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL308208 209227 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm00089a028
CHEMBL341751 209904 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm00021a021
10763577 59570 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 401 7 1 4 5.3 Cc1ccccc1C(Oc1cc(OCc2c(C)cccc2C)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL173054 59570 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 401 7 1 4 5.3 Cc1ccccc1C(Oc1cc(OCc2c(C)cccc2C)ccc1C#N)C(=O)O 10.1021/jm990378b
10916428 162133 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 402 4 1 5 4.4 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm031041j
CHEMBL417050 162133 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 402 4 1 5 4.4 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm031041j
15289331 99090 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 433 6 1 6 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3ccccc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL283648 99090 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 433 6 1 6 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3ccccc23)c1 10.1016/0960-894X(96)00232-6
10916428 162133 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 402 4 1 5 4.4 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
CHEMBL417050 162133 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 402 4 1 5 4.4 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
9810400 98142 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 710 14 2 12 5.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL276949 98142 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 710 14 2 12 5.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
10338501 101572 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00004a012
CHEMBL30199 101572 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00004a012
10275056 112004 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 440 6 1 5 5.2 CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL329890 112004 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
ChEMBL 440 6 1 5 5.2 CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
9998564 99009 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2cccc(S(=O)(=O)Nc3onc(C)c3C)c2c1 10.1021/jm00008a013
CHEMBL283175 99009 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2cccc(S(=O)(=O)Nc3onc(C)c3C)c2c1 10.1021/jm00008a013
9998564 99009 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2cccc(S(=O)(=O)Nc3onc(C)c3C)c2c1 10.1021/jm00004a012
CHEMBL283175 99009 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1ccc2cccc(S(=O)(=O)Nc3onc(C)c3C)c2c1 10.1021/jm00004a012
10602312 59336 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 531 11 5 5 4.5 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL172178 59336 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 531 11 5 5 4.5 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O 10.1021/jm950592+
10571971 167598 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 382 9 1 4 5.6 Cc1ccccc1C(CCC(=O)O)Oc1cccc(OCc2ccsc2)c1 10.1021/jm9707131
CHEMBL433209 167598 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
ChEMBL 382 9 1 4 5.6 Cc1ccccc1C(CCC(=O)O)Oc1cccc(OCc2ccsc2)c1 10.1021/jm9707131
137639474 156343 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 607 10 2 9 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4072165 156343 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 607 10 2 9 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10696788 175332 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory activity against human Endothelin A receptor using radioligand binding assay.In vitro inhibitory activity against human Endothelin A receptor using radioligand binding assay.
ChEMBL 501 5 2 9 3.9 Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL45872 175332 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory activity against human Endothelin A receptor using radioligand binding assay.In vitro inhibitory activity against human Endothelin A receptor using radioligand binding assay.
ChEMBL 501 5 2 9 3.9 Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
10338501 101572 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00029a001
CHEMBL30199 101572 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00029a001
10475320 96038 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 387 5 2 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(NC(=O)C(C)C)cccc23)c1C 10.1021/jm00008a013
CHEMBL26252 96038 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 387 5 2 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(NC(=O)C(C)C)cccc23)c1C 10.1021/jm00008a013
10338501 101572 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
CHEMBL30199 101572 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 359 4 2 5 3.2 CC(=O)Nc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12 10.1021/jm00008a013
56678452 62982 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC)C(=O)CNC(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1021/jm970161m
CHEMBL1793928 62982 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC)C(=O)CNC(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1021/jm970161m
44311288 202474 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 592 11 1 10 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1cccnc1 10.1016/S0960-894X(97)00400-9
CHEMBL70781 202474 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 592 11 1 10 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1cccnc1 10.1016/S0960-894X(97)00400-9
14673588 4326 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 342 6 1 4 5.0 CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12 10.1016/0960-894X(96)00232-6
CHEMBL10143 4326 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
ChEMBL 342 6 1 4 5.0 CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12 10.1016/0960-894X(96)00232-6
14673588 4326 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Compound was evaluated for binding affinity against human Endothelin A receptorCompound was evaluated for binding affinity against human Endothelin A receptor
ChEMBL 342 6 1 4 5.0 CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12 10.1016/0960-894X(96)00170-9
CHEMBL10143 4326 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Compound was evaluated for binding affinity against human Endothelin A receptorCompound was evaluated for binding affinity against human Endothelin A receptor
ChEMBL 342 6 1 4 5.0 CC(C)Oc1c(C(=O)O)sc2ccc(OCc3ccccc3)cc12 10.1016/0960-894X(96)00170-9
10790183 204512 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 461 8 1 6 4.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOc2ccccc2)cc1 10.1021/jm9505369
CHEMBL8677 204512 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 461 8 1 6 4.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOc2ccccc2)cc1 10.1021/jm9505369
127026058 136709 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 600 10 3 8 6.0 CCCc1nc2c(C)cc(C(=O)Nc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3751899 136709 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 600 10 3 8 6.0 CCCc1nc2c(C)cc(C(=O)Nc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
10839533 100962 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 513 5 2 9 2.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NC(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL297599 100962 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 513 5 2 9 2.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NC(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
10839947 116786 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 530 9 2 6 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL339657 116786 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 530 9 2 6 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
44320777 204473 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 550 10 2 8 4.7 COc1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL86505 204473 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
ChEMBL 550 10 2 8 4.7 COc1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00513-8
10415067 45094 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 546 8 2 6 5.0 O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
CHEMBL152713 45094 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 546 8 2 6 5.0 O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
10449375 95312 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 331 4 1 5 3.0 Cc1cc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)on1 10.1021/jm00008a013
CHEMBL25854 95312 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 331 4 1 5 3.0 Cc1cc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)on1 10.1021/jm00008a013
CHEMBL289687 209120 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
3811690 203689 3 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL80129 203689 3 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL289687 209120 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(95)00152-J
9826741 100277 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL292802 100277 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
127035082 135975 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 677 12 2 8 7.4 CCCc1nc2c(C)cc(C(=O)NCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3736262 135975 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 677 12 2 8 7.4 CCCc1nc2c(C)cc(C(=O)NCc3cccc(OC)c3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
15411002 108052 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 563 9 1 10 4.2 CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
CHEMBL320183 108052 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
ChEMBL 563 9 1 10 4.2 CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
44314661 102538 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 603 14 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL306977 102538 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 603 14 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
10646514 59012 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 434 7 1 6 5.1 N#Cc1ccc(OCc2ccc3ncoc3c2)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
CHEMBL170681 59012 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 434 7 1 6 5.1 N#Cc1ccc(OCc2ccc3ncoc3c2)cc1OC(C(=O)O)c1ccccc1Cl 10.1021/jm990378b
10619391 59907 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL173251 59907 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL174092 59907 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 374 7 1 5 4.0 Cc1ccccc1C(Oc1cc(OCc2ccncc2)ccc1C#N)C(=O)O 10.1021/jm990378b
9931773 77946 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1[C@H](Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
CHEMBL2110231 77946 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 417 7 1 6 4.4 Cc1ccccc1[C@H](Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O 10.1021/jm990378b
44311285 101816 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 635 13 2 10 6.4 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOC(=O)Nc2ccccn2)n1 10.1016/S0960-894X(97)00400-9
CHEMBL303428 101816 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 635 13 2 10 6.4 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOC(=O)Nc2ccccn2)n1 10.1016/S0960-894X(97)00400-9
10992620 201650 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL65070 201650 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44314646 203320 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 633 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCC1)C(=O)O 10.1021/jm9600914
CHEMBL77033 203320 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 633 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCC1)C(=O)O 10.1021/jm9600914
44314889 103254 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 633 12 5 4 4.7 CCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL308815 103254 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 633 12 5 4 4.7 CCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44314620 102657 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 587 12 5 4 4.4 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL307903 102657 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 587 12 5 4 4.4 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
23445404 100431 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 456 5 1 7 4.1 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00367-3
CHEMBL293877 100431 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
ChEMBL 456 5 1 7 4.1 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00367-3
10119105 100964 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 526 7 2 9 3.1 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC(=O)N(C)C)OCO3)c1Cl 10.1021/jm9608366
CHEMBL297618 100964 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 526 7 2 9 3.1 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC(=O)N(C)C)OCO3)c1Cl 10.1021/jm9608366
10650062 60108 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 537 10 4 6 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL175228 60108 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
ChEMBL 537 10 4 6 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
155517241 169580 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 522 14 2 11 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL4444355 169580 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 522 14 2 11 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
10129267 81262 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 617 13 1 12 3.9 CCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163714 81262 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 617 13 1 12 3.9 CCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
44314723 203279 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 583 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL76735 203279 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 583 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44314659 203400 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 631 12 5 4 4.5 C=CCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL77853 203400 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
ChEMBL 631 12 5 4 4.5 C=CCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
52949155 18212 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 557 10 2 7 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271640 18212 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 557 10 2 7 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10814318 9048 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 472 14 1 5 4.7 C=CCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL110064 9048 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
ChEMBL 472 14 1 5 4.7 C=CCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
52944083 18219 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 557 10 2 7 5.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)CC)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271691 18219 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
ChEMBL 557 10 2 7 5.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)CC)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
71456864 81266 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 618 13 2 12 3.0 CCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163718 81266 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 618 13 2 12 3.0 CCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
11734340 163148 0 None - 0 Pig 8.0 pIC50 = 8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 552 10 1 10 4.6 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccncc2)nc1 10.1021/jm0102304
CHEMBL420501 163148 0 None - 0 Pig 8.0 pIC50 = 8 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 552 10 1 10 4.6 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccncc2)nc1 10.1021/jm0102304
10501279 97753 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 402 6 1 5 4.1 COc1ccc(C2(O)OC(=O)C(c3cccc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL274307 97753 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 402 6 1 5 4.1 COc1ccc(C2(O)OC(=O)C(c3cccc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44371516 50697 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 469 7 1 6 5.6 CCOc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc(OC)cc2)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
CHEMBL157827 50697 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
ChEMBL 469 7 1 6 5.6 CCOc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc(OC)cc2)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
11794876 205437 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 393 7 1 4 4.9 O=C(O)/C(=C/c1cc(OCc2ccccc2)ccc1[N+](=O)[O-])c1ccccc1F 10.1021/jm970847e
CHEMBL92446 205437 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
ChEMBL 393 7 1 4 4.9 O=C(O)/C(=C/c1cc(OCc2ccccc2)ccc1[N+](=O)[O-])c1ccccc1F 10.1021/jm970847e
44213651 4218 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 343 3 1 4 4.2 OCC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
CHEMBL100795 4218 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
ChEMBL 343 3 1 4 4.2 OCC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12 10.1016/S0960-894X(96)00551-3
10742024 96482 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 446 7 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCc2ccccn2)cc1 10.1021/jm9505369
CHEMBL266143 96482 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
ChEMBL 446 7 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCc2ccccn2)cc1 10.1021/jm9505369
10841134 60112 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 589 10 4 6 5.3 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC23CC4CC(CC(C4)C2)C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL175277 60112 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 589 10 4 6 5.3 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC23CC4CC(CC(C4)C2)C3)nc1C(=O)O 10.1021/jm950592+
44311321 202475 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1cccnc1 10.1016/S0960-894X(97)00400-9
CHEMBL70788 202475 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1cccnc1 10.1016/S0960-894X(97)00400-9
5344 172891 98 None - 1 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/s0960-894x(00)00366-8
CHEMBL453 172891 98 None - 1 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/s0960-894x(00)00366-8
10015852 98969 2 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 268 3 2 5 1.8 Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C 10.1021/jm00004a012
CHEMBL282961 98969 2 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 268 3 2 5 1.8 Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C 10.1021/jm00004a012
22616255 203812 11 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL80945 203812 11 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1C 10.1016/0960-894X(96)00441-6
23445333 127271 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 484 6 1 7 4.4 Cc1cc2c(cc1CCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL366378 127271 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 484 6 1 7 4.4 Cc1cc2c(cc1CCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL313984 209367 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL317099 209442 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10792636 167939 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 544 10 2 6 5.4 CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.1021/jm990170q
CHEMBL435385 167939 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 544 10 2 6 5.4 CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.1021/jm990170q
CHEMBL315658 209435 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
127026042 136720 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 620 11 3 9 3.8 CCCc1nc2c(C)cc(C(=O)NCCN3CCN(C)CC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL3751986 136720 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
ChEMBL 620 11 3 9 3.8 CCCc1nc2c(C)cc(C(=O)NCCN3CCN(C)CC3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1 10.1039/C5MD00169B
CHEMBL315658 209435 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
11145367 9907 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 487 10 1 8 4.4 COCCOc1ncnc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1cccc(OC)c1 10.1021/jm0102304
CHEMBL114985 9907 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 487 10 1 8 4.4 COCCOc1ncnc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1cccc(OC)c1 10.1021/jm0102304
10745418 113480 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 9 2 6 6.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C(C)C)cccc2C(C)C)cc1 10.1021/jm990170q
CHEMBL332627 113480 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 9 2 6 6.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C(C)C)cccc2C(C)C)cc1 10.1021/jm990170q
10015852 98969 2 None - 0 Human 5.0 pIC50 = 5.0 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 268 3 2 5 1.8 Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C 10.1021/jm00029a001
CHEMBL282961 98969 2 None - 0 Human 5.0 pIC50 = 5.0 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 268 3 2 5 1.8 Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C 10.1021/jm00029a001
10015852 98969 2 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 268 3 2 5 1.8 Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C 10.1021/jm00008a013
CHEMBL282961 98969 2 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 268 3 2 5 1.8 Cc1noc(NS(=O)(=O)c2ccc(O)cc2)c1C 10.1021/jm00008a013
11813885 167220 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 579 12 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCCOc2ncc(C)cn2)c1 10.1021/jm0102304
CHEMBL430515 167220 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
ChEMBL 579 12 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCCOc2ncc(C)cn2)c1 10.1021/jm0102304
CHEMBL313056 209355 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
10576217 9654 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 467 12 1 5 4.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccnc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113494 9654 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
ChEMBL 467 12 1 5 4.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccnc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL146155 207023 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
11798109 12238 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 7 4.2 COc1cccc(NCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL1185459 12238 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 7 4.2 COc1cccc(NCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL416086 12238 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 7 4.2 COc1cccc(NCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
23445544 61031 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Tested for its activity in cloned human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for its activity in cloned human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 438 5 1 5 5.1 Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
CHEMBL176912 61031 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Tested for its activity in cloned human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for its activity in cloned human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 438 5 1 5 5.1 Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
3887 2033 39 None -436 4 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrs
ChEMBL None None None None 10.1021/acs.jmedchem.5b01781
5311192 2033 39 None -436 4 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrs
ChEMBL None None None None 10.1021/acs.jmedchem.5b01781
CHEMBL72410 2033 39 None -436 4 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrs
ChEMBL None None None None 10.1021/acs.jmedchem.5b01781
44386002 59963 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 503 9 1 9 3.9 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL174326 59963 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 503 9 1 9 3.9 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
11005242 201197 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2 10.1021/jm010382z
CHEMBL62719 201197 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2 10.1021/jm010382z
44293682 185094 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 447 7 1 6 4.4 CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL48652 185094 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 447 7 1 6 4.4 CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10553165 9633 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 492 7 1 6 5.4 O=C1OC(O)(c2ccc(OCc3ccccc3)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL11341 9633 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
ChEMBL 492 7 1 6 5.4 O=C1OC(O)(c2ccc(OCc3ccccc3)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL414917 211402 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity in LtK cells stably transfected with human endothelin A (ETA) receptorBinding affinity in LtK cells stably transfected with human endothelin A (ETA) receptor
ChEMBL None None None NC(=O)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00084-7
CHEMBL289687 209120 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
CHEMBL289687 209120 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
127035085 135896 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 661 12 2 7 7.4 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
CHEMBL3735574 135896 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
ChEMBL 661 12 2 7 7.4 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1039/C4MD00499J
44293741 186368 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 447 7 1 6 4.4 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1021/jm031041j
CHEMBL49040 186368 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
ChEMBL 447 7 1 6 4.4 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1021/jm031041j
44293868 101106 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 551 11 2 9 3.9 CCOc1ccc2c(c1)[C@H](c1ccc(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL298664 101106 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 551 11 2 9 3.9 CCOc1ccc2c(c1)[C@H](c1ccc(OC)c(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
44293741 186368 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 447 7 1 6 4.4 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL49040 186368 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
ChEMBL 447 7 1 6 4.4 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
44384766 59338 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 532 10 1 10 4.1 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL172184 59338 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 532 10 1 10 4.1 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
44385940 130137 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368255 130137 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 551 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O 10.1021/jm950592+
44386421 60398 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 537 10 4 5 4.5 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1CC(=O)O 10.1021/jm950592+
CHEMBL176093 60398 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
ChEMBL 537 10 4 5 4.5 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)nc1CC(=O)O 10.1021/jm950592+
9807456 60135 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 545 9 1 9 4.8 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL175435 60135 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
ChEMBL 545 9 1 9 4.8 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10195727 202220 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 487 7 1 8 5.6 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1016/s0960-894x(97)10151-2
CHEMBL69150 202220 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
ChEMBL 487 7 1 8 5.6 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1016/s0960-894x(97)10151-2
10195727 202220 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 487 7 1 8 5.6 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1021/jm0300429
CHEMBL69150 202220 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Potency at Endothelin A receptor was determinedPotency at Endothelin A receptor was determined
ChEMBL 487 7 1 8 5.6 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1021/jm0300429
44279360 106095 0 None - 0 Pig 6.0 pIC50 = 6.0 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 498 13 5 4 2.9 CC(C)C[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
CHEMBL31426 106095 0 None - 0 Pig 6.0 pIC50 = 6.0 Binding
Binding affinity against ETA receptor in porcine aortic smooth muscle membraneBinding affinity against ETA receptor in porcine aortic smooth muscle membrane
ChEMBL 498 13 5 4 2.9 CC(C)C[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)O 10.1016/0960-894X(95)00221-E
11048815 101832 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)OC(c1ccc3c(c1)OCO3)C(C(=O)O)=C2c1ccc(OC)cc1 10.1021/jm010382z
CHEMBL303531 101832 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)OC(c1ccc3c(c1)OCO3)C(C(=O)O)=C2c1ccc(OC)cc1 10.1021/jm010382z
10625738 168915 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 517 6 2 6 5.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(-c3ccccc3)cc2)c1Br 10.1021/jm9608366
CHEMBL44321 168915 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
ChEMBL 517 6 2 6 5.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(-c3ccccc3)cc2)c1Br 10.1021/jm9608366
9801094 59164 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 399 7 1 5 5.1 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1cccc(Cl)c1 10.1021/jm990378b
CHEMBL171446 59164 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
ChEMBL 399 7 1 5 5.1 N#Cc1ccc(OCc2ccsc2)cc1OC(C(=O)O)c1cccc(Cl)c1 10.1021/jm990378b
44316686 103029 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1C 10.1016/0960-894X(96)00441-6
CHEMBL308521 103029 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1C 10.1016/0960-894X(96)00441-6
10021240 95038 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 357 6 2 5 3.7 Cc1noc(NS(=O)(=O)c2ccc(NCc3ccccc3)cc2)c1C 10.1021/jm00029a001
CHEMBL25730 95038 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
ChEMBL 357 6 2 5 3.7 Cc1noc(NS(=O)(=O)c2ccc(NCc3ccccc3)cc2)c1C 10.1021/jm00029a001
10021240 95038 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 357 6 2 5 3.7 Cc1noc(NS(=O)(=O)c2ccc(NCc3ccccc3)cc2)c1C 10.1021/jm00008a013
CHEMBL25730 95038 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 357 6 2 5 3.7 Cc1noc(NS(=O)(=O)c2ccc(NCc3ccccc3)cc2)c1C 10.1021/jm00008a013
10087192 99109 1 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3cccc(N)c3c2)c1C 10.1021/jm00008a013
CHEMBL283879 99109 1 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3cccc(N)c3c2)c1C 10.1021/jm00008a013
10087192 99109 1 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3cccc(N)c3c2)c1C 10.1021/jm00004a012
CHEMBL283879 99109 1 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
ChEMBL 317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3cccc(N)c3c2)c1C 10.1021/jm00004a012
44276993 106358 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 362 5 1 3 3.8 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144831 106358 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
ChEMBL 362 5 1 3 3.8 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(00)00232-8
5472495 186041 41 None - 1 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 372 4 1 3 4.0 CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1 nan
CHEMBL488025 186041 41 None - 1 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 372 4 1 3 4.0 CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1 nan
18617381 105188 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 300 3 1 4 3.1 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL312551 105188 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 300 3 1 4 3.1 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1C 10.1016/0960-894X(96)00441-6
15453170 104409 4 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL311258 104409 4 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1C 10.1016/0960-894X(96)00441-6
1009 192 20 None - 1 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
5310991 192 20 None - 1 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
CHEMBL332794 192 20 None - 1 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
44284481 211967 0 None -6 5 Rat 9.8 pKd = 9.8 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL437472 211967 0 None -6 5 Rat 9.8 pKd = 9.8 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL409577 211012 0 None - 1 Rat 9.5 pKd = 9.5 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)
ChEMBL None None None CCCC[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC1=O 10.1016/S0960-894X(01)81085-4
CHEMBL442316 212153 0 None - 1 Rat 9.2 pKd = 9.2 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
19095644 169134 0 None - 1 Rat 6.9 pKd = 6.9 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 549 10 2 8 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4438132 169134 0 None - 1 Rat 6.9 pKd = 6.9 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 549 10 2 8 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccccc2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL438470 212014 0 None - 1 Rat 6.9 pKd = 6.9 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](C)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL412467 211236 0 None - 1 Rat 5.9 pKd = 5.9 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
19735343 175467 0 None - 1 Rat 5.8 pKd = 5.8 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 473 7 2 6 4.0 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4590568 175467 0 None - 1 Rat 5.8 pKd = 5.8 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 473 7 2 6 4.0 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL409577 211012 0 None - 1 Rat 7.8 pKd = 7.8 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)
ChEMBL None None None CCCC[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC1=O 10.1016/S0960-894X(01)81085-4
CHEMBL386629 210628 0 None - 1 Rat 6.7 pKd = 6.7 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
155519384 169839 0 None - 1 Rat 7.7 pKd = 7.7 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 674 12 1 13 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL4448273 169839 0 None - 1 Rat 7.7 pKd = 7.7 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 674 12 1 13 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL438027 211985 0 None - 1 Rat 5.7 pKd = 5.7 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL263581 208821 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/S0960-894X(01)81085-4
CHEMBL410001 211037 0 None - 1 Rat 5.5 pKd = 5.5 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL412467 211236 0 None - 1 Rat 7.5 pKd = 7.5 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL409171 210992 0 None - 1 Rat 5.5 pKd = 5.5 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/S0960-894X(01)81085-4
104865 697 94 None -1 4 Rat 7.4 pKd = 7.4 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
3494 697 94 None -1 4 Rat 7.4 pKd = 7.4 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
392 697 94 None -1 4 Rat 7.4 pKd = 7.4 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
CHEMBL957 697 94 None -1 4 Rat 7.4 pKd = 7.4 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
DB00559 697 94 None -1 4 Rat 7.4 pKd = 7.4 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
10395582 16772 0 None - 1 Rat 5.4 pKd = 5.4 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL 806 8 6 13 3.2 CC(=O)O[C@@]12CO[C@@H]1C[C@H](O)[C@@]1(C)C(=O)[C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)Nc4ccccc4)C(C)(C)C)C[C@@](O)([C@@H](OC(=O)c4ccccc4)[C@@H]12)C3(C)C 10.1016/S0960-894X(01)81085-4
CHEMBL125377 16772 0 None - 1 Rat 5.4 pKd = 5.4 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL 806 8 6 13 3.2 CC(=O)O[C@@]12CO[C@@H]1C[C@H](O)[C@@]1(C)C(=O)[C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)Nc4ccccc4)C(C)(C)C)C[C@@](O)([C@@H](OC(=O)c4ccccc4)[C@@H]12)C3(C)C 10.1016/S0960-894X(01)81085-4
CHEMBL414286 211362 0 None - 1 Rat 6.4 pKd = 6.4 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](C)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL409578 211013 0 None - 1 Rat 5.3 pKd = 5.3 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](NC(C)=O)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL412346 211227 0 None - 1 Rat 7.3 pKd = 7.3 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL438027 211985 0 None - 1 Rat 8.2 pKd = 8.2 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL268318 208989 0 None - 1 Rat 6.2 pKd = 6.2 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL442316 212153 0 None - 1 Rat 7.1 pKd = 7.1 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 2)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL414286 211362 0 None - 1 Rat 8.0 pKd = 8.0 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](C)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81085-4
CHEMBL407887 210935 0 None - 1 Rat 6.0 pKd = 6.0 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligandBinding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
ChEMBL None None None CSCC[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC1=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)O)CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N2 10.1016/S0960-894X(01)81085-4
10983585 172693 0 None - 1 Rat 6.0 pKd = 6.0 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 473 9 2 8 3.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4525321 172693 0 None - 1 Rat 6.0 pKd = 6.0 Binding
Antagonist activity at rat aortic ring ETA receptor in presence of ET1Antagonist activity at rat aortic ring ETA receptor in presence of ET1
ChEMBL 473 9 2 8 3.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL409171 210992 0 None - 1 Rat 7.0 pKd = 7.0 Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand (Exp 1)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/S0960-894X(01)81085-4
44277840 97789 0 None 81283 2 Human 11.0 pKi = 11 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 522 7 1 7 5.8 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2N(C)C(=O)CC(C)(C)C)c1C 10.1021/jm020289q
CHEMBL274489 97789 0 None 81283 2 Human 11.0 pKi = 11 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 522 7 1 7 5.8 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2N(C)C(=O)CC(C)(C)C)c1C 10.1021/jm020289q
11071765 168630 0 None 8709 2 Human 11.0 pKi = 11 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 556 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccc2)c1C 10.1021/jm020289q
CHEMBL440780 168630 0 None 8709 2 Human 11.0 pKi = 11 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 556 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccc2)c1C 10.1021/jm020289q
44275660 98210 0 None - 1 Human 11.0 pKi = 11 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 522 8 2 7 5.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNC(=O)CC(C)(C)C)c1C 10.1021/jm030480f
CHEMBL277447 98210 0 None - 1 Human 11.0 pKi = 11 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 522 8 2 7 5.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNC(=O)CC(C)(C)C)c1C 10.1021/jm030480f
9852318 9508 5 None 2691 2 Human 10.8 pKi = 10.8 Binding
Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL112624 9508 5 None 2691 2 Human 10.8 pKi = 10.8 Binding
Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL1627022 9508 5 None 2691 2 Human 10.8 pKi = 10.8 Binding
Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
10119517 98764 0 None 169824 2 Human 10.7 pKi = 10.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 536 8 1 7 5.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(C)(C)C)c1C 10.1021/jm020289q
CHEMBL281659 98764 0 None 169824 2 Human 10.7 pKi = 10.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 536 8 1 7 5.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(C)(C)C)c1C 10.1021/jm020289q
11124425 99389 0 None 75857 2 Human 10.7 pKi = 10.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 543 7 1 8 5.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccc(C(F)(F)F)n2)c1C 10.1021/jm020289q
CHEMBL285832 99389 0 None 75857 2 Human 10.7 pKi = 10.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 543 7 1 8 5.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccc(C(F)(F)F)n2)c1C 10.1021/jm020289q
10918301 101013 0 None 7585 2 Human 10.7 pKi = 10.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 514 8 1 7 6.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)c2ccccc2)c1C 10.1021/jm020289q
CHEMBL29793 101013 0 None 7585 2 Human 10.7 pKi = 10.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 514 8 1 7 6.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)c2ccccc2)c1C 10.1021/jm020289q
44284481 211967 0 None -4 5 Human 10.6 pKi = 10.6 Binding
Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.ejmech.2013.01.044
CHEMBL437472 211967 0 None -4 5 Human 10.6 pKi = 10.6 Binding
Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.ejmech.2013.01.044
11731054 98342 0 None 21379 2 Human 10.5 pKi = 10.5 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 522 7 1 7 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)(C)C)c1C 10.1021/jm020289q
CHEMBL27855 98342 0 None 21379 2 Human 10.5 pKi = 10.5 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 522 7 1 7 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)(C)C)c1C 10.1021/jm020289q
159594 518 38 None -1 3 Rat 10.5 pKi = 10.5 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm030528p
3487 518 38 None -1 3 Rat 10.5 pKi = 10.5 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm030528p
CHEMBL9194 518 38 None -1 3 Rat 10.5 pKi = 10.5 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm030528p
DB06199 518 38 None -1 3 Rat 10.5 pKi = 10.5 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm030528p
186002 102356 19 None -1 3 Rat 10.5 pKi = 10.5 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 531 10 2 6 5.4 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm030528p
CHEMBL305576 102356 19 None -1 3 Rat 10.5 pKi = 10.5 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 531 10 2 6 5.4 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm030528p
44284481 211967 0 None -6 5 Rat 10.5 pKi = 10.5 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
CHEMBL437472 211967 0 None -6 5 Rat 10.5 pKi = 10.5 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
159594 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/acs.jmedchem.5b01781
3487 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/acs.jmedchem.5b01781
CHEMBL9194 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/acs.jmedchem.5b01781
DB06199 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/acs.jmedchem.5b01781
159594 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
3487 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
CHEMBL9194 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
DB06199 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
9936145 18822 1 None - 1 Human 10.4 pKi = 10.4 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
CHEMBL128818 18822 1 None - 1 Human 10.4 pKi = 10.4 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
44284481 211967 0 None -3 5 Pig 10.4 pKi = 10.4 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL437472 211967 0 None -3 5 Pig 10.4 pKi = 10.4 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
9958321 78726 0 None 19498 2 Human 10.4 pKi = 10.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C 10.1021/jm020289q
CHEMBL2113316 78726 0 None 19498 2 Human 10.4 pKi = 10.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C 10.1021/jm020289q
11813553 98874 0 None 14454 2 Human 10.4 pKi = 10.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 542 8 1 7 5.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2ccccc2)c1C 10.1021/jm020289q
CHEMBL282359 98874 0 None 14454 2 Human 10.4 pKi = 10.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 542 8 1 7 5.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2ccccc2)c1C 10.1021/jm020289q
11027595 99764 0 None 19952 2 Human 10.4 pKi = 10.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)C)c1C 10.1021/jm020289q
CHEMBL28863 99764 0 None 19952 2 Human 10.4 pKi = 10.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)C)c1C 10.1021/jm020289q
10918368 102037 0 None 21379 2 Human 10.4 pKi = 10.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CC(C)(C)CC2=O)c1C 10.1021/jm020289q
CHEMBL30405 102037 0 None 21379 2 Human 10.4 pKi = 10.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CC(C)(C)CC2=O)c1C 10.1021/jm020289q
159594 518 38 None -1 3 Rat 10.3 pKi = 10.3 Binding
binding affinity against human Endothelin A receptorbinding affinity against human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
3487 518 38 None -1 3 Rat 10.3 pKi = 10.3 Binding
binding affinity against human Endothelin A receptorbinding affinity against human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
CHEMBL9194 518 38 None -1 3 Rat 10.3 pKi = 10.3 Binding
binding affinity against human Endothelin A receptorbinding affinity against human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
DB06199 518 38 None -1 3 Rat 10.3 pKi = 10.3 Binding
binding affinity against human Endothelin A receptorbinding affinity against human Endothelin A receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
11082168 98745 0 None 7585 2 Human 10.3 pKi = 10.3 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 548 8 1 7 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(F)(F)F)c1C 10.1021/jm020289q
CHEMBL281549 98745 0 None 7585 2 Human 10.3 pKi = 10.3 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 548 8 1 7 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(F)(F)F)c1C 10.1021/jm020289q
10929533 99878 0 None 10964 2 Human 10.3 pKi = 10.3 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 534 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)C)C2CC2)c1C 10.1021/jm020289q
CHEMBL28963 99878 0 None 10964 2 Human 10.3 pKi = 10.3 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 534 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)C)C2CC2)c1C 10.1021/jm020289q
9914310 204907 3 None 1995 2 Human 10.2 pKi = 10.2 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8923 204907 3 None 1995 2 Human 10.2 pKi = 10.2 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
11762890 100183 0 None 14791 2 Human 10.2 pKi = 10.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 505 8 2 9 5.3 Cc1cc(NCc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)no1 10.1021/jm020289q
CHEMBL29223 100183 0 None 14791 2 Human 10.2 pKi = 10.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 505 8 2 9 5.3 Cc1cc(NCc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)no1 10.1021/jm020289q
131845706 3403 6 None -11 2 Rat 10.1 pKi = 10.1 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL None None None None 10.1021/jm00087a001
71308726 3403 6 None -11 2 Rat 10.1 pKi = 10.1 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL None None None None 10.1021/jm00087a001
995 3403 6 None -11 2 Rat 10.1 pKi = 10.1 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL1222310 3403 6 None -11 2 Rat 10.1 pKi = 10.1 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL4524099 3403 6 None -11 2 Rat 10.1 pKi = 10.1 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL None None None None 10.1021/jm00087a001
44284481 211967 0 None -6 5 Rat 10.0 pKi = 10.0 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
CHEMBL437472 211967 0 None -6 5 Rat 10.0 pKi = 10.0 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
9937336 174097 1 None 229 2 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 510 9 1 7 4.8 CCCc1nc(C)ccc1O[C@@H](C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2016.06.014
CHEMBL4559129 174097 1 None 229 2 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 510 9 1 7 4.8 CCCc1nc(C)ccc1O[C@@H](C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2016.06.014
9865409 101846 0 None 199 2 Human 9.9 pKi = 9.9 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 394 8 1 6 3.2 COc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL303631 101846 0 None 199 2 Human 9.9 pKi = 9.9 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 394 8 1 6 3.2 COc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
9894460 204972 6 None 24 3 Human 9.9 pKi = 9.9 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm9505369
CHEMBL313871 204972 6 None 24 3 Human 9.9 pKi = 9.9 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm9505369
CHEMBL8978 204972 6 None 24 3 Human 9.9 pKi = 9.9 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm9505369
12286 933 30 None 1348 2 Human 9.9 pKi = 9.9 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1021/jm980217s
6433095 933 30 None 1348 2 Human 9.9 pKi = 9.9 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1021/jm980217s
CHEMBL109648 933 30 None 1348 2 Human 9.9 pKi = 9.9 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1021/jm980217s
DB06677 933 30 None 1348 2 Human 9.9 pKi = 9.9 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1021/jm980217s
44284481 211967 0 None -4 5 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2013.01.025
CHEMBL437472 211967 0 None -4 5 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2013.01.025
44284481 211967 0 None -4 5 Human 9.9 pKi = 9.9 Binding
Displacement of radiolabeled endothelin-1 from human endothelin ETA receptorDisplacement of radiolabeled endothelin-1 from human endothelin ETA receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm8007618
CHEMBL437472 211967 0 None -4 5 Human 9.9 pKi = 9.9 Binding
Displacement of radiolabeled endothelin-1 from human endothelin ETA receptorDisplacement of radiolabeled endothelin-1 from human endothelin ETA receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm8007618
10973161 100562 0 None 6456 2 Human 9.8 pKi = 9.8 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 502 8 2 9 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNc2ccncn2)c1C 10.1021/jm020289q
CHEMBL29464 100562 0 None 6456 2 Human 9.8 pKi = 9.8 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 502 8 2 9 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNc2ccncn2)c1C 10.1021/jm020289q
11103326 167331 0 None 12589 2 Human 9.8 pKi = 9.8 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 520 8 1 7 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(F)(F)F)c1C 10.1021/jm020289q
CHEMBL431296 167331 0 None 12589 2 Human 9.8 pKi = 9.8 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 520 8 1 7 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(F)(F)F)c1C 10.1021/jm020289q
9870830 204977 34 None 66 2 Human 9.8 pKi = 9.8 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9505369
CHEMBL8981 204977 34 None 66 2 Human 9.8 pKi = 9.8 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9505369
23670447 2968 2 None 114 2 Human 9.8 pKi = 9.8 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm980217s
999 2968 2 None 114 2 Human 9.8 pKi = 9.8 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm980217s
CHEMBL1204799 2968 2 None 114 2 Human 9.8 pKi = 9.8 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm980217s
CHEMBL25438 2968 2 None 114 2 Human 9.8 pKi = 9.8 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm980217s
108002 3425 14 None 56 2 Human 9.7 pKi = 9.7 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm970101g
3528 3425 14 None 56 2 Human 9.7 pKi = 9.7 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm970101g
CHEMBL8823 3425 14 None 56 2 Human 9.7 pKi = 9.7 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm970101g
11754273 100491 0 None 21877 2 Human 9.7 pKi = 9.7 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 466 7 2 7 4.1 CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm000105c
CHEMBL29422 100491 0 None 21877 2 Human 9.7 pKi = 9.7 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 466 7 2 7 4.1 CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm000105c
11059912 98868 0 None 23988 2 Human 9.7 pKi = 9.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 481 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COCC(C)C)c1C 10.1021/jm020289q
CHEMBL282303 98868 0 None 23988 2 Human 9.7 pKi = 9.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 481 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COCC(C)C)c1C 10.1021/jm020289q
10972867 99229 0 None 19952 2 Human 9.7 pKi = 9.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 480 7 1 7 4.4 CC(=O)N(C)Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm020289q
CHEMBL284656 99229 0 None 19952 2 Human 9.7 pKi = 9.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 480 7 1 7 4.4 CC(=O)N(C)Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm020289q
11754273 100491 0 None 21877 2 Human 9.7 pKi = 9.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 466 7 2 7 4.1 CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm020289q
CHEMBL29422 100491 0 None 21877 2 Human 9.7 pKi = 9.7 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 466 7 2 7 4.1 CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm020289q
131845706 3403 6 None -11 2 Rat 9.6 pKi = 9.6 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta
ChEMBL None None None None 10.1021/jm00087a001
71308726 3403 6 None -11 2 Rat 9.6 pKi = 9.6 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta
ChEMBL None None None None 10.1021/jm00087a001
995 3403 6 None -11 2 Rat 9.6 pKi = 9.6 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL1222310 3403 6 None -11 2 Rat 9.6 pKi = 9.6 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL4524099 3403 6 None -11 2 Rat 9.6 pKi = 9.6 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta
ChEMBL None None None None 10.1021/jm00087a001
11123603 101313 0 None 14125 2 Human 9.5 pKi = 9.5 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccnc2)c1C 10.1021/jm020289q
CHEMBL30009 101313 0 None 14125 2 Human 9.5 pKi = 9.5 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccnc2)c1C 10.1021/jm020289q
11730445 101425 0 None 4677 2 Human 9.5 pKi = 9.5 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2cccn2)c1C 10.1021/jm020289q
CHEMBL30092 101425 0 None 4677 2 Human 9.5 pKi = 9.5 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2cccn2)c1C 10.1021/jm020289q
11082049 99086 0 None 933 2 Human 9.4 pKi = 9.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 534 7 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCCC(C)(C)C2=O)c1C 10.1021/jm020289q
CHEMBL283610 99086 0 None 933 2 Human 9.4 pKi = 9.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 534 7 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCCC(C)(C)C2=O)c1C 10.1021/jm020289q
10432263 101669 0 None 85 2 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 420 8 1 6 3.4 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2 10.1021/jm960274q
CHEMBL302564 101669 0 None 85 2 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 420 8 1 6 3.4 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2 10.1021/jm960274q
10864118 100985 0 None 4265 2 Human 9.4 pKi = 9.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.2 CC(=O)N(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C)C(C)C 10.1021/jm020289q
CHEMBL29775 100985 0 None 4265 2 Human 9.4 pKi = 9.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.2 CC(=O)N(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C)C(C)C 10.1021/jm020289q
11477084 3540 46 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
216235 3540 46 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
3548 3540 46 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
3950 3540 46 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
CHEMBL282724 3540 46 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
DB06268 3540 46 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
11477084 3540 46 None -1 2 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
216235 3540 46 None -1 2 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
3548 3540 46 None -1 2 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
3950 3540 46 None -1 2 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
CHEMBL282724 3540 46 None -1 2 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
DB06268 3540 46 None -1 2 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
108002 3425 14 None 56 2 Human 9.4 pKi = 9.4 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm00037a003
3528 3425 14 None 56 2 Human 9.4 pKi = 9.4 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm00037a003
CHEMBL8823 3425 14 None 56 2 Human 9.4 pKi = 9.4 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm00037a003
108002 3425 14 None 56 2 Human 9.4 pKi = 9.4 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm9505369
3528 3425 14 None 56 2 Human 9.4 pKi = 9.4 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm9505369
CHEMBL8823 3425 14 None 56 2 Human 9.4 pKi = 9.4 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm9505369
44339756 110270 0 None - 1 Human 9.4 pKi = 9.4 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 454 6 1 8 4.0 Cc1cc2c(cc1CC(=O)c1ccsc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm980217s
CHEMBL326059 110270 0 None - 1 Human 9.4 pKi = 9.4 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 454 6 1 8 4.0 Cc1cc2c(cc1CC(=O)c1ccsc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm980217s
9849547 183414 0 None 34 2 Human 9.4 pKi = 9.4 Binding
Tested for in vitro inhibition of [125I]ET1 binding to CHO cells expressing human Endothelin A receptorTested for in vitro inhibition of [125I]ET1 binding to CHO cells expressing human Endothelin A receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)[C@@H](C(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL48196 183414 0 None 34 2 Human 9.4 pKi = 9.4 Binding
Tested for in vitro inhibition of [125I]ET1 binding to CHO cells expressing human Endothelin A receptorTested for in vitro inhibition of [125I]ET1 binding to CHO cells expressing human Endothelin A receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)[C@@H](C(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
11734435 100819 0 None 6456 2 Human 9.4 pKi = 9.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 562 9 1 7 6.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC2CCCCC2)c1C 10.1021/jm020289q
CHEMBL29652 100819 0 None 6456 2 Human 9.4 pKi = 9.4 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 562 9 1 7 6.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC2CCCCC2)c1C 10.1021/jm020289q
9915028 9306 12 None 28183 2 Human 9.3 pKi = 9.3 Binding
Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRA
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC nan
CHEMBL111612 9306 12 None 28183 2 Human 9.3 pKi = 9.3 Binding
Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRA
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC nan
CHEMBL4761843 9306 12 None 28183 2 Human 9.3 pKi = 9.3 Binding
Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000348aPTSA EDNRA
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC nan
9915028 9306 12 None 28183 2 Human 9.3 pKi = 9.3 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm010237l
CHEMBL111612 9306 12 None 28183 2 Human 9.3 pKi = 9.3 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm010237l
CHEMBL4761843 9306 12 None 28183 2 Human 9.3 pKi = 9.3 Binding
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm010237l
9915028 9306 12 None 28183 2 Human 9.3 pKi = 9.3 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL111612 9306 12 None 28183 2 Human 9.3 pKi = 9.3 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL4761843 9306 12 None 28183 2 Human 9.3 pKi = 9.3 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
10815239 108058 0 None 125 2 Human 9.3 pKi = 9.3 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 500 10 1 7 5.0 COc1ccc(OC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL320224 108058 0 None 125 2 Human 9.3 pKi = 9.3 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 500 10 1 7 5.0 COc1ccc(OC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
11794992 4888 0 None 39810 2 Human 9.3 pKi = 9.3 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cocn3)cc2)c1C 10.1021/jm000105c
CHEMBL104848 4888 0 None 39810 2 Human 9.3 pKi = 9.3 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cocn3)cc2)c1C 10.1021/jm000105c
11812665 99294 0 None 18197 2 Human 9.2 pKi = 9.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 467 8 1 7 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COC(C)C)c1C 10.1021/jm020289q
CHEMBL285118 99294 0 None 18197 2 Human 9.2 pKi = 9.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 467 8 1 7 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COC(C)C)c1C 10.1021/jm020289q
11124545 100890 0 None 4168 2 Human 9.2 pKi = 9.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 557 9 1 8 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccn2)c1C 10.1021/jm020289q
CHEMBL29710 100890 0 None 4168 2 Human 9.2 pKi = 9.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 557 9 1 8 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccn2)c1C 10.1021/jm020289q
10907333 101599 0 None 1819 2 Human 9.2 pKi = 9.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 508 7 2 7 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)NC(C)(C)C)c1C 10.1021/jm020289q
CHEMBL30215 101599 0 None 1819 2 Human 9.2 pKi = 9.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 508 7 2 7 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)NC(C)(C)C)c1C 10.1021/jm020289q
10786696 102301 0 None 223 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 392 8 1 5 3.8 CCc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL305270 102301 0 None 223 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 392 8 1 5 3.8 CCc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
11081276 100740 0 None 2238 2 Human 9.1 pKi = 9.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 476 7 1 8 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cc2ncco2)c1C 10.1021/jm020289q
CHEMBL29598 100740 0 None 2238 2 Human 9.1 pKi = 9.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 476 7 1 8 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cc2ncco2)c1C 10.1021/jm020289q
10973218 100487 0 None 3388 2 Human 9.1 pKi = 9.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 506 8 2 7 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNCC(F)(F)F)c1C 10.1021/jm020289q
CHEMBL29420 100487 0 None 3388 2 Human 9.1 pKi = 9.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 506 8 2 7 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNCC(F)(F)F)c1C 10.1021/jm020289q
44311692 102678 0 None -3 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 667 13 3 7 4.5 C=CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL308102 102678 0 None -3 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 667 13 3 7 4.5 C=CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
9822616 121465 0 None 17782 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL359273 121465 0 None 17782 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
9979632 102415 0 None 41 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 422 8 1 7 2.8 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2 10.1021/jm960274q
CHEMBL305980 102415 0 None 41 2 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 422 8 1 7 2.8 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2 10.1021/jm960274q
17979744 18055 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 657 10 1 8 6.6 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CN3CCC(C)(C)C3=O)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
CHEMBL12703 18055 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 657 10 1 8 6.6 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CN3CCC(C)(C)C3=O)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
197712 101697 51 None 194 2 Human 9.0 pKi = 9 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 378 7 1 5 3.5 COC(c1ccccc1)(c1ccccc1)C(Oc1nc(C)cc(C)n1)C(=O)O 10.1021/jm960274q
CHEMBL302753 101697 51 None 194 2 Human 9.0 pKi = 9 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 378 7 1 5 3.5 COC(c1ccccc1)(c1ccccc1)C(Oc1nc(C)cc(C)n1)C(=O)O 10.1021/jm960274q
10763862 162654 0 None 1096 2 Human 9.0 pKi = 9 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 406 9 1 5 4.0 CCc1cc(CC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL418326 162654 0 None 1096 2 Human 9.0 pKi = 9 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 406 9 1 5 4.0 CCc1cc(CC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
11733544 98765 0 None 7244 2 Human 9.0 pKi = 9 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 480 7 1 7 4.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)N(C)C)c1C 10.1021/jm020289q
CHEMBL281668 98765 0 None 7244 2 Human 9.0 pKi = 9 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 480 7 1 7 4.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)N(C)C)c1C 10.1021/jm020289q
11103112 99393 0 None 4570 2 Human 9.0 pKi = 9 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 501 8 1 7 6.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COc2ccccc2)c1C 10.1021/jm020289q
CHEMBL28586 99393 0 None 4570 2 Human 9.0 pKi = 9 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 501 8 1 7 6.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COc2ccccc2)c1C 10.1021/jm020289q
178103 167377 9 None 100 2 Human 9.0 pKi = 9.0 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 506 10 2 7 4.6 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm970101g
CHEMBL431651 167377 9 None 100 2 Human 9.0 pKi = 9.0 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 506 10 2 7 4.6 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm970101g
178103 167377 9 None 100 2 Human 9.0 pKi = 9.0 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 506 10 2 7 4.6 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm980217s
CHEMBL431651 167377 9 None 100 2 Human 9.0 pKi = 9.0 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 506 10 2 7 4.6 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm980217s
10840560 4584 0 None 2 2 Human 8.9 pKi = 8.9 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 558 13 1 8 5.2 COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC 10.1021/jm9910425
CHEMBL103201 4584 0 None 2 2 Human 8.9 pKi = 8.9 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 558 13 1 8 5.2 COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC 10.1021/jm9910425
9843631 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL24461 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1016/s0960-894x(01)00791-0
9843631 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm300682j
CHEMBL24461 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm300682j
9843631 92766 9 None -1 4 Rat 8.9 pKi = 8.9 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm030528p
CHEMBL24461 92766 9 None -1 4 Rat 8.9 pKi = 8.9 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm030528p
9843631 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm020138n
CHEMBL24461 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm020138n
9843631 92766 9 None -1 4 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting method
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1016/j.bmcl.2016.06.014
CHEMBL24461 92766 9 None -1 4 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting method
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1016/j.bmcl.2016.06.014
9843631 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm000105c
CHEMBL24461 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm000105c
9843631 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm020289q
CHEMBL24461 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm020289q
9843631 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm030480f
CHEMBL24461 92766 9 None 1 4 Human 8.9 pKi = 8.9 Binding
Inhibitory concentration against Endothelin A receptorInhibitory concentration against Endothelin A receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm030480f
9938533 104921 1 None -1 2 Human 8.8 pKi = 8.8 Binding
Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
CHEMBL311854 104921 1 None -1 2 Human 8.8 pKi = 8.8 Binding
Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
10553793 4380 0 None 75 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 512 11 2 6 4.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(C(=O)O)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL101742 4380 0 None 75 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 512 11 2 6 4.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(C(=O)O)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
11113812 100316 0 None 1258 2 Human 8.8 pKi = 8.8 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 497 7 1 6 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C\c2ccccc2)c1C 10.1021/jm020289q
CHEMBL29313 100316 0 None 1258 2 Human 8.8 pKi = 8.8 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 497 7 1 6 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C\c2ccccc2)c1C 10.1021/jm020289q
CHEMBL1790180 207130 0 None -72 3 Rat 8.8 pKi = 8.8 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
9938533 104921 1 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00387-4
CHEMBL311854 104921 1 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00387-4
9895957 10558 12 None 3 3 Human 8.7 pKi = 8.7 Binding
Binding affinity at endothelin receptor subtype ABinding affinity at endothelin receptor subtype A
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1016/j.bmc.2012.06.011
CHEMBL11706 10558 12 None 3 3 Human 8.7 pKi = 8.7 Binding
Binding affinity at endothelin receptor subtype ABinding affinity at endothelin receptor subtype A
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1016/j.bmc.2012.06.011
44311728 103861 0 None -13 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 653 12 3 7 4.4 C=CS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL310039 103861 0 None -13 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 653 12 3 7 4.4 C=CS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
9895957 10558 12 None 3 3 Human 8.7 pKi = 8.7 Binding
Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1021/jm020138n
CHEMBL11706 10558 12 None 3 3 Human 8.7 pKi = 8.7 Binding
Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1021/jm020138n
9895957 10558 12 None 3 3 Human 8.7 pKi = 8.7 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1021/jm058225d
CHEMBL11706 10558 12 None 3 3 Human 8.7 pKi = 8.7 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1021/jm058225d
10555112 4654 0 None 12 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 572 14 2 8 4.6 COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)ccc1OCC(=O)O 10.1021/jm9910425
CHEMBL103695 4654 0 None 12 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 572 14 2 8 4.6 COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)ccc1OCC(=O)O 10.1021/jm9910425
11799974 4448 0 None 12 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 514 12 1 7 4.8 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL102307 4448 0 None 12 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 514 12 1 7 4.8 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
44311805 202850 0 None -26 2 Human 8.0 pKi = 8 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 669 12 3 7 4.7 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)C(C)C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL73000 202850 0 None -26 2 Human 8.0 pKi = 8 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 669 12 3 7 4.7 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)C(C)C)c1 10.1016/s0960-894x(98)00387-4
156690 140803 23 None - 1 Human 8.0 pKi = 8 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 536 8 1 7 5.8 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(C)(C)C)c1C 10.1021/jm058225d
CHEMBL383581 140803 23 None - 1 Human 8.0 pKi = 8 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 536 8 1 7 5.8 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(C)(C)C)c1C 10.1021/jm058225d
10812403 38848 0 None 120 2 Rat 7.0 pKi = 7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 7 2 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(N)=O)c1C 10.1021/jm970872k
CHEMBL146904 38848 0 None 120 2 Rat 7.0 pKi = 7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 7 2 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(N)=O)c1C 10.1021/jm970872k
10573784 164774 0 None 95 2 Rat 7.0 pKi = 7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 413 7 2 5 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CN)c1C 10.1021/jm970872k
CHEMBL423583 164774 0 None 95 2 Rat 7.0 pKi = 7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 413 7 2 5 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CN)c1C 10.1021/jm970872k
1481 2027 109 None -112 3 Human 5.0 pKi = 5 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1021/jm300682j
3749 2027 109 None -112 3 Human 5.0 pKi = 5 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1021/jm300682j
589 2027 109 None -112 3 Human 5.0 pKi = 5 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1021/jm300682j
6908 2027 109 None -112 3 Human 5.0 pKi = 5 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1021/jm300682j
CHEMBL1513 2027 109 None -112 3 Human 5.0 pKi = 5 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1021/jm300682j
DB01029 2027 109 None -112 3 Human 5.0 pKi = 5 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 10.1021/jm300682j
10619232 121468 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 371 5 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2N(C)C)c1C 10.1021/jm970872k
CHEMBL359332 121468 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 371 5 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2N(C)C)c1C 10.1021/jm970872k
44267891 18557 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 532 8 1 7 5.9 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
CHEMBL12779 18557 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 532 8 1 7 5.9 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
44333366 106929 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 570 12 1 8 5.2 COc1ccc(CCOC(c2ccc(C)cc2)(c2ccc(C)cc2)C(Oc2nc3c(c(OC)n2)COC3)C(=O)O)cc1 10.1021/jm9910425
CHEMBL318146 106929 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 570 12 1 8 5.2 COc1ccc(CCOC(c2ccc(C)cc2)(c2ccc(C)cc2)C(Oc2nc3c(c(OC)n2)COC3)C(=O)O)cc1 10.1021/jm9910425
10742005 201993 0 None 162 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(F)c2)c2cccc(F)c2)n1 10.1021/jm960274q
CHEMBL67536 201993 0 None 162 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(F)c2)c2cccc(F)c2)n1 10.1021/jm960274q
10740258 109177 0 None 1096 2 Human 8.0 pKi = 8.0 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1cnc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)o1 10.1021/jm000105c
CHEMBL322674 109177 0 None 1096 2 Human 8.0 pKi = 8.0 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1cnc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)o1 10.1021/jm000105c
10321341 144891 0 None 93 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 446 7 1 5 5.2 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm00037a003
CHEMBL39142 144891 0 None 93 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 446 7 1 5 5.2 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm00037a003
10598958 41178 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 434 6 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(S(=O)(=O)C(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL149050 41178 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 434 6 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(S(=O)(=O)C(C)C)cc2)c1C 10.1021/jm970872k
10715881 121014 0 None 37 2 Rat 7.0 pKi = 7.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 398 5 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL358545 121014 0 None 37 2 Rat 7.0 pKi = 7.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 398 5 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)(C)C)cc2)c1C 10.1021/jm970872k
9848710 168503 4 None -301 4 Pig 5.0 pKi = 5.0 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 497 9 3 3 4.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/0960-894X(96)00421-0
CHEMBL439759 168503 4 None -301 4 Pig 5.0 pKi = 5.0 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 497 9 3 3 4.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/0960-894X(96)00421-0
9848710 168503 4 None -301 4 Human 5.0 pKi = 5.0 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 497 9 3 3 4.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL439759 168503 4 None -301 4 Human 5.0 pKi = 5.0 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 497 9 3 3 4.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
10761748 120500 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 371 5 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(N(C)C)c2)c1C 10.1021/jm970872k
CHEMBL356591 120500 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 371 5 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(N(C)C)c2)c1C 10.1021/jm970872k
44286764 145276 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 314 3 1 1 4.7 O=C(O)[C@@H]1[C@@H](c2ccccc2)c2ccccc2[C@H]1c1ccccc1 10.1021/jm00037a003
CHEMBL39171 145276 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 314 3 1 1 4.7 O=C(O)[C@@H]1[C@@H](c2ccccc2)c2ccccc2[C@H]1c1ccccc1 10.1021/jm00037a003
10503999 41058 0 None 6 2 Rat 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 456 8 3 6 3.9 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL148953 41058 0 None 6 2 Rat 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 456 8 3 6 3.9 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10762600 167728 0 None 154 2 Rat 7.9 pKi = 7.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 6 1 4 5.0 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL434082 167728 0 None 154 2 Rat 7.9 pKi = 7.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 6 1 4 5.0 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10209324 14321 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 546 8 1 7 6.2 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
CHEMBL12013 14321 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 546 8 1 7 6.2 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
44311851 202947 0 None -162 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 564 10 3 5 4.9 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccon3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL73697 202947 0 None -162 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 564 10 3 5 4.9 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccon3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
10692125 201365 0 None 26 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 396 8 2 7 2.3 COc1cc(OC)nc(OC(C(=O)O)C(O)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL63648 201365 0 None 26 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 396 8 2 7 2.3 COc1cc(OC)nc(OC(C(=O)O)C(O)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
44314607 160702 0 None -1412 2 Pig 5.9 pKi = 5.9 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1534 46 19 18 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
77282208 160702 0 None -1412 2 Pig 5.9 pKi = 5.9 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1534 46 19 18 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL412003 160702 0 None -1412 2 Pig 5.9 pKi = 5.9 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1534 46 19 18 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
10620897 41360 0 None 14 2 Rat 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 398 6 1 4 5.3 Cc1cccc(-c2ccc(CC(C)C)cc2)c1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL149171 41360 0 None 14 2 Rat 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 398 6 1 4 5.3 Cc1cccc(-c2ccc(CC(C)C)cc2)c1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL4513786 212207 5 None -2344 8 Human 4.9 pKi = 4.9 Binding
Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000289bCl EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000289bCl EDNRA
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC nan
CHEMBL4796803 212207 5 None -2344 8 Human 4.9 pKi = 4.9 Binding
Affinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000289bCl EDNRAAffinity Biochemical interaction ([125I]-endothelin-1 saturation binding assay) EUB0000289bCl EDNRA
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC nan
5344 172891 98 None - 1 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C nan
CHEMBL453 172891 98 None - 1 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C nan
10740469 39053 0 None 154 2 Rat 7.9 pKi = 7.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 413 7 2 5 5.0 CNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL147081 39053 0 None 154 2 Rat 7.9 pKi = 7.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 413 7 2 5 5.0 CNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10668636 121445 0 None 147 2 Rat 7.9 pKi = 7.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccc(N)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL359167 121445 0 None 147 2 Rat 7.9 pKi = 7.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccc(N)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10166561 9954 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 562 9 2 8 5.4 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CO)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
CHEMBL11528 9954 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 562 9 2 8 5.4 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CO)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
10809354 120609 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 373 5 1 6 3.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2[N+](=O)[O-])c1C 10.1021/jm970872k
CHEMBL357580 120609 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 373 5 1 6 3.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2[N+](=O)[O-])c1C 10.1021/jm970872k
19934544 204469 0 None -2 2 Human 4.9 pKi = 4.9 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 482 7 3 4 4.9 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)Cc3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL86489 204469 0 None -2 2 Human 4.9 pKi = 4.9 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 482 7 3 4 4.9 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)Cc3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
44267862 15174 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 571 9 1 8 5.9 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CC#N)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
CHEMBL12144 15174 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 571 9 1 8 5.9 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CC#N)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
10453858 159543 0 None 31 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 404 4 2 5 4.1 COc1ccc([C@@H]2c3cc(O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm00037a003
CHEMBL41087 159543 0 None 31 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 404 4 2 5 4.1 COc1ccc([C@@H]2c3cc(O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm00037a003
10837085 101826 0 None 39 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2F)c2ccccc2F)n1 10.1021/jm960274q
CHEMBL303501 101826 0 None 39 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2F)c2ccccc2F)n1 10.1021/jm960274q
10670204 41278 0 None 17 2 Rat 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 428 7 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(=O)O)c1C 10.1021/jm970872k
CHEMBL149111 41278 0 None 17 2 Rat 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 428 7 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(=O)O)c1C 10.1021/jm970872k
10603135 109243 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 570 14 1 7 6.0 CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL322996 109243 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 570 14 1 7 6.0 CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
10521320 119247 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 343 4 2 5 3.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2N)c1C 10.1021/jm970872k
CHEMBL347958 119247 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 343 4 2 5 3.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2N)c1C 10.1021/jm970872k
10549727 164324 0 None 125 2 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 414 7 1 5 5.0 COc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
CHEMBL422128 164324 0 None 125 2 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 414 7 1 5 5.0 COc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
44267893 97952 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 535 10 2 7 4.9 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
CHEMBL275523 97952 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 535 10 2 7 4.9 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
10740953 5229 0 None 758 2 Human 7.8 pKi = 7.8 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 423 5 1 6 5.0 Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)oc1C 10.1021/jm000105c
CHEMBL106749 5229 0 None 758 2 Human 7.8 pKi = 7.8 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 423 5 1 6 5.0 Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)oc1C 10.1021/jm000105c
44274885 93639 0 None 29 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 454 10 1 7 4.5 COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(SC)cc2)c2ccccc2)n1 10.1021/jm030480f
CHEMBL24906 93639 0 None 29 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 454 10 1 7 4.5 COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(SC)cc2)c2ccccc2)n1 10.1021/jm030480f
44307287 202054 0 None 29 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 470 10 0 9 4.1 COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(SC)cc1)c1ccccc1 10.1021/jm960274q
CHEMBL67957 202054 0 None 29 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 470 10 0 9 4.1 COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(SC)cc1)c1ccccc1 10.1021/jm960274q
176 394 63 None -7 31 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -7 31 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -7 31 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -7 31 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -7 31 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
10620185 119133 0 None 89 2 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 386 6 1 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL346853 119133 0 None 89 2 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 386 6 1 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OC(C)C)cc2)c1C 10.1021/jm970872k
10741144 119251 0 None 407 2 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 8 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC=O)c1C 10.1021/jm970872k
CHEMBL347982 119251 0 None 407 2 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 8 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC=O)c1C 10.1021/jm970872k
17979733 96781 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 576 10 1 8 6.0 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(COC)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
CHEMBL268706 96781 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 576 10 1 8 6.0 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(COC)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
44303033 201518 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 472 6 1 5 5.4 COc1ccc(CC2C(c3ccc(Cl)c(Cl)c3)C(=O)O[C@@]2(O)c2ccc(OC)cc2)cc1 10.1021/jm990504b
CHEMBL64424 201518 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 472 6 1 5 5.4 COc1ccc(CC2C(c3ccc(Cl)c(Cl)c3)C(=O)O[C@@]2(O)c2ccc(OC)cc2)cc1 10.1021/jm990504b
9934204 106449 0 None -1 2 Human 4.8 pKi = 4.8 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 465 7 2 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL314915 106449 0 None -1 2 Human 4.8 pKi = 4.8 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 465 7 2 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
10836754 201887 0 None 14 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 438 11 1 7 3.7 CCOc1cc(OCC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL66893 201887 0 None 14 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 438 11 1 7 3.7 CCOc1cc(OCC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10691437 4998 0 None -1 4 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL105490 4998 0 None -1 4 Rat 7.8 pKi = 7.8 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
443289 702 40 None 2 3 Human 7.8 pKi = 7.8 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
997 702 40 None 2 3 Human 7.8 pKi = 7.8 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
CHEMBL314691 702 40 None 2 3 Human 7.8 pKi = 7.8 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
DB12054 702 40 None 2 3 Human 7.8 pKi = 7.8 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
10691437 4998 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm000105c
CHEMBL105490 4998 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm000105c
CHEMBL1201469 14326 0 None -1 4 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL None None None None nan
22103797 41122 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 408 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccn3C)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL149010 41122 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 408 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccn3C)cc2)c1C 10.1016/s0960-894x(01)00791-0
5122650 102445 6 None 100 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 364 7 1 5 3.2 COC(c1ccccc1)(c1ccccc1)C(Oc1nccc(C)n1)C(=O)O 10.1021/jm960274q
CHEMBL306218 102445 6 None 100 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 364 7 1 5 3.2 COC(c1ccccc1)(c1ccccc1)C(Oc1nccc(C)n1)C(=O)O 10.1021/jm960274q
11797288 201913 0 None 89 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 438 11 1 7 3.7 CCCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
CHEMBL67084 201913 0 None 89 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 438 11 1 7 3.7 CCCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
10669224 107967 0 None 1778 2 Human 7.7 pKi = 7.7 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 6 1 6 4.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cc3ncco3)cc2)c1C 10.1021/jm000105c
CHEMBL319924 107967 0 None 1778 2 Human 7.7 pKi = 7.7 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 6 1 6 4.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cc3ncco3)cc2)c1C 10.1021/jm000105c
10673091 162762 0 None 4 2 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 502 10 1 5 5.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(Cl)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL418992 162762 0 None 4 2 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 502 10 1 5 5.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(Cl)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
10836583 39440 0 None 43 2 Rat 6.7 pKi = 6.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 434 7 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCc3ccccc3)cc2)c1C 10.1021/jm970872k
CHEMBL147521 39440 0 None 43 2 Rat 6.7 pKi = 6.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 434 7 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCc3ccccc3)cc2)c1C 10.1021/jm970872k
10643748 120910 0 None 29 2 Rat 6.7 pKi = 6.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(CC(C)C)c2)c1C 10.1021/jm970872k
CHEMBL358226 120910 0 None 29 2 Rat 6.7 pKi = 6.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(CC(C)C)c2)c1C 10.1021/jm970872k
10813050 43788 0 None 602 2 Rat 8.7 pKi = 8.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 441 9 2 5 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CNC=O)c1C 10.1021/jm970872k
CHEMBL151440 43788 0 None 602 2 Rat 8.7 pKi = 8.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 441 9 2 5 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CNC=O)c1C 10.1021/jm970872k
9895957 10558 12 None 3 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1016/s0960-894x(03)00018-0
CHEMBL11706 10558 12 None 3 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 659 11 1 7 6.8 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CN2CCC(C)(C)C2=O)c1 10.1016/s0960-894x(03)00018-0
10835335 4753 0 None 50118 2 Human 8.7 pKi = 8.7 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1coc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1 10.1021/jm000105c
CHEMBL104223 4753 0 None 50118 2 Human 8.7 pKi = 8.7 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1coc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1 10.1021/jm000105c
11799973 4351 0 None 31 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 514 11 1 7 5.1 COc1ccc(COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL101587 4351 0 None 31 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 514 11 1 7 5.1 COc1ccc(COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
9893800 106733 10 None 2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting method
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/acs.jmedchem.5b01781
CHEMBL316735 106733 10 None 2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting method
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/acs.jmedchem.5b01781
9893800 106733 10 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL316735 106733 10 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
44311727 202754 0 None -9 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 669 13 3 7 4.7 CCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL72348 202754 0 None -9 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 669 13 3 7 4.7 CCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
76312118 84909 0 None 691 2 Human 8.7 pKi = 8.7 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261361 84909 0 None 691 2 Human 8.7 pKi = 8.7 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
18660521 41440 0 None 2754 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL149232 41440 0 None 2754 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
44311915 104299 0 None -6 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 703 12 3 7 5.4 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)c2ccccc2)c1 10.1016/s0960-894x(98)00387-4
CHEMBL310920 104299 0 None -6 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 703 12 3 7 5.4 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)c2ccccc2)c1 10.1016/s0960-894x(98)00387-4
10768897 107158 0 None 6 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 544 13 1 8 4.8 COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL319031 107158 0 None 6 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 544 13 1 8 4.8 COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL1790180 207130 0 None -72 3 Rat 8.6 pKi = 8.6 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat aortaCompound was evaluated for the binding affinity to Endothelin A receptor in the rat aorta
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
11049336 99465 0 None 3630 2 Human 8.6 pKi = 8.6 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 497 7 1 6 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C/c2ccccc2)c1C 10.1021/jm020289q
CHEMBL286279 99465 0 None 3630 2 Human 8.6 pKi = 8.6 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 497 7 1 6 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C/c2ccccc2)c1C 10.1021/jm020289q
10670965 42066 0 None 851 2 Rat 8.6 pKi = 8.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 444 9 2 6 4.3 Cc1noc(NS(=O)(=O)c2cccc(OCCO)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL149819 42066 0 None 851 2 Rat 8.6 pKi = 8.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 444 9 2 6 4.3 Cc1noc(NS(=O)(=O)c2cccc(OCCO)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
44311804 102531 0 None -12 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 683 14 3 7 5.1 CCCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL306950 102531 0 None -12 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 683 14 3 7 5.1 CCCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
10501931 43610 0 None 64 2 Rat 7.7 pKi = 7.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 414 7 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CO)c1C 10.1021/jm970872k
CHEMBL151160 43610 0 None 64 2 Rat 7.7 pKi = 7.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 414 7 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CO)c1C 10.1021/jm970872k
10668819 120588 0 None 602 2 Rat 7.7 pKi = 7.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 402 6 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2F)c1C 10.1021/jm970872k
CHEMBL357395 120588 0 None 602 2 Rat 7.7 pKi = 7.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 402 6 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2F)c1C 10.1021/jm970872k
22574798 15330 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 579 13 2 8 5.2 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCC)c1 10.1016/s0960-894x(03)00018-0
CHEMBL12175 15330 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 579 13 2 8 5.2 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCC)c1 10.1016/s0960-894x(03)00018-0
17979749 17650 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 550 8 1 7 6.0 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(F)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
CHEMBL12590 17650 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 550 8 1 7 6.0 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(F)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
44267860 166561 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 590 11 1 8 6.4 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(COCC)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
CHEMBL429037 166561 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 590 11 1 8 6.4 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(COCC)c1)C(=O)CCCC2 10.1016/s0960-894x(03)00018-0
10599129 101753 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 438 9 1 7 3.5 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(C)cc2)c2ccc(C)cc2)n1 10.1021/jm960274q
CHEMBL303034 101753 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 438 9 1 7 3.5 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(C)cc2)c2ccc(C)cc2)n1 10.1021/jm960274q
44314882 156622 0 None -380 2 Pig 5.7 pKi = 5.7 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1562 47 19 18 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
77282212 156622 0 None -380 2 Pig 5.7 pKi = 5.7 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1562 47 19 18 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL407559 156622 0 None -380 2 Pig 5.7 pKi = 5.7 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1562 47 19 18 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
10813228 107161 0 None 46 2 Human 5.7 pKi = 5.7 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 445 5 1 6 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nc4ccccc4o3)cc2)c1C 10.1021/jm000105c
CHEMBL319036 107161 0 None 46 2 Human 5.7 pKi = 5.7 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 445 5 1 6 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nc4ccccc4o3)cc2)c1C 10.1021/jm000105c
10545378 38964 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 344 5 1 5 3.9 Cc1noc(NS(=O)(=O)c2ccccc2Oc2ccccc2)c1C 10.1021/jm970872k
CHEMBL147007 38964 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 344 5 1 5 3.9 Cc1noc(NS(=O)(=O)c2ccccc2Oc2ccccc2)c1C 10.1021/jm970872k
20747573 16954 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 593 13 2 8 5.4 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCC)c1 10.1016/s0960-894x(03)00018-0
CHEMBL12557 16954 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 593 13 2 8 5.4 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCC)c1 10.1016/s0960-894x(03)00018-0
10719157 101812 0 None 58 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 470 11 1 9 2.9 COc1cccc(C(OC)(c2cccc(OC)c2)C(Oc2nc(OC)cc(OC)n2)C(=O)O)c1 10.1021/jm960274q
CHEMBL303390 101812 0 None 58 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 470 11 1 9 2.9 COc1cccc(C(OC)(c2cccc(OC)c2)C(Oc2nc(OC)cc(OC)n2)C(=O)O)c1 10.1021/jm960274q
19085508 39333 0 None 218 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 466 7 1 8 4.2 COc1cc(OC)nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1 10.1016/s0960-894x(01)00791-0
CHEMBL147365 39333 0 None 218 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 466 7 1 8 4.2 COc1cc(OC)nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1 10.1016/s0960-894x(01)00791-0
CHEMBL315927 209438 0 None - 1 Human 6.7 pKi = 6.7 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2cccc3ccccc23)NC1=O 10.1016/0960-894X(95)00019-P
10505434 4583 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 496 11 1 5 5.8 Cc1ccc(CCCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL103190 4583 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 496 11 1 5 5.8 Cc1ccc(CCCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
11801906 98063 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 612 13 1 8 6.2 COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1 10.1021/jm9910425
CHEMBL276288 98063 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 612 13 1 8 6.2 COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1 10.1021/jm9910425
44311698 202401 0 None -524 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 574 10 3 4 5.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccccn3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL70310 202401 0 None -524 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 574 10 3 4 5.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccccn3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
10670662 201747 0 None 53 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 438 9 1 7 3.5 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(C)c2)c2cccc(C)c2)n1 10.1021/jm960274q
CHEMBL65833 201747 0 None 53 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 438 9 1 7 3.5 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(C)c2)c2cccc(C)c2)n1 10.1021/jm960274q
CHEMBL87296 214108 0 None - 1 Human 5.6 pKi = 5.6 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1016/0960-894X(95)00019-P
10645256 40784 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 410 6 1 4 5.2 CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc3c2CCCC3)cc1 10.1021/jm970872k
CHEMBL148757 40784 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 410 6 1 4 5.2 CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc3c2CCCC3)cc1 10.1021/jm970872k
10552683 201412 0 None 5 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 478 9 1 7 4.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1 10.1021/jm960274q
CHEMBL64009 201412 0 None 5 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 478 9 1 7 4.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1 10.1021/jm960274q
18660522 119134 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccncn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL346862 119134 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccncn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
3921421 106802 8 None 9 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 468 10 1 5 5.1 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccccc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL317233 106802 8 None 9 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 468 10 1 5 5.1 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccccc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
44314832 160714 0 None -251 2 Pig 6.6 pKi = 6.6 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1496 45 18 17 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL412065 160714 0 None -251 2 Pig 6.6 pKi = 6.6 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1496 45 18 17 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
44274960 99089 0 None 12 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 450 10 1 6 4.9 COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(C(C)C)cc2)c2ccccc2)n1 10.1021/jm030480f
CHEMBL283637 99089 0 None 12 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
ChEMBL 450 10 1 6 4.9 COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(C(C)C)cc2)c2ccccc2)n1 10.1021/jm030480f
44311699 202459 0 None -331 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 563 10 3 4 5.5 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccco3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL70686 202459 0 None -331 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 563 10 3 4 5.5 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccco3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
44307412 201954 0 None 12 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 466 10 0 8 4.5 COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(C(C)C)cc1)c1ccccc1 10.1021/jm960274q
CHEMBL67325 201954 0 None 12 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 466 10 0 8 4.5 COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(C(C)C)cc1)c1ccccc1 10.1021/jm960274q
10721484 106864 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 554 13 1 6 6.3 CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL317716 106864 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 554 13 1 6 6.3 CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
10621777 42813 0 None 12 2 Rat 5.6 pKi = 5.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 415 7 1 6 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1[N+](=O)[O-] 10.1021/jm970872k
CHEMBL150481 42813 0 None 12 2 Rat 5.6 pKi = 5.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 415 7 1 6 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1[N+](=O)[O-] 10.1021/jm970872k
9797546 40636 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 329 4 1 5 3.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccnc2)c1C 10.1021/jm970872k
CHEMBL148637 40636 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 329 4 1 5 3.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccnc2)c1C 10.1021/jm970872k
22103537 41812 0 None 144 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccno3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL149592 41812 0 None 144 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccno3)cc2)c1C 10.1016/s0960-894x(01)00791-0
44312023 202749 0 None -22 2 Human 4.6 pKi = 4.6 Binding
Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
CHEMBL72295 202749 0 None -22 2 Human 4.6 pKi = 4.6 Binding
Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
10595347 42221 0 None 537 2 Rat 7.6 pKi = 7.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 370 6 1 4 4.7 CCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
CHEMBL149953 42221 0 None 537 2 Rat 7.6 pKi = 7.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 370 6 1 4 4.7 CCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
10741830 42582 0 None 3 2 Rat 5.6 pKi = 5.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 441 7 2 5 4.9 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1 10.1021/jm970872k
CHEMBL150269 42582 0 None 3 2 Rat 5.6 pKi = 5.6 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 441 7 2 5 4.9 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1 10.1021/jm970872k
15297287 163849 0 None -3 2 Human 4.6 pKi = 4.6 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 424 5 2 4 5.2 O=C(O)CN1C(=O)c2ccccc2Nc2ccc(OCc3cccc4ccccc34)cc21 10.1016/0960-894X(95)00019-P
CHEMBL421349 163849 0 None -3 2 Human 4.6 pKi = 4.6 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 424 5 2 4 5.2 O=C(O)CN1C(=O)c2ccccc2Nc2ccc(OCc3cccc4ccccc34)cc21 10.1016/0960-894X(95)00019-P
10599293 38774 0 None 128 2 Rat 7.5 pKi = 7.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 441 9 2 5 5.8 CCCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL146845 38774 0 None 128 2 Rat 7.5 pKi = 7.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 441 9 2 5 5.8 CCCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10508342 4647 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 638 13 1 8 6.3 COc1ccc(CCOC(c2ccc(Cl)cc2)(c2ccc(Cl)cc2)C(Oc2nc3c(c(OC)n2)CCC3)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL103605 4647 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 638 13 1 8 6.3 COc1ccc(CCOC(c2ccc(Cl)cc2)(c2ccc(Cl)cc2)C(Oc2nc3c(c(OC)n2)CCC3)C(=O)O)cc1OC 10.1021/jm9910425
44311849 102586 0 None -5 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 694 14 2 7 5.8 CCCCS(=O)(=O)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL307384 102586 0 None -5 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 694 14 2 7 5.8 CCCCS(=O)(=O)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
11800649 4526 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 542 13 1 7 5.5 CCOc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL102797 4526 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 542 13 1 7 5.5 CCOc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
19085510 119037 0 None 6025 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccnc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL345951 119037 0 None 6025 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccnc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
10528863 4537 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 484 10 2 6 4.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(O)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL102868 4537 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 484 10 2 6 4.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(O)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
6433100 4466 6 None 2 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL102405 4466 6 None 2 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
10548722 5391 0 None 20892 2 Human 8.4 pKi = 8.4 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnco3)cc2)c1C 10.1021/jm000105c
CHEMBL107574 5391 0 None 20892 2 Human 8.4 pKi = 8.4 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnco3)cc2)c1C 10.1021/jm000105c
44311726 102598 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 667 12 3 7 4.8 C/C=C/S(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL307471 102598 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 667 12 3 7 4.8 C/C=C/S(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
18660523 41567 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cncnc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL149340 41567 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cncnc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
10525034 119156 0 None 89 2 Rat 7.5 pKi = 7.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 400 7 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL347125 119156 0 None 89 2 Rat 7.5 pKi = 7.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 400 7 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCC(C)C)cc2)c1C 10.1021/jm970872k
10505357 108902 0 None 10 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 494 10 1 5 5.9 Cc1ccc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL321984 108902 0 None 10 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 494 10 1 5 5.9 Cc1ccc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
10624645 4252 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 482 10 1 5 5.4 Cc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL100954 4252 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 482 10 1 5 5.4 Cc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
10713411 164382 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 358 5 1 5 3.8 COc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
CHEMBL422496 164382 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 358 5 1 5 3.8 COc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
10671031 102208 0 None 29 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(F)cc2)c2ccc(F)cc2)n1 10.1021/jm960274q
CHEMBL304721 102208 0 None 29 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(F)cc2)c2ccc(F)cc2)n1 10.1021/jm960274q
10622410 43764 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 7 1 5 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N(C)C)c1C 10.1021/jm970872k
CHEMBL151395 43764 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 7 1 5 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N(C)C)c1C 10.1021/jm970872k
19934534 106200 0 None -5 2 Human 4.5 pKi = 4.5 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 468 6 3 4 5.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cc4ccccc4[nH]3)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL314364 106200 0 None -5 2 Human 4.5 pKi = 4.5 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 468 6 3 4 5.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cc4ccccc4[nH]3)ccc21 10.1016/0960-894X(95)00019-P
10741834 43778 0 None 85 2 Rat 7.5 pKi = 7.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 441 8 2 5 5.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC(C)C)c1C 10.1021/jm970872k
CHEMBL151422 43778 0 None 85 2 Rat 7.5 pKi = 7.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 441 8 2 5 5.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC(C)C)c1C 10.1021/jm970872k
9864017 41072 0 None 194 2 Human 6.5 pKi = 6.5 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 367 4 2 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2cc3ccccc3[nH]2)c1C 10.1021/jm970872k
CHEMBL148967 41072 0 None 194 2 Human 6.5 pKi = 6.5 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 367 4 2 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2cc3ccccc3[nH]2)c1C 10.1021/jm970872k
10743346 102125 0 None 4 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 480 11 1 7 4.7 COc1cc(OC)nc(OC(C(=O)O)C(OCCC(C)(C)C)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL304173 102125 0 None 4 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 480 11 1 7 4.7 COc1cc(OC)nc(OC(C(=O)O)C(OCCC(C)(C)C)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10709109 43864 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2ccccc2[N+](=O)[O-])c1C 10.1021/jm970872k
CHEMBL151545 43864 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2ccccc2[N+](=O)[O-])c1C 10.1021/jm970872k
10691438 44226 0 None 51 2 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 7 1 4 5.1 CCCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
CHEMBL151926 44226 0 None 51 2 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 7 1 4 5.1 CCCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
44213540 39229 0 None 831 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 421 5 1 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccc[n+]3[O-])cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL147238 39229 0 None 831 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 421 5 1 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccc[n+]3[O-])cc2)c1C 10.1016/s0960-894x(01)00791-0
10693130 121442 0 None 16 2 Rat 6.4 pKi = 6.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 414 7 1 5 5.0 COc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1 10.1021/jm970872k
CHEMBL359152 121442 0 None 16 2 Rat 6.4 pKi = 6.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 414 7 1 5 5.0 COc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1 10.1021/jm970872k
44365561 42010 0 None 524 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 404 5 1 4 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL149763 42010 0 None 524 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 404 5 1 4 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
44365878 42026 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 396 5 2 7 2.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nn[nH]n3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL149778 42026 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 396 5 2 7 2.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nn[nH]n3)cc2)c1C 10.1016/s0960-894x(01)00791-0
10501299 119336 0 None 147 2 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 402 6 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(SC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL348685 119336 0 None 147 2 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 402 6 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(SC(C)C)cc2)c1C 10.1021/jm970872k
11813485 17890 0 None -8 2 Human 7.4 pKi = 7.4 Binding
Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor
ChEMBL 534 9 1 6 6.0 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm020138n
CHEMBL126755 17890 0 None -8 2 Human 7.4 pKi = 7.4 Binding
Compound was evaluated for its binding affinity towards human Endothelin A receptorCompound was evaluated for its binding affinity towards human Endothelin A receptor
ChEMBL 534 9 1 6 6.0 CCCCC1=NC2(CCCC2)C(=O)N1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm020138n
10769887 106993 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 600 15 1 8 6.0 CCc1ccc(C(OCCc2ccc(OC)c(OC)c2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL318535 106993 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 600 15 1 8 6.0 CCc1ccc(C(OCCc2ccc(OC)c(OC)c2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
10526510 120542 0 None 12 2 Rat 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 8 1 6 4.2 COc1cc(OC)nc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)n1 10.1021/jm970872k
CHEMBL356972 120542 0 None 12 2 Rat 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 8 1 6 4.2 COc1cc(OC)nc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)n1 10.1021/jm970872k
22103385 120559 0 None 19054 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 396 5 1 7 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nnco3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL357077 120559 0 None 19054 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 396 5 1 7 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nnco3)cc2)c1C 10.1016/s0960-894x(01)00791-0
20747574 11986 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 565 12 2 8 4.8 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1 10.1016/s0960-894x(03)00018-0
CHEMBL11840 11986 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 565 12 2 8 4.8 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1 10.1016/s0960-894x(03)00018-0
9807200 84907 0 None 346 2 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261359 84907 0 None 346 2 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
9908909 5222 7 None -1 3 Rat 8.3 pKi = 8.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C 10.1021/jm970872k
CHEMBL106684 5222 7 None -1 3 Rat 8.3 pKi = 8.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C 10.1021/jm970872k
10811477 4735 0 None 19952 2 Human 8.3 pKi = 8.3 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncoc3C)cc2)c1C 10.1021/jm000105c
CHEMBL104172 4735 0 None 19952 2 Human 8.3 pKi = 8.3 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncoc3C)cc2)c1C 10.1021/jm000105c
9908909 5222 7 None 1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C 10.1021/jm000105c
CHEMBL106684 5222 7 None 1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C 10.1021/jm000105c
443289 702 40 None -2 3 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL None None None None 10.1021/jm970872k
997 702 40 None -2 3 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL None None None None 10.1021/jm970872k
CHEMBL314691 702 40 None -2 3 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL None None None None 10.1021/jm970872k
DB12054 702 40 None -2 3 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL None None None None 10.1021/jm970872k
9950670 43295 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 358 5 2 5 3.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2CO)c1C 10.1021/jm970872k
CHEMBL150891 43295 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 358 5 2 5 3.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2CO)c1C 10.1021/jm970872k
18004820 16261 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 527 9 2 7 4.7 CCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
CHEMBL12333 16261 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 527 9 2 7 4.7 CCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
10208527 97731 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 526 9 1 7 5.8 CCCc1nc(Cl)c(C(C)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
CHEMBL274154 97731 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 526 9 1 7 5.8 CCCc1nc(Cl)c(C(C)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
11795351 42588 0 None 109 2 Rat 6.4 pKi = 6.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 401 6 1 4 4.8 CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2ccc(Cl)nn2)cc1 10.1021/jm970872k
CHEMBL150273 42588 0 None 109 2 Rat 6.4 pKi = 6.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 401 6 1 4 4.8 CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2ccc(Cl)nn2)cc1 10.1021/jm970872k
44303148 201458 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 456 4 1 5 5.1 O=C1O[C@@](O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)C1c1ccc2c(c1)OCO2 10.1021/jm990504b
CHEMBL64200 201458 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 456 4 1 5 5.1 O=C1O[C@@](O)(c2ccc(Cl)c(Cl)c2)C(Cc2ccccc2)C1c1ccc2c(c1)OCO2 10.1021/jm990504b
19934549 105500 0 None -3 2 Human 4.4 pKi = 4.4 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 439 6 2 3 5.4 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(Cc3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL313184 105500 0 None -3 2 Human 4.4 pKi = 4.4 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 439 6 2 3 5.4 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(Cc3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
10280531 162369 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 541 10 2 7 5.1 CCCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
CHEMBL417429 162369 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 541 10 2 7 5.1 CCCCc1nc(Cl)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
10528341 14393 0 None 95 2 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 458 9 2 6 4.4 Cc1noc(NS(=O)(=O)c2cccc(OCC(=O)O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL1204523 14393 0 None 95 2 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 458 9 2 6 4.4 Cc1noc(NS(=O)(=O)c2cccc(OCC(=O)O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL149152 14393 0 None 95 2 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 458 9 2 6 4.4 Cc1noc(NS(=O)(=O)c2cccc(OCC(=O)O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
155543936 172654 0 None -218776 2 Rat 5.4 pKi = 5.4 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL 2514 48 34 38 -9.8 CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00087a001
CHEMBL4524100 172654 0 None -218776 2 Rat 5.4 pKi = 5.4 Binding
Compound was evaluated for the binding affinity to Endothelin A receptor in the rat atriumCompound was evaluated for the binding affinity to Endothelin A receptor in the rat atrium
ChEMBL 2514 48 34 38 -9.8 CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00087a001
10407051 99914 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 374 5 1 3 4.7 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc(OC)cc3)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
CHEMBL290026 99914 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 374 5 1 3 4.7 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc(OC)cc3)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
10647471 42065 0 None 125 2 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 456 7 3 5 4.7 CNC(=O)Nc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL149818 42065 0 None 125 2 Rat 7.4 pKi = 7.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 456 7 3 5 4.7 CNC(=O)Nc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10045790 141108 0 None 17 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 388 4 1 4 4.4 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc4c(c3)OCO4)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
CHEMBL38537 141108 0 None 17 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]ET1 binding to cloned human ET-A receptorInhibition of [125I]ET1 binding to cloned human ET-A receptor
ChEMBL 388 4 1 4 4.4 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc4c(c3)OCO4)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
22103589 40920 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 394 5 2 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncc[nH]3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL148855 40920 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 394 5 2 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncc[nH]3)cc2)c1C 10.1016/s0960-894x(01)00791-0
3887 2033 39 None -436 4 Pig 6.4 pKi = 6.4 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL None None None None 10.1016/0960-894X(96)00421-0
5311192 2033 39 None -436 4 Pig 6.4 pKi = 6.4 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL None None None None 10.1016/0960-894X(96)00421-0
CHEMBL72410 2033 39 None -436 4 Pig 6.4 pKi = 6.4 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL None None None None 10.1016/0960-894X(96)00421-0
3887 2033 39 None -436 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00387-4
5311192 2033 39 None -436 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00387-4
CHEMBL72410 2033 39 None -436 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00387-4
10499516 120452 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 372 5 2 5 3.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(=O)O)cc2)c1C 10.1021/jm970872k
CHEMBL356220 120452 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 372 5 2 5 3.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(=O)O)cc2)c1C 10.1021/jm970872k
44311701 167582 1 None -213 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 564 10 3 5 4.9 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL433106 167582 1 None -213 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 564 10 3 5 4.9 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
10280562 15325 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 542 9 1 8 5.4 CCCc1nc(Cl)c(C(=O)OC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
CHEMBL12172 15325 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 542 9 1 8 5.4 CCCc1nc(Cl)c(C(=O)OC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
10516176 203479 3 None - 1 Rat 5.3 pKi = 5.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccccc2F)c1C 10.1021/jm970872k
CHEMBL78499 203479 3 None - 1 Rat 5.3 pKi = 5.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccccc2F)c1C 10.1021/jm970872k
10793160 97941 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 570 13 1 8 5.6 COc1cc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC 10.1021/jm9910425
CHEMBL275471 97941 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 570 13 1 8 5.6 COc1cc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC 10.1021/jm9910425
122272 96637 23 None 1 2 Human 7.3 pKi = 7.3 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm9505369
CHEMBL267458 96637 23 None 1 2 Human 7.3 pKi = 7.3 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm9505369
122272 96637 23 None 1 2 Human 7.3 pKi = 7.3 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm980217s
CHEMBL267458 96637 23 None 1 2 Human 7.3 pKi = 7.3 Binding
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]-ET-1 from chinese hamster ovary cells(CHO)
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm980217s
10810897 120966 0 None 3801 2 Rat 8.3 pKi = 8.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 398 6 1 4 5.3 Cc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL358254 120966 0 None 3801 2 Rat 8.3 pKi = 8.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 398 6 1 4 5.3 Cc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10621010 164299 0 None 186 2 Rat 8.3 pKi = 8.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cccc(O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL421955 164299 0 None 186 2 Rat 8.3 pKi = 8.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cccc(O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
9871837 15019 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 535 10 2 7 4.9 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1016/s0960-894x(03)00018-0
CHEMBL12106 15019 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 535 10 2 7 4.9 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1016/s0960-894x(03)00018-0
9985001 96548 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 549 10 2 7 5.2 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1016/s0960-894x(03)00018-0
CHEMBL266628 96548 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 549 10 2 7 5.2 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1016/s0960-894x(03)00018-0
44311772 102546 0 None -10 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 628 15 2 8 4.1 CCCCS(=O)(=O)NC(=O)C(CCSC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL307045 102546 0 None -10 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 628 15 2 8 4.1 CCCCS(=O)(=O)NC(=O)C(CCSC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311838 202902 0 None -13 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 655 12 3 7 4.3 CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL73373 202902 0 None -13 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 655 12 3 7 4.3 CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311850 102703 0 None -10 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 717 13 3 7 5.5 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)Cc2ccccc2)c1 10.1016/s0960-894x(98)00387-4
CHEMBL308269 102703 0 None -10 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 717 13 3 7 5.5 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)Cc2ccccc2)c1 10.1016/s0960-894x(98)00387-4
44311773 202962 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 582 13 2 7 3.8 CCCCS(=O)(=O)NC(=O)C(CC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL73835 202962 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 582 13 2 7 3.8 CCCCS(=O)(=O)NC(=O)C(CC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
22103743 42575 0 None 9332 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 411 5 1 6 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccs3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL150260 42575 0 None 9332 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 411 5 1 6 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccs3)cc2)c1C 10.1016/s0960-894x(01)00791-0
10667808 118773 0 None 338 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 385 6 2 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(NC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL343867 118773 0 None 338 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 385 6 2 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(NC(C)C)cc2)c1C 10.1021/jm970872k
10761688 119337 0 None 380 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 370 5 1 4 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL348700 119337 0 None 380 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 370 5 1 4 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)C)cc2)c1C 10.1021/jm970872k
10501166 41619 0 None 47 2 Rat 6.3 pKi = 6.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cc(O)ccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL149391 41619 0 None 47 2 Rat 6.3 pKi = 6.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cc(O)ccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
44314444 161161 0 None -457 2 Pig 5.3 pKi = 5.3 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1470 45 18 17 -0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL413604 161161 0 None -457 2 Pig 5.3 pKi = 5.3 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1470 45 18 17 -0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
9799352 120581 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 367 4 2 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2c[nH]c3ccccc23)c1C 10.1021/jm970872k
CHEMBL357331 120581 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 367 4 2 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2c[nH]c3ccccc23)c1C 10.1021/jm970872k
10690608 120533 0 None 112 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 371 5 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL356901 120533 0 None 112 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 371 5 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C)cc2)c1C 10.1021/jm970872k
44311700 102336 0 None -234 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 579 10 3 4 6.0 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL305462 102336 0 None -234 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 579 10 3 4 6.0 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
122272 96637 23 None -1 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm970872k
CHEMBL267458 96637 23 None -1 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm970872k
10521258 120770 0 None 416 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 342 4 1 4 4.1 Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
CHEMBL358020 120770 0 None 416 2 Rat 7.3 pKi = 7.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 342 4 1 4 4.1 Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
122272 96637 23 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards ET1 receptor was determined in A10 cellsBinding affinity towards ET1 receptor was determined in A10 cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00029a001
CHEMBL267458 96637 23 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards ET1 receptor was determined in A10 cellsBinding affinity towards ET1 receptor was determined in A10 cells
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm00029a001
10166104 14993 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 549 10 1 7 5.2 CCCc1nc(CC)c(C(=O)N(C)C)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
CHEMBL12102 14993 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 549 10 1 7 5.2 CCCc1nc(CC)c(C(=O)N(C)C)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
17979745 17722 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 521 10 2 7 4.6 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
CHEMBL12592 17722 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 521 10 2 7 4.6 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/s0960-894x(03)00018-0
122272 96637 23 None 1 2 Human 7.3 pKi = 7.3 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm000105c
CHEMBL267458 96637 23 None 1 2 Human 7.3 pKi = 7.3 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1021/jm000105c
10718666 120994 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 457 9 3 6 4.5 Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL358461 120994 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 457 9 3 6 4.5 Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10670536 120561 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 435 6 1 6 3.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(S(=O)(=O)N(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL357099 120561 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 435 6 1 6 3.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(S(=O)(=O)N(C)C)cc2)c1C 10.1021/jm970872k
10088869 143812 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [125I]ET1 binding to cloned human Endothelin A receptorInhibition of [125I]ET1 binding to cloned human Endothelin A receptor
ChEMBL 344 4 1 2 4.7 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccccc3)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
CHEMBL39057 143812 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [125I]ET1 binding to cloned human Endothelin A receptorInhibition of [125I]ET1 binding to cloned human Endothelin A receptor
ChEMBL 344 4 1 2 4.7 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccccc3)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
10839202 118718 0 None 6 2 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 503 8 2 5 6.2 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL343477 118718 0 None 6 2 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 503 8 2 5 6.2 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10563752 40712 2 None - 1 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccccc2N)c1C 10.1021/jm970872k
CHEMBL148702 40712 2 None - 1 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccccc2N)c1C 10.1021/jm970872k
9953358 94346 9 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Endothelin A receptor; orally active in vivo at 30 mg/kg, poBinding affinity against human Endothelin A receptor; orally active in vivo at 30 mg/kg, po
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm030480f
CHEMBL25344 94346 9 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Endothelin A receptor; orally active in vivo at 30 mg/kg, poBinding affinity against human Endothelin A receptor; orally active in vivo at 30 mg/kg, po
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm030480f
44311803 202838 0 None -26 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 699 15 3 8 4.3 CCOCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL72924 202838 0 None -26 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 699 15 3 8 4.3 CCOCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
177236 1293 39 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1021/jm030528p
3508 1293 39 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1021/jm030528p
CHEMBL23261 1293 39 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1021/jm030528p
DB04883 1293 39 None -2 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1021/jm030528p
9953358 94346 9 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL25344 94346 9 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
177236 1293 39 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
3508 1293 39 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
CHEMBL23261 1293 39 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
DB04883 1293 39 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
11006149 100616 0 None 380 2 Human 8.2 pKi = 8.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 550 8 1 7 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)(C)C)C(C)C)c1C 10.1021/jm020289q
CHEMBL29502 100616 0 None 380 2 Human 8.2 pKi = 8.2 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 550 8 1 7 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)(C)C)C(C)C)c1C 10.1021/jm020289q
10648996 4273 0 None 3 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 498 11 1 6 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL101069 4273 0 None 3 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cellsInhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells
ChEMBL 498 11 1 6 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
18660520 39311 0 None 3548 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL147340 39311 0 None 3548 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
10741151 42806 0 None 223 2 Rat 8.2 pKi = 8.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 8 2 5 5.4 CCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL150474 42806 0 None 223 2 Rat 8.2 pKi = 8.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 427 8 2 5 5.4 CCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10503421 118991 0 None 245 2 Rat 8.2 pKi = 8.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 443 9 3 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCCO)c1C 10.1021/jm970872k
CHEMBL345542 118991 0 None 245 2 Rat 8.2 pKi = 8.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 443 9 3 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCCO)c1C 10.1021/jm970872k
104865 697 94 None 1 4 Human 8.2 pKi = 8.2 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
3494 697 94 None 1 4 Human 8.2 pKi = 8.2 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
392 697 94 None 1 4 Human 8.2 pKi = 8.2 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
CHEMBL957 697 94 None 1 4 Human 8.2 pKi = 8.2 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
DB00559 697 94 None 1 4 Human 8.2 pKi = 8.2 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
104865 697 94 None -1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm030528p
3494 697 94 None -1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm030528p
392 697 94 None -1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm030528p
CHEMBL957 697 94 None -1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm030528p
DB00559 697 94 None -1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm030528p
44265871 166354 0 None 53 2 Human 8.2 pKi = 8.2 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 547 10 2 8 4.6 COc1ccccc1Cc1c(CCCO)nc(-c2ncccn2)nc1NS(=O)(=O)c1ccc(C(C)(C)C)cc1 10.1021/jm9505369
CHEMBL428661 166354 0 None 53 2 Human 8.2 pKi = 8.2 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 547 10 2 8 4.6 COc1ccccc1Cc1c(CCCO)nc(-c2ncccn2)nc1NS(=O)(=O)c1ccc(C(C)(C)C)cc1 10.1021/jm9505369
22103787 40736 0 None 1380 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 394 5 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-n3cccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL148719 40736 0 None 1380 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.Binding affinity to CHO cells stably expressing human Endothelin A receptor.
ChEMBL 394 5 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-n3cccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
44311989 202855 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 610 14 2 7 4.4 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)CC 10.1016/s0960-894x(98)00387-4
CHEMBL73042 202855 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 610 14 2 7 4.4 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)CC 10.1016/s0960-894x(98)00387-4
10620958 41452 0 None 331 2 Rat 7.2 pKi = 7.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 399 6 1 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL149241 41452 0 None 331 2 Rat 7.2 pKi = 7.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 399 6 1 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C(C)C)cc2)c1C 10.1021/jm970872k
10803738 118470 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 294 4 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccccc2C(C)C)c1C 10.1021/jm970872k
CHEMBL342498 118470 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 294 4 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccccc2C(C)C)c1C 10.1021/jm970872k
5472495 186041 41 None - 1 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 372 4 1 3 4.0 CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1 nan
CHEMBL488025 186041 41 None - 1 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
ChEMBL 372 4 1 3 4.0 CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1 nan
10691439 44277 0 None 245 2 Rat 7.2 pKi = 7.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 4 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL151971 44277 0 None 245 2 Rat 7.2 pKi = 7.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 384 4 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)(C)C)cc2)c1C 10.1021/jm970872k
10783588 165119 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 343 4 2 5 3.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(N)c2)c1C 10.1021/jm970872k
CHEMBL424504 165119 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 343 4 2 5 3.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(N)c2)c1C 10.1021/jm970872k
44314783 165885 0 None -7943 2 Pig 6.2 pKi = 6.2 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1576 47 19 18 0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
77282213 165885 0 None -7943 2 Pig 6.2 pKi = 6.2 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1576 47 19 18 0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL427778 165885 0 None -7943 2 Pig 6.2 pKi = 6.2 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1576 47 19 18 0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
5310990 166266 9 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL428504 166266 9 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10600059 44253 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 460 8 1 4 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1Cc1ccccc1 10.1021/jm970872k
CHEMBL151954 44253 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 460 8 1 4 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1Cc1ccccc1 10.1021/jm970872k
9830098 102543 0 None -5 2 Human 5.2 pKi = 5.2 Binding
Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
CHEMBL307033 102543 0 None -5 2 Human 5.2 pKi = 5.2 Binding
Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
22574723 15747 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 549 11 2 7 5.2 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CC)c1 10.1016/s0960-894x(03)00018-0
CHEMBL12233 15747 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 549 11 2 7 5.2 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(CC)c1 10.1016/s0960-894x(03)00018-0
20747575 97959 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 579 12 2 8 5.0 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1 10.1016/s0960-894x(03)00018-0
CHEMBL275545 97959 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 579 12 2 8 5.0 CCCc1nc(CC)c(C(=O)NC)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COC)c1 10.1016/s0960-894x(03)00018-0
10693607 102220 0 None 354 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 424 10 1 7 3.3 CCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
CHEMBL304778 102220 0 None 354 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 424 10 1 7 3.3 CCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
10549472 5250 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)co1 10.1021/jm000105c
CHEMBL106846 5250 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of Human Endothelin A receptor expressed in CHO Cells.Inhibition of Human Endothelin A receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)co1 10.1021/jm000105c
10734431 43070 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 320 3 1 4 3.1 Cc1noc(NS(=O)(=O)c2ccccc2C(F)(F)F)c1C 10.1021/jm970872k
CHEMBL150697 43070 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 320 3 1 4 3.1 Cc1noc(NS(=O)(=O)c2ccccc2C(F)(F)F)c1C 10.1021/jm970872k
20747572 16285 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 555 10 2 7 5.3 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(Cl)c1 10.1016/s0960-894x(03)00018-0
CHEMBL12348 16285 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 555 10 2 7 5.3 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(Cl)c1 10.1016/s0960-894x(03)00018-0
19934546 204482 0 None 8 2 Human 5.2 pKi = 5.2 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 466 7 1 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(OCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL86581 204482 0 None 8 2 Human 5.2 pKi = 5.2 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 466 7 1 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(OCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
10718053 43848 0 None 5 2 Rat 5.1 pKi = 5.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 442 8 1 6 4.8 CCOC(=O)c1c(C)noc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
CHEMBL151525 43848 0 None 5 2 Rat 5.1 pKi = 5.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 442 8 1 6 4.8 CCOC(=O)c1c(C)noc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
10597897 40919 0 None 724 2 Rat 7.1 pKi = 7.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 414 7 1 5 5.0 COc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL148853 40919 0 None 724 2 Rat 7.1 pKi = 7.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 414 7 1 5 5.0 COc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10668703 164620 0 None 1230 2 Rat 8.1 pKi = 8.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2O)c1C 10.1021/jm970872k
CHEMBL422851 164620 0 None 1230 2 Rat 8.1 pKi = 8.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2O)c1C 10.1021/jm970872k
44311763 202734 0 None -6 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 610 14 2 7 4.4 CCCCS(=O)(=O)NC(=O)C(CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL72217 202734 0 None -6 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 610 14 2 7 4.4 CCCCS(=O)(=O)NC(=O)C(CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
22574645 17596 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 597 14 2 8 5.1 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCCF)c1 10.1016/s0960-894x(03)00018-0
CHEMBL12588 17596 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
ChEMBL 597 14 2 8 5.1 CCCc1nc(CC)c(C(N)=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)c(COCCF)c1 10.1016/s0960-894x(03)00018-0
104865 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
3494 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
392 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
CHEMBL957 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
DB00559 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
11071062 98797 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 494 9 1 7 5.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(C)C)c1C 10.1021/jm020289q
CHEMBL281869 98797 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibitory activity against human endothelin A receptor expressed in CHO cellsInhibitory activity against human endothelin A receptor expressed in CHO cells
ChEMBL 494 9 1 7 5.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(C)C)c1C 10.1021/jm020289q
44311873 202755 0 None -2 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 636 13 2 7 5.0 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C1CCCCC1 10.1016/s0960-894x(98)00387-4
CHEMBL72358 202755 0 None -2 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 636 13 2 7 5.0 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C1CCCCC1 10.1016/s0960-894x(98)00387-4
10548904 118992 0 None 380 2 Rat 7.1 pKi = 7.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 398 7 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CCC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL345551 118992 0 None 380 2 Rat 7.1 pKi = 7.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 398 7 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CCC(C)C)cc2)c1C 10.1021/jm970872k
10711546 203755 6 None - 1 Rat 5.1 pKi = 5.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle (Endothelin A receptor) was determined by radioligand binding assayAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle (Endothelin A receptor) was determined by radioligand binding assay
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2ccccc2Br)c1C 10.1021/jm970872k
CHEMBL80506 203755 6 None - 1 Rat 5.1 pKi = 5.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle (Endothelin A receptor) was determined by radioligand binding assayAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle (Endothelin A receptor) was determined by radioligand binding assay
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2ccccc2Br)c1C 10.1021/jm970872k
19934535 106479 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 468 6 3 4 5.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL315096 106479 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 468 6 3 4 5.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
104865 697 94 None 1 4 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
3494 697 94 None 1 4 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
392 697 94 None 1 4 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
CHEMBL957 697 94 None 1 4 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
DB00559 697 94 None 1 4 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cellsAbility to inhibit [125I]ET1 binding to human cloned endothelin A receptor expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
9949368 41130 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 329 4 1 5 3.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccn2)c1C 10.1021/jm970872k
CHEMBL149018 41130 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 329 4 1 5 3.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccn2)c1C 10.1021/jm970872k
44320537 106654 0 None - 1 Human 4.1 pKi = 4.1 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 479 6 2 4 5.7 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL316247 106654 0 None - 1 Human 4.1 pKi = 4.1 Binding
Affinity against ET A receptorAffinity against ET A receptor
ChEMBL 479 6 2 4 5.7 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
44311810 104298 0 None -35 2 Human 6.1 pKi = 6.1 Binding
Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
CHEMBL310919 104298 0 None -35 2 Human 6.1 pKi = 6.1 Binding
Compound was tested for the binding affinity against Endothelin A receptorCompound was tested for the binding affinity against Endothelin A receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
10814297 201826 0 None 17 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 472 10 1 7 4.3 COc1cc(OC)nc(OC(C(=O)O)C(Oc2ccccc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL66402 201826 0 None 17 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cellsBinding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
ChEMBL 472 10 1 7 4.3 COc1cc(OC)nc(OC(C(=O)O)C(Oc2ccccc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
44311852 102597 0 None -144 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 579 10 3 4 6.0 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3cccs3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL307470 102597 0 None -144 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 579 10 3 4 6.0 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3cccs3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
9818889 120618 0 None - 1 Human 5.1 pKi = 5.1 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 330 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ncccn2)c1C 10.1021/jm970872k
CHEMBL357678 120618 0 None - 1 Human 5.1 pKi = 5.1 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 330 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ncccn2)c1C 10.1021/jm970872k
10742502 120741 0 None 134 2 Rat 7.1 pKi = 7.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 457 9 3 6 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCC(=O)O)c1C 10.1021/jm970872k
CHEMBL357823 120741 0 None 134 2 Rat 7.1 pKi = 7.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 457 9 3 6 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCC(=O)O)c1C 10.1021/jm970872k
44311858 96142 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 598 13 3 8 2.8 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)O 10.1016/s0960-894x(98)00387-4
CHEMBL263301 96142 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to Endothelin A receptorBinding affinity to Endothelin A receptor
ChEMBL 598 13 3 8 2.8 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)O 10.1016/s0960-894x(98)00387-4
10257882 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 10.1021/jm300682j
8448 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 10.1021/jm300682j
CHEMBL539423 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 10.1021/jm300682j
DB12548 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
ChEMBL 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 10.1021/jm300682j
10257882 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 10.1021/jm058225d
8448 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 10.1021/jm058225d
CHEMBL539423 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 10.1021/jm058225d
DB12548 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
ChEMBL 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 10.1021/jm058225d
9840391 104047 6 None - 1 Rat 7.1 pKi = 7.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C 10.1021/jm970872k
CHEMBL310427 104047 6 None - 1 Rat 7.1 pKi = 7.1 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C 10.1021/jm970872k
9840650 44104 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 334 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccsc2)c1C 10.1021/jm970872k
CHEMBL151819 44104 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 334 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccsc2)c1C 10.1021/jm970872k
9927658 120693 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 334 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccs2)c1C 10.1021/jm970872k
CHEMBL357789 120693 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.Ability to inhibit Endothelin A receptor induced contractions in rabbit carotid artery rings (ETA) was determined in an in vitro functional assay.
ChEMBL 334 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccs2)c1C 10.1021/jm970872k
44314820 155168 0 None -380 2 Pig 7.0 pKi = 7.0 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1518 45 18 17 1.0 CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
77282210 155168 0 None -380 2 Pig 7.0 pKi = 7.0 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1518 45 18 17 1.0 CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL405377 155168 0 None -380 2 Pig 7.0 pKi = 7.0 Binding
Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated
ChEMBL 1518 45 18 17 1.0 CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
10737908 41195 0 None 102 2 Rat 6.0 pKi = 6.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 370 6 1 4 4.6 Cc1cnoc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
CHEMBL149060 41195 0 None 102 2 Rat 6.0 pKi = 6.0 Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptorAbility to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL 370 6 1 4 4.6 Cc1cnoc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
5340 168154 104 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
Drug Central 255 3 2 5 1.5 Nc1ccc(S(=O)(=O)Nc2nccs2)cc1 None
CHEMBL437 168154 104 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
Drug Central 255 3 2 5 1.5 Nc1ccc(S(=O)(=O)Nc2nccs2)cc1 None
5329 168898 114 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
Drug Central 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1 None
CHEMBL443 168898 114 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
Drug Central 253 3 2 5 1.4 Cc1cc(NS(=O)(=O)c2ccc(N)cc2)no1 None
5344 172891 98 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
CHEMBL453 172891 98 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
6662 216009 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
Drug Central 309 3 1 6 1.6 CC(=O)N(C1=C(C)C(C)=NO1)S(=O)(=O)C1=CC=C(N)C=C1 None
104865 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3494 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
392 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
CHEMBL957 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
DB00559 697 94 None - 4 Pig 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
16004692 2411 85 None - 0 Human 8.0 pIC50 = 8.0 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
4809 2411 85 None - 0 Human 8.0 pIC50 = 8.0 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
7352 2411 85 None - 0 Human 8.0 pIC50 = 8.0 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
CHEMBL2103873 2411 85 None - 0 Human 8.0 pIC50 = 8.0 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
DB08932 2411 85 None - 0 Human 8.0 pIC50 = 8.0 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETAIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETA
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
10605470 2971 0 None - 1 Human 9.0 pKd = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 823 17 3 10 6.2 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)O)/Cc1cc(OCCCC(=O)NCCc2ccc(c(c2)I)O)c(c(c1)OC)OC 9489609
3519 2971 0 None - 1 Human 9.0 pKd = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 823 17 3 10 6.2 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)O)/Cc1cc(OCCCC(=O)NCCc2ccc(c(c2)I)O)c(c(c1)OC)OC 9489609
CHEMBL2068816 2971 0 None - 1 Human 9.0 pKd = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 823 17 3 10 6.2 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)O)/Cc1cc(OCCCC(=O)NCCc2ccc(c(c2)I)O)c(c(c1)OC)OC 9489609
23670447 2968 2 None 114 2 Human 9.4 pKd = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 9023329
999 2968 2 None 114 2 Human 9.4 pKd = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 9023329
CHEMBL1204799 2968 2 None 114 2 Human 9.4 pKd = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 9023329
CHEMBL25438 2968 2 None 114 2 Human 9.4 pKd = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 9023329
186002 102356 19 125I-ENDOTHELIN 1 3 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 531 10 2 6 5.4 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 None
CHEMBL305576 102356 19 125I-ENDOTHELIN 1 3 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 531 10 2 6 5.4 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 None
None 214295 0 125I-ENDOTHELIN 52 2 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 520 10 2 7 4.7 CCCOC1=CC2=C(C=C1)C(C(C2C3=C(C=C(C=C3)OC)OCC(=O)O)C(=O)O)C4=CC5=C(C=C4)OCO5 None
3075702 215584 0 125I-Endothelin 1 -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
44208932 140163 6 UNDEFINED -120226 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 140163 6 UNDEFINED -120226 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
1973 201781 12 125I-ENDOTHELIN -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 201781 12 125I-ENDOTHELIN -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 201781 12 125I-ENDOTHELIN -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
None 214742 0 125I-ENDOTHELIN -10471285 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 372 2 1 3 4.4 CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl None
104865 697 94 125I-ENDOTHELIN 1 4 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3494 697 94 125I-ENDOTHELIN 1 4 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
392 697 94 125I-ENDOTHELIN 1 4 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
CHEMBL957 697 94 125I-ENDOTHELIN 1 4 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
DB00559 697 94 125I-ENDOTHELIN 1 4 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
176 394 63 None -7 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 394 63 None -7 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 394 63 None -7 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 394 63 None -7 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 394 63 None -7 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
1481 2027 109 None -112 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
Drug Central 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 None
3749 2027 109 None -112 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
Drug Central 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 None
589 2027 109 None -112 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
Drug Central 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 None
6908 2027 109 None -112 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
Drug Central 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 None
CHEMBL1513 2027 109 None -112 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
Drug Central 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 None
DB01029 2027 109 None -112 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to ETA receptorBinding affinity to ETA receptor
Drug Central 428 7 1 5 4.8 CCCCC1=NC2(C(=O)N1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)CCCC2 None
5472495 186041 41 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
Drug Central 372 4 1 3 4.0 CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1 None
CHEMBL488025 186041 41 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
Drug Central 372 4 1 3 4.0 CC1=C(CC(=O)O)c2cc(F)ccc2/C1=C\c1ccc(S(C)(=O)=O)cc1 None
104865 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3494 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
392 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
CHEMBL957 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
DB00559 697 94 None 1 4 Human 8.1 pKi = 8.1 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
104865 697 94 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3494 697 94 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
392 697 94 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
CHEMBL957 697 94 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
DB00559 697 94 None -1 4 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
104865 697 94 125I-ENDOTHELIN 1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3494 697 94 125I-ENDOTHELIN 1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
392 697 94 125I-ENDOTHELIN 1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
CHEMBL957 697 94 125I-ENDOTHELIN 1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
DB00559 697 94 125I-ENDOTHELIN 1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
11477084 3540 46 None 1 2 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
216235 3540 46 None 1 2 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
3548 3540 46 None 1 2 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
3950 3540 46 None 1 2 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
CHEMBL282724 3540 46 None 1 2 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
DB06268 3540 46 None 1 2 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Endothelin A receptorBinding affinity against human Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
11477084 3540 46 None -1 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
216235 3540 46 None -1 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
3548 3540 46 None -1 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
3950 3540 46 None -1 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
CHEMBL282724 3540 46 None -1 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
DB06268 3540 46 None -1 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity towards Endothelin A receptorBinding affinity towards Endothelin A receptor
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
3951 388 82 None -1 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
4337 388 82 None -1 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
6918493 388 82 None -1 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
CHEMBL1111 388 82 None -1 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
DB06403 388 82 None -1 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
12286 933 30 None 1348 2 Human 9.9 pKi = 9.9 Binding
Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>
Guide to Pharmacology 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 9703472
6433095 933 30 None 1348 2 Human 9.9 pKi = 9.9 Binding
Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>
Guide to Pharmacology 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 9703472
CHEMBL109648 933 30 None 1348 2 Human 9.9 pKi = 9.9 Binding
Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>
Guide to Pharmacology 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 9703472
DB06677 933 30 None 1348 2 Human 9.9 pKi = 9.9 Binding
Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>Binding affinity measured as displacement of ET-1 from CHO cells expressing hET<sub>A</sub>
Guide to Pharmacology 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 9703472
159594 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8632312
159594 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8676339
3487 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8632312
3487 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8676339
CHEMBL9194 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8632312
CHEMBL9194 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8676339
DB06199 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8632312
DB06199 518 38 None 1 3 Human 10.5 pKi = 10.5 Binding
CHO cells expressing human ET<sub>A</sub> receptor.CHO cells expressing human ET<sub>A</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8676339
10257882 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 16220969
8448 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 16220969
CHEMBL539423 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 16220969
DB12548 3576 37 None -11 2 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 592 12 1 7 6.5 CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2 16220969
177236 1293 39 None 2 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 8667356
3508 1293 39 None 2 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 8667356
CHEMBL23261 1293 39 None 2 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 8667356
DB04883 1293 39 None 2 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 8667356