Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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ligand
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Assay Type Assay Description Source Mol
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H don H acc LogP Smiles DOI
CHEMBL3980643 210757 0 None 6 2 Human 10.0 pIC50 = 10 Functional
Agonist activity at human recombinant ETB receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization by fluorimetric methodAgonist activity at human recombinant ETB receptor expressed in CHOK1 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
5311032 59915 26 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric 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 10.1016/j.ejmech.2016.06.006
CHEMBL1515091 59915 26 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric 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 10.1016/j.ejmech.2016.06.006
CHEMBL1741040 59915 26 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric 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 10.1016/j.ejmech.2016.06.006
10187997 109471 0 None -4 4 Human 9.2 pIC50 = 9.2 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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 -4 4 Human 9.2 pIC50 = 9.2 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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
CHEMBL284250 209105 0 None 1 4 Human 9.1 pIC50 = 9.1 Functional
Functional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B receptorFunctional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B 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
10603409 110102 0 None -1 4 Human 9.1 pIC50 = 9.1 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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 9.1 pIC50 = 9.1 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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
10210629 8661 0 None -7 4 Human 9.0 pIC50 = 9.0 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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 -7 4 Human 9.0 pIC50 = 9.0 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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
CHEMBL3143473 209578 0 None 1071 2 Human 8.9 pIC50 = 8.9 Functional
Antagonistic activity against endothelin B (ETB) receptor using human girardi heart cells.Antagonistic activity against endothelin B (ETB) receptor using human girardi heart cells.
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 8.9 pIC50 = 8.9 Functional
Antagonistic activity against endothelin B (ETB) receptor using human girardi heart cells.Antagonistic activity against endothelin B (ETB) receptor using human girardi heart cells.
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
9916235 9248 1 None -4 4 Human 8.9 pIC50 = 8.9 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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 -4 4 Human 8.9 pIC50 = 8.9 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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
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 B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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 B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) 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
11318978 167329 0 None -7 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 8.0 pIC50 = 8.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11387205 111060 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10298354 111501 0 None -15 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.0 pIC50 = 7.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10187313 106945 0 None -18 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.0 pIC50 = 7.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11169125 205815 0 None -5 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.0 pIC50 = 7.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10303258 161315 0 None -3 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 8.0 pIC50 = 8.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
9957883 98191 0 None -25 2 Human 6.0 pIC50 = 6.0 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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 6.0 pIC50 = 6.0 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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
9890440 8155 0 None -301 2 Human 5.9 pIC50 = 5.9 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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 5.9 pIC50 = 5.9 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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
11753582 205844 0 None -4 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.9 pIC50 = 6.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
3951 388 82 None -47 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.9 pIC50 = 5.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.9 pIC50 = 5.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.9 pIC50 = 5.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.9 pIC50 = 5.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11753090 105709 0 None -7 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.9 pIC50 = 6.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11398658 205855 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.9 pIC50 = 7.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10120430 205777 0 None -5 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.9 pIC50 = 7.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11330923 206077 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.9 pIC50 = 7.9 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
CHEMBL96822 214133 0 None 1 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing recombinant rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing recombinant rat ET- B receptors
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
11238540 205782 0 None -11 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.8 pIC50 = 5.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10166139 162780 0 None -2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.8 pIC50 = 7.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11376627 107133 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.8 pIC50 = 7.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11386977 205803 0 None -1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
9955200 9227 0 None -380 3 Human 5.8 pIC50 = 5.8 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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 -380 3 Human 5.8 pIC50 = 5.8 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm00008a002
11318409 205712 0 None -3 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.8 pIC50 = 7.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
CHEMBL413825 211329 0 None 4 2 Human 4.8 pIC50 = 4.8 Functional
Ability to block sarafotoxin-6c (SRTX-6c) stimulated arachidonic acid release in chinese hamster ovary (CHO) cells expressing recombinant rat endothelin B (ETB) receptorAbility to block sarafotoxin-6c (SRTX-6c) stimulated arachidonic acid release in chinese hamster ovary (CHO) cells expressing recombinant rat endothelin B (ETB) 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
10230737 111815 0 None -16 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.8 pIC50 = 7.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
18995992 99364 0 None -3 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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 6.8 pIC50 = 6.8 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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
18995991 99823 0 None -9 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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 6.8 pIC50 = 6.8 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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
10342643 5073 0 None -144 2 Human 5.8 pIC50 = 5.8 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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 5.8 pIC50 = 5.8 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm00008a002
11752174 172146 0 None -4 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.8 pIC50 = 5.8 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11410074 206045 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11421392 205643 0 None -5 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11387315 205691 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11397857 206046 0 None -6 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.7 pIC50 = 5.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10224745 112180 0 None -15 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.7 pIC50 = 6.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11226740 206155 0 None -9 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.7 pIC50 = 6.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
CHEMBL328942 209560 0 None -1 4 Rat 7.7 pIC50 = 7.7 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
CHEMBL433406 211882 0 None 9 2 Rat 7.7 pIC50 = 7.7 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
10187261 111039 0 None -3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11489318 206054 0 None -5 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
15289330 99328 0 None -18 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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 6.7 pIC50 = 6.7 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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
10230546 106750 0 None -4 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11273181 206120 0 None 4 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.7 pIC50 = 7.7 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
44327659 109321 0 None 1 2 Rat 6.7 pIC50 = 6.7 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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 Rat 6.7 pIC50 = 6.7 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
9955200 9227 0 None -53 3 Rat 6.7 pIC50 = 6.7 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
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 Rat 6.7 pIC50 = 6.7 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm00008a002
345351 9254 1 None -24 3 Rat 4.7 pIC50 = 4.7 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
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 Rat 4.7 pIC50 = 4.7 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
11365059 206050 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11467573 106743 0 None -9 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.6 pIC50 = 6.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11331242 106923 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11342005 205805 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11307805 106844 0 None -3 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10226239 206142 0 None -4 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.6 pIC50 = 6.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
44328057 96433 0 None 7 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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 7 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
11156376 112156 0 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.6 pIC50 = 6.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11375934 206166 0 None -3 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.6 pIC50 = 7.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11156301 78239 0 None -4 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.6 pIC50 = 6.6 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10070783 96596 0 None -5 3 Human 5.6 pIC50 = 5.6 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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 -5 3 Human 5.6 pIC50 = 5.6 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
11478911 155757 0 None -4 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
44327890 140868 0 None 46 3 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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 46 3 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
44327656 141245 0 None 1 2 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
11421972 206100 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
345351 9254 1 None -33 3 Human 4.5 pIC50 = 4.5 Functional
Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
CHEMBL11131 9254 1 None -33 3 Human 4.5 pIC50 = 4.5 Functional
Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
11455999 206084 0 None -31 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.5 pIC50 = 5.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10282008 205342 0 None -12 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11364770 163093 0 None -5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11191999 205756 0 None -4 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11168474 206158 0 None -9 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11308052 112155 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11330570 205840 0 None -4 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.5 pIC50 = 7.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11432855 206108 0 None -28 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.5 pIC50 = 5.5 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11444738 164316 0 None -4 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.4 pIC50 = 7.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
44327347 96302 0 None 3 3 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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 3 3 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
11235126 206179 0 None -52 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.4 pIC50 = 5.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11786120 168591 0 None -17 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.4 pIC50 = 5.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11409474 205816 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.4 pIC50 = 7.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
9845562 4658 0 None -7 3 Human 6.4 pIC50 = 6.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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 6.4 pIC50 = 6.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1 10.1021/jm00008a002
11330927 205764 0 None -8 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.4 pIC50 = 6.4 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
44283270 167307 0 None -1 4 Human 8.4 pIC50 = 8.4 Functional
Functional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B receptorFunctional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B 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 -1 4 Human 8.4 pIC50 = 8.4 Functional
Functional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B receptorFunctional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B 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
44327881 161114 0 None 2 2 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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 2 2 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
23670447 2968 2 None -501 4 Human 6.4 pIC50 = 6.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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 -501 4 Human 6.4 pIC50 = 6.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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 -501 4 Human 6.4 pIC50 = 6.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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 -501 4 Human 6.4 pIC50 = 6.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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
9807691 99589 0 None -134 2 Human 6.4 pIC50 = 6.4 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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 6.4 pIC50 = 6.4 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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
9845562 4658 0 None -87 3 Rat 5.4 pIC50 = 5.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
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 -87 3 Rat 5.4 pIC50 = 5.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1 10.1021/jm00008a002
9865706 97669 0 None -1 2 Rat 5.4 pIC50 = 5.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
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 Rat 5.4 pIC50 = 5.4 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 400 4 1 5 4.1 Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm00008a002
11742628 97770 0 None -234 3 Human 5.3 pIC50 = 5.3 Functional
Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).
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 -234 3 Human 5.3 pIC50 = 5.3 Functional
Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm00008a002
10166981 205349 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11283571 205854 0 None -7 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11477664 167593 0 None -6 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11408654 206188 0 None -19 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.3 pIC50 = 6.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10230703 206113 0 None -4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
9870830 204977 34 None -776 4 Human 6.3 pIC50 = 6.3 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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 -776 4 Human 6.3 pIC50 = 6.3 Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
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
11307457 205867 0 None -5 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11785813 106426 0 None -8 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10209814 205530 0 None -7 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11284285 106832 0 None -8 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11742628 97770 0 None -25 3 Rat 6.3 pIC50 = 6.3 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
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 Rat 6.3 pIC50 = 6.3 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm00008a002
10070783 96596 0 None -3 3 Rat 5.3 pIC50 = 5.3 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
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 Rat 5.3 pIC50 = 5.3 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
11490160 205758 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.3 pIC50 = 6.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11432418 106452 0 None -6 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.3 pIC50 = 7.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10140418 105707 0 None -43 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.3 pIC50 = 6.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
44327585 161222 0 None 14 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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 14 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
11167889 206090 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.3 pIC50 = 5.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10347783 206089 0 None -32 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.3 pIC50 = 6.3 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
1009 192 20 None 2238 2 Human 8.2 pIC50 = 8.2 Functional
Eurofins cellular functional assay - Antagonist (EDNRB)Eurofins cellular functional assay - Antagonist (EDNRB)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
5310991 192 20 None 2238 2 Human 8.2 pIC50 = 8.2 Functional
Eurofins cellular functional assay - Antagonist (EDNRB)Eurofins cellular functional assay - Antagonist (EDNRB)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
CHEMBL332794 192 20 None 2238 2 Human 8.2 pIC50 = 8.2 Functional
Eurofins cellular functional assay - Antagonist (EDNRB)Eurofins cellular functional assay - Antagonist (EDNRB)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
9894443 112068 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 8.2 pIC50 = 8.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11385689 112286 0 None -10 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.2 pIC50 = 5.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10163956 205845 0 None -10 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.2 pIC50 = 7.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11224973 106951 0 None -32 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.2 pIC50 = 6.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11353580 206190 0 None -21 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.2 pIC50 = 7.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11156692 167302 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.2 pIC50 = 7.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11204331 112074 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 8.2 pIC50 = 8.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10303311 106665 0 None -9 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.2 pIC50 = 7.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11202819 112059 0 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11478553 162886 0 None -10 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11744509 5343 0 None -5 2 Rat 6.1 pIC50 = 6.1 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
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 Rat 6.1 pIC50 = 6.1 Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 450 5 1 6 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1 10.1021/jm00008a002
11307120 111898 0 None 4 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11456110 206094 0 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
18995989 100076 0 None 2 2 Human 6.1 pIC50 = 6.1 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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 6.1 pIC50 = 6.1 Functional
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B 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
11318559 206057 0 None -5 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.1 pIC50 = 6.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11410410 205806 0 None -25 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.1 pIC50 = 6.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
CHEMBL413825 211329 0 None 4 2 Human 5.1 pIC50 = 5.1 Functional
Ability to block endothelin-1 (ET-1) stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells (AARA) expressing recombinant rat endothelin B (ETB) receptorAbility to block endothelin-1 (ET-1) stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells (AARA) expressing recombinant rat endothelin B (ETB) 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
11489946 205606 0 None -2 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.1 pIC50 = 6.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11785180 111007 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.1 pIC50 = 5.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11238500 206079 0 None -3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11441050 206086 0 None -85 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.1 pIC50 = 5.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11398818 167357 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11168401 111799 0 None -18 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.1 pIC50 = 5.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11489174 112043 0 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
10166543 111857 0 None -33 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11387934 106680 0 None -28 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11157599 162919 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 588 8 2 4 7.0 CC(C)c1ccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL420072 162919 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 588 8 2 4 7.0 CC(C)c1ccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)cc1 10.1021/jm031115r
11155687 206082 0 None -12 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11377200 107799 0 None -11 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.1 pIC50 = 7.1 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
44327466 95991 0 None 16 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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 16 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
11477084 3540 46 None -20 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration towards endothelin B receptor in humanInhibitory concentration towards endothelin B 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 -20 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration towards endothelin B receptor in humanInhibitory concentration towards endothelin B 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 -20 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration towards endothelin B receptor in humanInhibitory concentration towards endothelin B 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 -20 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration towards endothelin B receptor in humanInhibitory concentration towards endothelin B 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 -20 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration towards endothelin B receptor in humanInhibitory concentration towards endothelin B 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 -20 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration towards endothelin B receptor in humanInhibitory concentration towards endothelin B receptor in human
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm030528p
CHEMBL319537 209463 0 None -2 2 Rat 5.0 pIC50 = 5.0 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
11362537 107022 0 None -24 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.0 pIC50 = 5.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
44327348 161346 0 None -1 2 Rat 5.0 pIC50 = 5.0 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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 -1 2 Rat 5.0 pIC50 = 5.0 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
CHEMBL407933 210937 0 None -1 2 Rat 5.0 pIC50 = 5.0 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
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
11342089 106711 0 None -9 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 7.0 pIC50 = 7.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11488556 206123 0 None -10 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 5.0 pIC50 = 5.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
11226767 205783 0 None -6 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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 6.0 pIC50 = 6.0 Functional
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B 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
9809919 202694 0 None - 2 Rat 6.0 pKd = 6 Functional
In vitro functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETB receptors)In vitro functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETB 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 6.0 pKd = 6 Functional
In vitro functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETB receptors)In vitro functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETB 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
18184194 130027 0 None - 2 Rat 7.0 pKd = 7.0 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 7.0 pKd = 7.0 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9831249 59370 0 None - 2 Rat 8.0 pKd = 8.0 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 8.0 pKd = 8.0 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9985589 167669 0 None - 1 Human 6.9 pKd = 6.9 Functional
In vitro antagonistic activity against endothelin B receptor in isolated rabbit jugularis veinIn vitro antagonistic activity against endothelin B receptor in isolated rabbit jugularis vein
ChEMBL 576 9 1 8 5.0 CCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
CHEMBL433700 167669 0 None - 1 Human 6.9 pKd = 6.9 Functional
In vitro antagonistic activity against endothelin B receptor in isolated rabbit jugularis veinIn vitro antagonistic activity against endothelin B receptor in isolated rabbit jugularis vein
ChEMBL 576 9 1 8 5.0 CCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
104865 697 94 None -11 5 Rat 5.8 pKd = 5.8 Functional
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 -11 5 Rat 5.8 pKd = 5.8 Functional
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 -11 5 Rat 5.8 pKd = 5.8 Functional
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 -11 5 Rat 5.8 pKd = 5.8 Functional
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 -11 5 Rat 5.8 pKd = 5.8 Functional
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9848132 205833 0 None - 2 Human 5.8 pKd = 5.8 Functional
Compound was evaluated for the antagonism at the Endothelin B receptor in isolated rabbit jugularis veinCompound was evaluated for the antagonism at the Endothelin B receptor in isolated rabbit jugularis vein
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 - 2 Human 5.8 pKd = 5.8 Functional
Compound was evaluated for the antagonism at the Endothelin B receptor in isolated rabbit jugularis veinCompound was evaluated for the antagonism at the Endothelin B receptor in isolated rabbit jugularis vein
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
9961131 131622 0 None - 2 Rat 6.6 pKd = 6.6 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 6.6 pKd = 6.6 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9809919 202694 0 None - 2 Rat 7.6 pKd = 7.6 Functional
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 7.6 pKd = 7.6 Functional
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9809270 130805 0 None - 2 Rat 5.6 pKd = 5.6 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 5.6 pKd = 5.6 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9873255 59307 0 None - 2 Rat 6.6 pKd = 6.6 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 6.6 pKd = 6.6 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
18184234 61865 0 None - 2 Rat 6.6 pKd = 6.6 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 6.6 pKd = 6.6 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9807691 99589 0 None -134 2 Human 5.5 pKd = 5.5 Functional
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
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 5.5 pKd = 5.5 Functional
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
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
9810571 61042 0 None - 2 Rat 7.5 pKd = 7.5 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 7.5 pKd = 7.5 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9897092 59606 0 None - 2 Rat 7.5 pKd = 7.5 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 - 2 Rat 7.5 pKd = 7.5 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
18184229 59281 0 None - 2 Rat 6.4 pKd = 6.4 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 6.4 pKd = 6.4 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9853680 98182 0 None - 2 Rat 7.4 pKd = 7.4 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 - 2 Rat 7.4 pKd = 7.4 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9830773 129691 0 None - 2 Rat 6.4 pKd = 6.4 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 6.4 pKd = 6.4 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9874557 129203 0 None - 2 Rat 7.3 pKd = 7.3 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 7.3 pKd = 7.3 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9831527 128947 0 None - 2 Rat 7.3 pKd = 7.3 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 - 2 Rat 7.3 pKd = 7.3 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9957883 98191 0 None -25 2 Human 6.2 pKd = 6.2 Functional
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
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 6.2 pKd = 6.2 Functional
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
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
18995992 99364 0 None -3 2 Human 6.2 pKd = 6.2 Functional
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
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 6.2 pKd = 6.2 Functional
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
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
9917072 61759 0 None - 2 Rat 7.2 pKd = 7.2 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 7.2 pKd = 7.2 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9853077 59300 0 None - 2 Rat 7.2 pKd = 7.2 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 7.2 pKd = 7.2 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9917706 129204 0 None - 2 Rat 8.0 pKd = 8.0 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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 8.0 pKd = 8.0 Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB 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
9843631 92766 9 None - 0 Human 4.7 pKi = 4.7 Functional
Inhibitory concentration against endotheline ETB receptorInhibitory concentration against endotheline ETB receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm030480f
CHEMBL24461 92766 9 None - 0 Human 4.7 pKi = 4.7 Functional
Inhibitory concentration against endotheline ETB receptorInhibitory concentration against endotheline ETB receptor
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm030480f
10096179 176436 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against human Endothelin B receptor expressed in CHO cellsAntagonist activity against human Endothelin B receptor expressed in 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 6.5 pKi = 6.5 Functional
Antagonist activity against human Endothelin B receptor expressed in CHO cellsAntagonist activity against human Endothelin B receptor expressed in 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 5.5 pA2 = 5.5 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 5.5 pA2 = 5.5 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 5.5 pA2 = 5.5 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 5.5 pA2 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
104865 697 94 None -11 5 Rat 6.0 pA2 = 6 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 -11 5 Rat 6.0 pA2 = 6 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 -11 5 Rat 6.0 pA2 = 6 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 -11 5 Rat 6.0 pA2 = 6 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 -11 5 Rat 6.0 pA2 = 6 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
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
104865 697 94 None -11 5 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
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 -11 5 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
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 -11 5 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
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 -11 5 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
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 -11 5 Rat 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3951 388 82 None -47 2 Human 5.9 pIC50 = 5.9 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 5.9 pIC50 = 5.9 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 5.9 pIC50 = 5.9 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 5.9 pIC50 = 5.9 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 5.9 pIC50 = 5.9 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
10070 445 41 None -109 2 Human 6.0 pIC50 = 6.0 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 6.0 pIC50 = 6.0 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 6.0 pIC50 = 6.0 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 6.0 pIC50 = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
16004692 2411 85 None -107 2 Human 6.4 pIC50 = 6.4 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 6.4 pIC50 = 6.4 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 6.4 pIC50 = 6.4 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 6.4 pIC50 = 6.4 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 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
1011 3288 24 None 102 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 8612786
5312146 3288 24 None 102 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 8612786
CHEMBL1628620 3288 24 None 102 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 8612786
3911 3253 0 None 501 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8183252
CHEMBL429908 3253 0 None 501 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8183252
9651 2134 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 682 12 2 10 6.9 COc1ccccc1Oc1c(OCCC(=O)Nc2c(C)cccc2C)nc(nc1NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 28805809
9810112 2134 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 682 12 2 10 6.9 COc1ccccc1Oc1c(OCCC(=O)Nc2c(C)cccc2C)nc(nc1NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 28805809
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 Rat 6.8 pEC50 = 6.8 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
CHEMBL2370067 208023 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
CHEMBL315841 209437 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
CHEMBL407269 210894 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
CHEMBL387200 210651 0 None - 0 Rat 7.2 pEC50 = 7.2 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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 Rat 5.2 pEC50 = 5.2 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
CHEMBL313344 209356 0 None - 0 Rat 5.2 pEC50 = 5.2 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
CHEMBL1790180 207130 0 None -1 3 Human 10.5 pIC50 = 10.5 Binding
Binding affinity to human ETB receptor by radioligand displacement assayBinding affinity to human ETB 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]([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 10.1016/j.ejmech.2013.01.044
CHEMBL1790180 207130 0 None -1 3 Human 10.4 pIC50 = 10.4 Binding
Binding affinity to human ETB receptor by radioligand displacement assayBinding affinity to human ETB 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]([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 10.1016/j.bmc.2013.03.016
CHEMBL1790180 207130 0 None -1 3 Human 10.0 pIC50 = 10.0 Binding
Displacement of radiolabeled endothelin-3 from human endothelin ETB receptorDisplacement of radiolabeled endothelin-3 from human endothelin ETB 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]([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/jm8007618
CHEMBL438733 212033 0 None - 0 Bovine 10.0 pIC50 = 10.0 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B 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
44284481 211967 0 None - 5 Bovine 9.9 pIC50 = 9.9 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B 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 - 5 Bovine 9.9 pIC50 = 9.9 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B 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
44284481 211967 0 None -4 5 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETB 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 pIC50 = 9.9 Binding
Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETB 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
10603409 110102 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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 9.9 pIC50 = 9.9 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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
CHEMBL1790962 207157 0 None - 1 Bovine 9.8 pIC50 = 9.8 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B 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
CHEMBL427748 211614 0 None - 0 Bovine 9.8 pIC50 = 9.8 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B 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
10603409 110102 0 None - 0 Pig 9.7 pIC50 = 9.7 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.7 pIC50 = 9.7 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10651488 162815 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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 9.7 pIC50 = 9.7 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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
44284481 211967 0 None -4 5 Human 9.7 pIC50 = 9.7 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB 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 10.1016/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 membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB 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 10.1016/S0960-894X(97)00400-9
CHEMBL2165327 207577 7 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
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](Cc1cnc[nH]1)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/jm3009103
CHEMBL263855 208839 0 None - 0 Bovine 9.6 pIC50 = 9.6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
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](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CC(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)NCC(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N2CCC[C@@H]2C(=O)N1)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/S0960-894X(97)00296-5
CHEMBL2373292 208620 0 None - 1 Bovine 9.6 pIC50 = 9.6 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B 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
10839947 116786 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 9.6 pIC50 = 9.6 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
9916235 9248 1 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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 9.6 pIC50 = 9.6 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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
9916235 9248 1 None - 0 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10187997 109471 0 None - 0 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
CHEMBL1790963 207158 0 None - 0 Bovine 9.5 pIC50 = 9.5 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B 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
10210629 8661 0 None - 0 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
CHEMBL2373291 208619 0 None - 1 Bovine 9.4 pIC50 = 9.4 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B 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
CHEMBL411171 211110 0 None - 1 Bovine 9.4 pIC50 = 9.4 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B 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
10187997 109471 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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 9.3 pIC50 = 9.3 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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
10210629 8661 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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 9.3 pIC50 = 9.3 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) 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
10555806 12001 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 9.2 pIC50 = 9.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 9.2 pIC50 = 9.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
1009 192 20 None - 1 Human 9.1 pIC50 = 9.1 Binding
Affinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRBAffinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRB
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 nan
5310991 192 20 None - 1 Human 9.1 pIC50 = 9.1 Binding
Affinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRBAffinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRB
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 nan
CHEMBL332794 192 20 None - 1 Human 9.1 pIC50 = 9.1 Binding
Affinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRBAffinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRB
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 nan
10792711 114280 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 9.1 pIC50 = 9.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
44314619 202970 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 9.1 pIC50 = 9.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
CHEMBL284250 209105 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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
9916235 9248 1 None - 0 Pig 9.1 pIC50 = 9.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.1 pIC50 = 9.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10816963 112817 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 9.1 pIC50 = 9.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
9896468 170092 0 None - 0 Pig 9.1 pIC50 = 9.1 Binding
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 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 Pig 9.1 pIC50 = 9.1 Binding
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 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
10626362 11331 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 9.0 pIC50 = 9.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 9.0 pIC50 = 9.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
10651488 162815 0 None - 0 Pig 9.0 pIC50 = 9.0 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.0 pIC50 = 9.0 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10187997 109471 0 None - 0 Pig 9.0 pIC50 = 9 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.0 pIC50 = 9 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10603409 110102 0 None - 0 Pig 9.0 pIC50 = 9 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 9.0 pIC50 = 9 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10698065 11992 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 9.0 pIC50 = 9.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 9.0 pIC50 = 9.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
10841170 11998 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 9.0 pIC50 = 9.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 9.0 pIC50 = 9.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
44314619 202970 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell 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 9.0 pIC50 = 9.0 Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell 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
10816963 112817 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 9.0 pIC50 = 9.0 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
10167052 109138 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.9 pIC50 = 8.9 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
137630807 160553 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 641 12 4 7 4.8 CCCC[C@@H](NC(=O)[C@@H](Cc1cc2ccccc2n1C(=O)OC)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/j.bmcl.2017.04.049
CHEMBL4075238 160553 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 641 12 4 7 4.8 CCCC[C@@H](NC(=O)[C@@H](Cc1cc2ccccc2n1C(=O)OC)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/j.bmcl.2017.04.049
CHEMBL4117106 160553 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 641 12 4 7 4.8 CCCC[C@@H](NC(=O)[C@@H](Cc1cc2ccccc2n1C(=O)OC)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/j.bmcl.2017.04.049
10792636 167939 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.9 pIC50 = 8.9 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
CHEMBL2370534 208114 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
155560344 175919 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-B receptor in human Girardi heart 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 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-B receptor in human Girardi heart 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 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-B receptor in human Girardi heart 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
44283453 138235 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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 8.9 pIC50 = 8.9 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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
44314620 102657 0 None - 0 Pig 8.9 pIC50 = 8.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.9 pIC50 = 8.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
3887 2033 39 None -7 4 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrs
ChEMBL None None None None 10.1021/acs.jmedchem.5b01781
5311192 2033 39 None -7 4 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrs
ChEMBL None None None None 10.1021/acs.jmedchem.5b01781
CHEMBL72410 2033 39 None -7 4 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrs
ChEMBL None None None None 10.1021/acs.jmedchem.5b01781
10839947 116786 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.9 pIC50 = 8.9 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
10210629 8661 0 None - 0 Pig 8.8 pIC50 = 8.8 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.8 pIC50 = 8.8 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10792934 163350 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.8 pIC50 = 8.8 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
10120499 109255 0 None - 0 Pig 8.8 pIC50 = 8.8 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.8 pIC50 = 8.8 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
44314472 103308 0 None - 0 Pig 8.8 pIC50 = 8.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.8 pIC50 = 8.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44284481 211967 0 None 3 5 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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](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 3 5 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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](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
44283420 161231 0 None - 0 Pig 8.8 pIC50 = 8.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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 8.8 pIC50 = 8.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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
10604119 11337 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.8 pIC50 = 8.8 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.8 pIC50 = 8.8 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
9846994 105496 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.8 pIC50 = 8.8 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
44315008 102345 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
9961347 11842 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.7 pIC50 = 8.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.7 pIC50 = 8.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
44315007 202833 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
CHEMBL411057 211103 0 None - 0 Bovine 8.0 pIC50 = 8 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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(96)00127-8
CHEMBL384792 210578 0 None - 0 Bovine 8.0 pIC50 = 8 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
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[C@H](C(=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/S0960-894X(97)00296-5
CHEMBL405599 210811 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
CHEMBL413825 211329 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) 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
10627805 16387 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.0 pIC50 = 8 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
22004774 100329 0 None - 0 Pig 7.0 pIC50 = 7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.0 pIC50 = 7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10146305 173689 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 7.0 pIC50 = 7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
44385008 130826 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.0 pIC50 = 7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44333867 4559 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.0 pIC50 = 7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44284196 100044 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.0 pIC50 = 7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
9853025 59489 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.0 pIC50 = 7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
104865 697 94 None -6 4 Human 6.0 pIC50 = 6 Binding
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
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 -6 4 Human 6.0 pIC50 = 6 Binding
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
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 -6 4 Human 6.0 pIC50 = 6 Binding
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
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 -6 4 Human 6.0 pIC50 = 6 Binding
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
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 -6 4 Human 6.0 pIC50 = 6 Binding
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
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
CHEMBL407188 210888 0 None - 0 Bovine 6.0 pIC50 = 6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
44284481 211967 0 None - 5 Bovine 6.0 pIC50 = 6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
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)00296-5
CHEMBL437472 211967 0 None - 5 Bovine 6.0 pIC50 = 6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
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)00296-5
10814440 97682 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.0 pIC50 = 6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)ccc2OC)cc1 10.1021/jm9606507
44279383 99519 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
122044 10063 47 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of 125I-ET1 from rat aortic ring ETB receptorDisplacement of 125I-ET1 from rat aortic ring ETB receptor
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 Rat 6.0 pIC50 = 6 Binding
Displacement of 125I-ET1 from rat aortic ring ETB receptorDisplacement of 125I-ET1 from rat aortic ring ETB receptor
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
17869373 14450 0 None - 0 Pig 6.0 pIC50 = 6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.0 pIC50 = 6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.0 pIC50 = 6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
44276969 106343 0 None - 0 Rat 6.0 pIC50 = 6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 6.0 pIC50 = 6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
44311225 202991 0 None - 0 Human 6.0 pIC50 = 6 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
CHEMBL269428 209032 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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](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
44267002 98094 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.0 pIC50 = 5 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 546 5 1 7 5.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3c2CCc2ccccc2C3=O)cc1 10.1021/jm9606507
10552883 109503 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 5.0 pIC50 = 5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
11100307 201502 0 None - 0 Pig 5.0 pIC50 = 5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.0 pIC50 = 5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 354 5 1 5 3.8 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL289687 209120 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
10453733 111806 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cccnc2)ccc1C#N 10.1021/jm9707131
11797717 205322 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccncc2)ccc1C#N 10.1021/jm9707131
10504148 205518 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 459 10 1 5 6.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ccccn1 10.1021/jm9707131
10599453 205531 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 445 9 1 6 5.2 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N 10.1021/jm9707131
10740214 205563 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 408 9 1 6 4.9 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cnsc2)ccc1C#N 10.1021/jm9707131
10693679 205631 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 425 10 2 5 4.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(N)=O 10.1021/jm9707131
11796594 205636 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 424 10 1 5 5.8 CC(=O)c1ccc(OCc2ccsc2)cc1OC(CCC(=O)O)c1ccccc1C 10.1021/jm9707131
10669120 205702 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1[C@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
10694804 206075 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 449 10 1 6 6.3 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ncco1 10.1021/jm9707131
CHEMBL289687 209120 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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](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
137661460 158816 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.0 pIC50 = 6 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
9852624 128146 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.0 pIC50 = 7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10502577 12283 0 None - 0 Human 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10814776 99001 0 None - 0 Human 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.0 pIC50 = 5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
18184234 61865 0 None - 2 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.0 pIC50 = 7.0 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9961131 131622 0 None - 2 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.0 pIC50 = 7.0 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
42630654 18205 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
10210086 60937 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
42630654 18205 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
11071347 117290 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
44279677 101743 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
10504475 205214 0 None - 0 Pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44458669 84236 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.0 pIC50 = 6.0 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
10168939 130833 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
76320429 85400 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETB 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
10625633 205400 0 None - 0 Pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.0 pIC50 = 6.0 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10817024 12007 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 7.0 pIC50 = 7.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 7.0 pIC50 = 7.0 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
11798504 96662 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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 6.0 pIC50 = 6.0 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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
71458721 81275 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
CHEMBL2304010 207711 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44320192 106560 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.0 pIC50 = 8.0 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
10321290 4553 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 8.0 pIC50 = 8.0 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44284287 160688 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 8.0 pIC50 = 8.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
44314657 102715 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 7.0 pIC50 = 7.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
159594 518 38 None - 3 Pig 7.0 pIC50 = 7.0 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 - 3 Pig 7.0 pIC50 = 7.0 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 - 3 Pig 7.0 pIC50 = 7.0 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 - 3 Pig 7.0 pIC50 = 7.0 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
122044 10063 47 None - 0 Human 6.0 pIC50 = 6.0 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B 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 Human 6.0 pIC50 = 6.0 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1021/jm0102304
15289330 99328 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.0 pIC50 = 6.0 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
18995998 161829 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.0 pIC50 = 6.0 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
CHEMBL438768 212038 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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
15453179 203760 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 6.0 pIC50 = 6.0 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
11783885 100407 0 None - 0 Pig 6.0 pIC50 = 6.0 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.0 pIC50 = 6.0 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 382 7 1 5 4.6 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
44279350 167602 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
44314609 203030 0 None - 0 Pig 6.0 pIC50 = 6.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 6.0 pIC50 = 6.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44458999 167654 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.0 pIC50 = 6.0 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
44266552 4431 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
44317109 104400 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.0 pIC50 = 5.0 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10694591 9121 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.0 pIC50 = 5.0 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 444 6 1 6 4.6 CC(C)Oc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10551532 110082 0 None - 0 Pig 5.0 pIC50 = 5.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 5.0 pIC50 = 5.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10791702 194133 0 None - 0 Pig 5.0 pIC50 = 5.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 5.0 pIC50 = 5.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
15340612 106336 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 5.0 pIC50 = 5.0 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
CHEMBL2367550 207829 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar 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)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
44439103 91505 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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
10836835 96641 0 None - 0 Pig 5.0 pIC50 = 5.0 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.0 pIC50 = 5.0 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44351961 18633 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
10218058 81243 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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
42630532 18200 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
10218058 81243 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
42630532 18200 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
22467230 84917 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 5.9 pIC50 = 5.9 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
10281943 59734 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
71460536 81260 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.9 pIC50 = 5.9 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
23445593 59904 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 4.9 pIC50 = 4.9 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
10553017 97643 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
9807456 60135 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9852318 9508 5 None -2691 2 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B 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 7.9 pIC50 = 7.9 Binding
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B 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 7.9 pIC50 = 7.9 Binding
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B 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
CHEMBL263294 208809 0 None - 0 Bovine 7.9 pIC50 = 7.9 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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](Cc2ccccc2)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
CHEMBL385492 210595 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
1009 192 20 None - 1 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
9852318 9508 5 None -2691 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 7.9 pIC50 = 7.9 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 7.9 pIC50 = 7.9 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
21462932 48855 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 548 8 2 8 4.6 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(NS(C)(=O)=O)ccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL156194 48855 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 548 8 2 8 4.6 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(NS(C)(=O)=O)ccc23)cc1 10.1016/s0960-894x(99)00040-2
10173807 50594 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
CHEMBL410321 211055 0 None - 0 Bovine 6.9 pIC50 = 6.9 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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)NCC(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
9825494 200914 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
CHEMBL2304007 207708 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
155551580 173411 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
11757759 173864 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
9870830 204977 34 None -66 2 Human 6.9 pIC50 = 6.9 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 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 6.9 pIC50 = 6.9 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 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
44311135 202480 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 6.9 pIC50 = 6.9 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
8260 527 46 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at ETB receptor (unknown origin) in presence of ET1Antagonist activity at ETB 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 5.9 pIC50 = 5.9 Binding
Antagonist activity at ETB receptor (unknown origin) in presence of ET1Antagonist activity at ETB 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 5.9 pIC50 = 5.9 Binding
Antagonist activity at ETB receptor (unknown origin) in presence of ET1Antagonist activity at ETB 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
15453180 104733 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.9 pIC50 = 5.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10288020 14445 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.9 pIC50 = 5.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.9 pIC50 = 5.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
44266646 98100 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
10310877 202182 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
10769526 102214 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
44211959 55133 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 5.9 pIC50 = 5.9 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
44327412 205837 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.9 pIC50 = 5.9 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
11038320 18670 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
10501279 97753 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 4.9 pIC50 = 4.9 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 402 6 1 5 4.1 COc1ccc(C2(O)OC(=O)C(c3cccc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44277368 106349 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
44386144 61640 0 None - 0 Pig 4.9 pIC50 = 4.9 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.9 pIC50 = 4.9 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
44266575 4560 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
9830773 129691 0 None - 2 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.9 pIC50 = 6.9 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44291897 100810 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10190108 130163 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.9 pIC50 = 6.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
19432672 202511 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 5.9 pIC50 = 5.9 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
23445333 127271 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 4.9 pIC50 = 4.9 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
10599829 96668 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44368390 45036 0 None - 0 Pig 4.9 pIC50 = 4.9 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 4.9 pIC50 = 4.9 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
71462321 81581 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.9 pIC50 = 5.9 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10577111 205160 0 None - 0 Pig 4.9 pIC50 = 4.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 4.9 pIC50 = 4.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44371495 53945 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 590 10 1 8 5.4 CCCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
CHEMBL160768 53945 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 590 10 1 8 5.4 CCCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
44314575 103084 0 None - 0 Pig 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44314723 203279 0 None - 0 Pig 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44386169 130854 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
123883 14460 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 6.9 pIC50 = 6.9 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 6.9 pIC50 = 6.9 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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
11102201 201523 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11005243 201681 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
CHEMBL2304015 207716 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell 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
10505755 14400 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 6.9 pIC50 = 6.9 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 6.9 pIC50 = 6.9 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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
44334053 4468 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 6.9 pIC50 = 6.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
CHEMBL328942 209560 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranesInhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar 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)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
44371516 50697 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
44351968 117564 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
44327348 161346 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
CHEMBL407933 210937 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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(=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
10503067 8071 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.9 pIC50 = 5.9 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 436 5 1 6 4.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCCC2)cc1 10.1021/jm9606507
15411005 4677 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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 5.9 pIC50 = 5.9 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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
11026025 201187 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.9 pIC50 = 5.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11762081 201619 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.9 pIC50 = 5.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
CHEMBL147908 207029 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
10649086 174671 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.9 pIC50 = 5.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
44299023 194813 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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
56681797 62979 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
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 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
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
44270523 48337 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 5.9 pIC50 = 5.9 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
15453178 104261 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 348 4 1 4 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
18617303 105302 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
18617389 162914 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
18617374 203795 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
CHEMBL414917 211402 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) 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
10575552 110808 0 None - 0 Pig 4.9 pIC50 = 4.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.9 pIC50 = 4.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
CHEMBL2369710 207898 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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
9915028 9306 12 None -28183 2 Human 4.9 pIC50 = 4.9 Binding
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B 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 4.9 pIC50 = 4.9 Binding
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B 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 4.9 pIC50 = 4.9 Binding
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B 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
44385621 127661 0 None - 0 Pig 4.9 pIC50 = 4.9 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.9 pIC50 = 4.9 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
23445537 60802 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 5.9 pIC50 = 5.9 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
44320488 106489 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 438 5 1 5 5.7 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1C1CCCCC1 10.1016/s0960-894x(00)00513-8
23445547 111837 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.9 pIC50 = 4.9 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2cc(-c3ccccc3)cs2)c1Br 10.1016/S0960-894X(96)00496-9
137652304 156672 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 5.9 pIC50 = 5.9 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
10119105 100964 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
11798504 96662 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.9 pIC50 = 5.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
23445336 59845 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.9 pIC50 = 5.9 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44314890 104584 0 None - 0 Pig 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 7.9 pIC50 = 7.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44334128 4325 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.9 pIC50 = 7.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44334145 4569 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.9 pIC50 = 7.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44284292 167538 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.9 pIC50 = 7.9 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
44311346 102675 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 7.9 pIC50 = 7.9 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
17885912 106602 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 7.8 pIC50 = 7.8 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
CHEMBL433406 211882 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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(=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
15453172 203267 4 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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 6.9 pIC50 = 6.9 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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
44298381 194220 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
CHEMBL2304009 207710 0 None - 0 Pig 6.9 pIC50 = 6.9 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
CHEMBL86814 214105 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
44333721 167219 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 6.9 pIC50 = 6.9 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
CHEMBL436899 211936 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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
10916428 162133 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.9 pIC50 = 5.9 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 402 4 1 5 4.4 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
44295106 14558 0 None - 0 Pig 5.9 pIC50 = 5.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.9 pIC50 = 5.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.9 pIC50 = 5.9 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
10212163 129561 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44266646 98100 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
122272 96637 23 None - 2 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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 - 2 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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
18617345 104712 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
18617314 203511 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
3811690 203689 3 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.9 pIC50 = 4.9 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
CHEMBL441006 212117 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) 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
44277035 106356 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
10646831 183328 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
CHEMBL1791277 207165 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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(=O)O)NC(=O)[C@H](Cc1c[nH]cn1)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
10625530 205301 3 None - 0 Pig 4.9 pIC50 = 4.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 4.9 pIC50 = 4.9 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44266595 4312 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
10766385 97963 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.9 pIC50 = 5.9 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 460 6 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
9870959 8814 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 4.9 pIC50 = 4.9 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10811595 98299 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.9 pIC50 = 4.9 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
155562688 174598 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
44352026 116969 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
137633653 156044 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 5.8 pIC50 = 5.8 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
44311283 101850 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
10553490 180524 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
71455062 81253 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44266538 5376 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 371 4 1 4 4.8 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccccc1 10.1016/0960-894X(96)00170-9
52950137 18235 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 5.8 pIC50 = 5.8 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
71456863 81264 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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 6.8 pIC50 = 6.8 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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
71456863 81264 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10625083 204910 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
71460537 81271 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.8 pIC50 = 5.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
21041266 81586 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.8 pIC50 = 5.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44304492 96099 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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 10.1021/jm00015a003
CHEMBL262993 96099 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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 10.1021/jm00015a003
CHEMBL2304006 207707 0 None - 0 Pig 7.8 pIC50 = 7.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
22467235 96065 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 7.8 pIC50 = 7.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
23288645 169149 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 580 12 3 8 5.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(SC)cc3)cc(C(=O)Nc3ccccc3)cc2OCCO)c1 10.1016/j.bmcl.2016.06.014
CHEMBL4438411 169149 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 580 12 3 8 5.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(SC)cc3)cc(C(=O)Nc3ccccc3)cc2OCCO)c1 10.1016/j.bmcl.2016.06.014
9917072 61759 0 None - 2 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.8 pIC50 = 7.8 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44304492 96099 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranesInhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar 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 10.1021/jm970161m
CHEMBL262993 96099 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranesInhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar 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 10.1021/jm970161m
44284287 160688 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.8 pIC50 = 7.8 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
CHEMBL94983 214129 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
10983045 201208 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11144344 201314 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
104865 697 94 None -6 4 Human 6.8 pIC50 = 6.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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 -6 4 Human 6.8 pIC50 = 6.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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 -6 4 Human 6.8 pIC50 = 6.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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 -6 4 Human 6.8 pIC50 = 6.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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 -6 4 Human 6.8 pIC50 = 6.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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
CHEMBL89736 214114 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL328942 209560 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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)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
104865 697 94 None -6 4 Human 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB 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(97)00400-9
3494 697 94 None -6 4 Human 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB 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(97)00400-9
392 697 94 None -6 4 Human 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB 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(97)00400-9
CHEMBL957 697 94 None -6 4 Human 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB 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(97)00400-9
DB00559 697 94 None -6 4 Human 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB 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(97)00400-9
10671649 98101 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 460 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
10961546 96298 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
18738881 79158 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 5.8 pIC50 = 5.8 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
19363918 14452 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
CHEMBL1793934 207179 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
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
18995988 99860 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 389 6 1 4 5.5 COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3ccccc23)c1 10.1016/0960-894X(96)00232-6
44317215 203542 2 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.8 pIC50 = 4.8 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
18617377 203753 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.8 pIC50 = 4.8 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10665805 97713 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 354 4 1 6 3.0 CCC1=C(c2ccc3c(c2)OCO3)C(=O)OC1(O)c1ccc(OC)cc1 10.1021/jm9606507
CHEMBL413880 211336 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) 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
10882352 201285 0 None - 0 Pig 4.8 pIC50 = 4.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 4.8 pIC50 = 4.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 340 4 1 5 3.4 CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
44276577 106361 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
44266592 5288 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
71458718 81248 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.8 pIC50 = 5.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
23445250 167532 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 5.8 pIC50 = 5.8 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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
10302118 60088 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
18184249 127937 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.8 pIC50 = 5.8 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10528383 11116 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
9915028 9306 12 None -28183 2 Human 4.8 pIC50 = 4.8 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 4.8 pIC50 = 4.8 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 4.8 pIC50 = 4.8 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
9955200 9227 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
24997097 18272 2 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
23445507 59433 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
24997097 18272 2 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 4.8 pIC50 = 4.8 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
11797486 11923 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10671037 130909 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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
21041264 81585 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10554539 100760 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10743872 96746 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
CHEMBL319719 209465 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
10625270 112863 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
177236 1293 39 None -134 3 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 -134 3 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 -134 3 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 -134 3 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
9853077 59300 0 None - 2 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.8 pIC50 = 7.8 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10950843 201254 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10152810 14602 1 None - 0 Pig 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
44311284 202534 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
44371532 51185 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
44278161 99330 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 5.8 pIC50 = 5.8 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
CHEMBL2370247 208058 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
10790686 5164 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 474 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCCO3)cc1 10.1021/jm9606507
10552007 6231 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
11058717 201119 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 412 8 1 6 4.6 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCC)cc21 10.1021/jm010382z
10951244 201255 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44294580 14451 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
44266552 4431 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
44310016 202133 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
10195727 202220 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
9809526 14675 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
19010508 56036 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 5.8 pIC50 = 5.8 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
22616262 203818 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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 4.8 pIC50 = 4.8 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 366 3 1 4 3.7 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1Br 10.1016/0960-894X(96)00441-6
10505209 9212 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
10767210 110814 0 None - 0 Pig 4.8 pIC50 = 4.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.8 pIC50 = 4.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10813007 112808 0 None - 0 Pig 4.8 pIC50 = 4.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.8 pIC50 = 4.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
137655525 158433 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 4.8 pIC50 = 4.8 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
71462247 81272 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
71455063 81269 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.8 pIC50 = 6.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10304227 129473 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9915028 9306 12 None -28183 2 Human 4.8 pIC50 = 4.8 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 4.8 pIC50 = 4.8 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 4.8 pIC50 = 4.8 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10744041 96840 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10140965 100690 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
44371357 119221 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 515 8 1 8 5.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2cc(OC)c(OC)c(OC)c2)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
CHEMBL347680 119221 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 515 8 1 8 5.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2cc(OC)c(OC)c(OC)c2)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
18995992 99364 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.8 pIC50 = 6.8 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
10994373 161892 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11102844 201541 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44314581 104385 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 6.8 pIC50 = 6.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
CHEMBL2304014 207715 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44311233 202400 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 6.8 pIC50 = 6.8 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
CHEMBL408141 210946 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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
CHEMBL436884 211932 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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
44327726 206146 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.8 pIC50 = 5.8 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
18617393 203556 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.8 pIC50 = 4.8 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10623877 8388 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
10649122 9632 0 None - 0 Pig 4.8 pIC50 = 4.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.8 pIC50 = 4.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
15340616 106338 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
10344511 59356 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.8 pIC50 = 5.8 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
10525281 182258 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
12286 933 30 None -1348 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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 6.8 pIC50 = 6.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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 6.8 pIC50 = 6.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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 6.8 pIC50 = 6.8 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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
10342643 5073 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
71455061 81247 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.8 pIC50 = 5.8 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
5310990 166266 9 None - 1 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10741025 181089 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.8 pIC50 = 4.8 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
44320782 106576 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 6.8 pIC50 = 6.8 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
23445438 61155 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 4.8 pIC50 = 4.8 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
10815726 11328 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
10122442 130162 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.8 pIC50 = 7.8 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10602743 7063 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.8 pIC50 = 6.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
9933950 201129 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.8 pIC50 = 6.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44295173 14449 0 None - 0 Pig 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.8 pIC50 = 6.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
9868822 8490 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.8 pIC50 = 5.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
9960931 107522 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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 5.8 pIC50 = 5.8 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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
CHEMBL433349 211879 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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
9868379 100303 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11733232 201167 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1cccc2c1C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
11826062 201291 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.8 pIC50 = 5.8 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
9868379 100303 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
44295032 14606 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
44294929 14610 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.8 pIC50 = 5.8 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
CHEMBL317064 209441 13 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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](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
11798999 205841 0 None - 0 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.8 pIC50 = 5.8 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
CHEMBL303185 209162 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding activity against Endothelin B receptor 0f Porcine cerebellum membranesBinding activity against Endothelin B receptor 0f Porcine cerebellum 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
10647021 6881 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1OC 10.1021/jm9606507
10740614 97843 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 4.8 pIC50 = 4.8 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 416 5 1 6 3.8 COc1cccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c1 10.1021/jm9606507
CHEMBL303185 209162 0 None - 0 Pig 4.8 pIC50 = 4.8 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
443289 702 40 None - 3 Pig 4.8 pIC50 = 4.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
997 702 40 None - 3 Pig 4.8 pIC50 = 4.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
CHEMBL314691 702 40 None - 3 Pig 4.8 pIC50 = 4.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
DB12054 702 40 None - 3 Pig 4.8 pIC50 = 4.8 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
CHEMBL336033 209818 1 None - 0 Pig 4.8 pIC50 = 4.8 Binding
Inhibitory effect against porcine Endothelin B receptorInhibitory effect against porcine Endothelin B 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
9806559 9046 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 4.8 pIC50 = 4.8 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
10224228 179022 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10601795 96511 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.7 pIC50 = 5.7 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
73669994 117114 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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
10140871 58924 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10224745 112180 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
10647373 96510 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.7 pIC50 = 6.7 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
CHEMBL273391 209054 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
CHEMBL273391 209054 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
44284238 99652 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.7 pIC50 = 7.7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
9874557 129203 0 None - 2 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.7 pIC50 = 7.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44311516 202409 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 7.7 pIC50 = 7.7 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
71453357 81256 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 7.7 pIC50 = 7.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44328057 96433 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
11732966 201472 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.7 pIC50 = 6.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44279309 161256 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.7 pIC50 = 6.7 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
44334097 109567 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 6.7 pIC50 = 6.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44371460 49250 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
CHEMBL319537 209463 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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](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
10815005 9641 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 492 6 1 6 5.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm9606507
54587165 59975 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 5.7 pIC50 = 5.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
CHEMBL315047 209430 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
44295114 14696 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.7 pIC50 = 5.7 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.7 pIC50 = 5.7 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
10768294 14404 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 5.7 pIC50 = 5.7 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 5.7 pIC50 = 5.7 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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
19010490 53238 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 5.7 pIC50 = 5.7 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
44368480 44341 0 None - 0 Pig 4.7 pIC50 = 4.7 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 4.7 pIC50 = 4.7 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
10837347 8766 0 None - 0 Pig 4.7 pIC50 = 4.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.7 pIC50 = 4.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10841134 60112 0 None - 0 Pig 4.7 pIC50 = 4.7 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.7 pIC50 = 4.7 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
CHEMBL414165 211357 0 None - 0 Pig 4.7 pIC50 = 4.7 Binding
Inhibitory effect against porcine Endothelin B receptorInhibitory effect against porcine Endothelin B 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
159594 518 38 None - 3 Pig 6.7 pIC50 = 6.7 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 - 3 Pig 6.7 pIC50 = 6.7 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 - 3 Pig 6.7 pIC50 = 6.7 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 - 3 Pig 6.7 pIC50 = 6.7 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44439111 96715 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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 5.7 pIC50 = 5.7 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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
10622380 100972 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
21041372 81274 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
71462246 81265 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
3951 388 82 None 1 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
44384766 59338 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10576888 170268 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10211781 129206 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
73669820 117112 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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
10697883 11120 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.7 pIC50 = 4.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
137639474 156343 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 5.7 pIC50 = 5.7 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
52949155 18212 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 5.7 pIC50 = 5.7 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
10122495 30640 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9870117 193207 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
9870117 193207 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 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 Pig 8.7 pIC50 = 8.7 Binding
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 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
9831249 59370 0 None - 2 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 8.7 pIC50 = 8.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10720982 127282 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.7 pIC50 = 8.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.7 pIC50 = 8.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
44314889 103254 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
9808545 11332 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.7 pIC50 = 8.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.7 pIC50 = 8.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
44314579 102431 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44283270 167307 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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
CHEMBL414047 211347 0 None - 0 Bovine 8.6 pIC50 = 8.6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
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](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CC(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)NCC(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N2CCC[C@@H]2C(=O)N1)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/S0960-894X(97)00296-5
44314750 165089 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44283419 99840 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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
10603546 109945 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.6 pIC50 = 8.6 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10625694 11326 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.6 pIC50 = 8.6 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.6 pIC50 = 8.6 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
11123269 204567 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 452 6 1 5 5.8 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
44314664 202980 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.6 pIC50 = 8.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
10555516 9136 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.5 pIC50 = 8.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
44314904 102659 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.5 pIC50 = 8.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44314905 203328 0 None - 0 Pig 8.5 pIC50 = 8.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.5 pIC50 = 8.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
10649119 11318 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 7.7 pIC50 = 7.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 7.7 pIC50 = 7.7 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
CHEMBL317099 209442 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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](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
44298382 193432 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
10792316 167906 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.7 pIC50 = 7.7 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
CHEMBL313984 209367 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
56671734 62984 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
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 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
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
44284236 121796 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.7 pIC50 = 7.7 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
21462927 119724 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
9825494 200914 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at human Endothelin B receptorBinding affinity at human Endothelin B 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 6.7 pIC50 = 6.7 Binding
Binding affinity at human Endothelin B receptorBinding affinity at human Endothelin B 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
10896413 100128 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.7 pIC50 = 6.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11755275 198316 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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
10627272 202349 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
44311527 202414 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 6.7 pIC50 = 6.7 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
44327868 110943 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
10791694 97735 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
9934580 162368 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
10765057 162598 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 430 4 1 7 3.5 O=C1OC(O)(c2ccc3c(c2)OCO3)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
19735343 175467 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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 5.7 pIC50 = 5.7 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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
CHEMBL86814 214105 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
CHEMBL1791279 207166 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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
44383753 59736 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.7 pIC50 = 5.7 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44327661 164027 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.7 pIC50 = 5.7 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
44316515 203285 2 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.7 pIC50 = 4.7 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
18617288 203426 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.7 pIC50 = 4.7 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 316 3 1 4 2.5 Cc1noc(NS(=O)(=O)c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
11800804 161275 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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 4.7 pIC50 = 4.7 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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
104865 697 94 None -6 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B 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
104865 697 94 None -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 -6 4 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10122033 81251 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
58688005 174378 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
10144372 165490 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
22467229 98487 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.7 pIC50 = 6.7 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
44320338 106478 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 5.7 pIC50 = 5.7 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
10281192 60736 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
71462245 81240 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44177614 129116 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10479787 59288 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.7 pIC50 = 5.7 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
151174 201023 37 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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 7.7 pIC50 = 7.7 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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
44334130 4427 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.7 pIC50 = 7.7 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
10745564 6133 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 6.7 pIC50 = 6.7 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
CHEMBL263295 208810 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
44304492 96099 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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 6.7 pIC50 = 6.7 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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
18738880 167600 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.7 pIC50 = 6.7 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
21041283 172566 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
10960638 100586 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44279371 99449 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
10814743 178781 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.7 pIC50 = 5.7 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10555424 202329 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
44266568 97633 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
CHEMBL133257 206963 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory effect against Human Endothelin B receptorInhibitory effect against Human Endothelin B 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
44383537 58922 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B 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 4.7 pIC50 = 4.7 Binding
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B 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
10648937 205565 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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 6.7 pIC50 = 6.7 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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
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 ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
23445358 111062 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.7 pIC50 = 4.7 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 412 4 1 5 4.6 Cc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
44352079 116028 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
137649809 156833 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 5.7 pIC50 = 5.7 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
23548253 81250 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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 6.7 pIC50 = 6.7 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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
23548253 81250 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
76330201 84911 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
44214320 84912 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.7 pIC50 = 6.7 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
CHEMBL2304017 207718 0 None - 0 Pig 7.7 pIC50 = 7.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
11059576 201593 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.7 pIC50 = 6.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44295097 14579 0 None - 0 Pig 6.7 pIC50 = 6.7 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.7 pIC50 = 6.7 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.7 pIC50 = 6.7 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
11827880 10115 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 6.7 pIC50 = 6.7 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 6.7 pIC50 = 6.7 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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
10552548 98057 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.7 pIC50 = 5.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2OC)cc1 10.1021/jm9606507
11145841 100474 0 None - 0 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.7 pIC50 = 5.7 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
18738879 89788 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 5.7 pIC50 = 5.7 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
15340617 98767 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 5.7 pIC50 = 5.7 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
18617379 203503 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.7 pIC50 = 4.7 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
44276948 106340 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.7 pIC50 = 4.7 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
9845967 10974 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 4.7 pIC50 = 4.7 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 4.7 pIC50 = 4.7 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 4.7 pIC50 = 4.7 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
44385941 130141 0 None - 0 Pig 4.7 pIC50 = 4.7 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.7 pIC50 = 4.7 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
44266532 4419 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
10282163 60077 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9932004 97712 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.7 pIC50 = 6.7 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 422 5 1 6 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCC2)cc1 10.1021/jm9606507
44458604 98148 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.6 pIC50 = 6.6 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
44386161 60932 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.6 pIC50 = 5.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
CHEMBL2304008 207709 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44284391 138758 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.6 pIC50 = 7.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
18995991 99823 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.6 pIC50 = 6.6 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
44279127 99015 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
19010493 97891 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 6.6 pIC50 = 6.6 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
11048815 101832 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)OC(c1ccc3c(c1)OCO3)C(C(=O)O)=C2c1ccc(OC)cc1 10.1021/jm010382z
10862228 201263 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 398 7 1 6 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC)cc21 10.1021/jm010382z
10722371 101745 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
44316768 203522 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
443289 702 40 None - 3 Pig 4.6 pIC50 = 4.6 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.
ChEMBL None None None None 10.1021/jm00087a001
997 702 40 None - 3 Pig 4.6 pIC50 = 4.6 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL314691 702 40 None - 3 Pig 4.6 pIC50 = 4.6 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.
ChEMBL None None None None 10.1021/jm00087a001
DB12054 702 40 None - 3 Pig 4.6 pIC50 = 4.6 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.
ChEMBL None None None None 10.1021/jm00087a001
10478562 131263 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 4.6 pIC50 = 4.6 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
10717279 96587 0 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 4.6 pIC50 = 4.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10122675 98007 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10742024 96482 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
135884434 130030 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9810571 61042 0 None - 2 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.6 pIC50 = 7.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
18184194 130027 0 None - 2 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.6 pIC50 = 7.6 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44368819 168315 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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 6.6 pIC50 = 6.6 Binding
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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 6.6 pIC50 = 6.6 Binding
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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
10815823 9689 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.6 pIC50 = 6.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
44298304 101072 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
44298409 193318 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
CHEMBL2304018 207719 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
76319370 84918 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.6 pIC50 = 6.6 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
10886132 9701 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 6.6 pIC50 = 6.6 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 6.6 pIC50 = 6.6 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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
10440821 205794 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
44279351 99469 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
44279129 106499 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
22998446 106137 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)c1Br 10.1016/S0960-894X(96)00496-9
44277263 106341 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 5.6 pIC50 = 5.6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
10744085 102384 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
44327727 167623 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
44386536 130178 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
44266655 4959 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
18617363 163997 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
5344 172891 98 None - 1 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
15453210 203525 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
44276596 106346 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.6 pIC50 = 4.6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
44276907 106359 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.6 pIC50 = 4.6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
10146377 60078 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
71449713 81242 21 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.6 pIC50 = 5.6 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10575061 205156 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.6 pIC50 = 5.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
22467266 84908 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.6 pIC50 = 6.6 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
23445366 105689 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 5.6 pIC50 = 5.6 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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
CHEMBL2370070 208024 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
71455140 81582 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.6 pIC50 = 5.6 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
71456865 81276 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.6 pIC50 = 5.6 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44284405 99879 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.6 pIC50 = 7.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
44284328 127006 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.6 pIC50 = 7.6 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
9939238 202419 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 7.6 pIC50 = 7.6 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
44311345 202507 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 7.6 pIC50 = 7.6 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
CHEMBL85341 214101 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
15411009 106693 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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 5.6 pIC50 = 5.6 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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
10938122 162444 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
135415889 58942 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.6 pIC50 = 5.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44266542 162248 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
18617351 103619 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
18617407 203262 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10788853 6018 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)cc3OC)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10766396 110077 0 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.6 pIC50 = 4.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
44276886 106337 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.6 pIC50 = 4.6 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
44459272 90795 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 5.6 pIC50 = 5.6 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
10279940 100868 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.6 pIC50 = 4.6 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10504920 162548 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.6 pIC50 = 4.6 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
44384611 128119 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44314647 203366 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
10745418 113480 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
44320461 105855 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 7.6 pIC50 = 7.6 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
10118046 9330 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 6.6 pIC50 = 6.6 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
44327659 109321 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
CHEMBL96822 214133 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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](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
10789524 5106 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.6 pIC50 = 6.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2)cc1 10.1021/jm9606507
10530409 5615 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.6 pIC50 = 6.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
73669821 117111 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of S6c from rat ETB receptor after 1 hr by Lowry methodDisplacement of S6c from rat ETB 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 6.6 pIC50 = 6.6 Binding
Displacement of S6c from rat ETB receptor after 1 hr by Lowry methodDisplacement of S6c from rat ETB 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
44295177 14597 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.6 pIC50 = 6.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.6 pIC50 = 6.6 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
10789525 61426 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
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 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
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
10346184 9091 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
CHEMBL315328 209433 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL87252 214107 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None None 10.1021/jm00070a001
18936171 194821 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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
44327252 205790 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
44327226 206168 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.6 pIC50 = 5.6 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
22616258 104914 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
9870959 8814 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 4.6 pIC50 = 4.6 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10625152 109957 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44386621 60933 0 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.6 pIC50 = 4.6 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
11801544 61433 0 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.6 pIC50 = 4.6 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
44385805 60952 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.6 pIC50 = 5.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10552413 110166 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10346184 9091 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
21462925 119421 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 7.6 pIC50 = 7.6 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
CHEMBL2304011 207712 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
CHEMBL2369709 207897 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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
44371421 51145 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
10412464 9034 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.6 pIC50 = 5.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
10961720 201782 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44314461 203061 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 5.6 pIC50 = 5.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
10216862 194728 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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
CHEMBL265066 96354 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Tested for its inhibitory activity against Endothelin B receptorTested for its inhibitory activity against Endothelin B 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
22616257 203295 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 272 3 1 4 2.4 Cc1noc(NS(=O)(=O)c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
44316831 203794 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10070783 96596 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 4.6 pIC50 = 4.6 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
10502226 101045 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.6 pIC50 = 4.6 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10719007 11122 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.6 pIC50 = 4.6 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.6 pIC50 = 4.6 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10646637 205309 0 None - 0 Pig 4.6 pIC50 = 4.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 4.6 pIC50 = 4.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10347080 84789 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.6 pIC50 = 6.6 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
44314646 203320 0 None - 0 Pig 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 7.6 pIC50 = 7.6 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
11766844 109280 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 7.6 pIC50 = 7.6 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 7.6 pIC50 = 7.6 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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
10212088 96235 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9957883 98191 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.6 pIC50 = 6.6 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
44279370 106709 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
104865 697 94 None -6 4 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 -6 4 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 -6 4 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 -6 4 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 -6 4 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
11091217 100585 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cc(OCCC)ccc21 10.1021/jm010382z
11014820 201214 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10894688 201803 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 402 4 1 5 4.4 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)c1 10.1021/jm010382z
44298325 193994 0 None - 0 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 5.6 pIC50 = 5.6 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
44311218 102639 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 5.6 pIC50 = 5.6 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
10278777 167558 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 5.6 pIC50 = 5.6 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
23445284 112292 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.6 pIC50 = 4.6 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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
71455060 81237 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.6 pIC50 = 5.6 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44265861 96747 0 None - 0 Pig 6.6 pIC50 = 6.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.6 pIC50 = 6.6 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10553384 109167 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
25211074 18284 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 5.5 pIC50 = 5.5 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
25211074 18284 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in membranes by radioligand assayAntagonist activity at ETB 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 5.5 pIC50 = 5.5 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in membranes by radioligand assayAntagonist activity at ETB 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
44215416 174498 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
10205429 61262 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
23445408 111132 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 5.5 pIC50 = 5.5 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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
CHEMBL2304006 207707 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell 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
CHEMBL2304017 207718 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell 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
70240112 171027 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
21041288 173344 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
CHEMBL406279 210845 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
44294712 14608 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
44284381 127974 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 6.5 pIC50 = 6.5 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
17869371 14605 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.5 pIC50 = 5.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.5 pIC50 = 5.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
10457385 112178 0 None - 1 Pig 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
10527706 96540 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
18995990 98884 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 4.5 pIC50 = 4.5 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
18617385 203491 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.5 pIC50 = 4.5 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
44277387 106354 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.5 pIC50 = 4.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
10366742 106611 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 5.5 pIC50 = 5.5 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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
10715441 175343 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10697636 167246 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
135512539 127939 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10529715 205411 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44384852 59909 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
CHEMBL67074 201911 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Tested for its ability to inhibit the binding of [125I]ET1 to the Endothelin B receptor in rat cerebellum membranes.Tested for its ability to inhibit the binding of [125I]ET1 to the Endothelin B receptor in rat cerebellum 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
44386162 60073 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44383754 59554 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44383742 167929 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44339662 9744 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44385523 60723 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.5 pIC50 = 6.5 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
17885918 105480 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccsc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
44320431 106460 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
10723203 11330 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
9961347 11842 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
44320212 106504 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
10768904 12009 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
10555208 12284 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.5 pIC50 = 8.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
17885921 106305 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccn2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
155511294 168991 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
9985589 167669 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 576 9 1 8 5.0 CCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
CHEMBL433700 167669 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 576 9 1 8 5.0 CCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
44315008 102345 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity rowards Endothelin B receptor in human girardi heart cell membranesBinding affinity rowards Endothelin B receptor in human girardi heart cell 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 8.4 pIC50 = 8.4 Binding
Binding affinity rowards Endothelin B receptor in human girardi heart cell membranesBinding affinity rowards Endothelin B receptor in human girardi heart cell 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
10792636 167939 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
CHEMBL408437 210956 0 None - 0 Bovine 8.4 pIC50 = 8.4 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
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](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CC(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)NCC(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N2CCC[C@@H]2C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/S0960-894X(97)00296-5
10769177 112400 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
11006532 12122 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 8.4 pIC50 = 8.4 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 8.4 pIC50 = 8.4 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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
10119177 116949 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 7.5 pIC50 = 7.5 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
44327890 140868 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
CHEMBL146155 207023 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
44333913 5017 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.5 pIC50 = 7.5 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44371410 49141 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
11827657 19169 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 6.5 pIC50 = 6.5 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
44279126 100247 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
44279128 106416 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
44279349 167573 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
44298393 198139 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
44309996 202055 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
9870830 204977 34 None -66 2 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 -66 2 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
44387128 168013 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 6.5 pIC50 = 6.5 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
44371571 118971 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
CHEMBL414168 211358 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
CHEMBL436894 211935 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
CHEMBL437610 211969 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
10767505 5213 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.5 pIC50 = 5.5 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
10601191 112294 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 492 11 3 6 5.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc(C(=O)O)[nH]n1 10.1021/jm9707131
CHEMBL293874 209137 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding activity against Endothelin B receptor 0f Porcine cerebellum membranesBinding activity against Endothelin B receptor 0f Porcine cerebellum 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
22616255 203812 11 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.5 pIC50 = 4.5 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
345351 9254 1 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 4.5 pIC50 = 4.5 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
44298419 161438 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 420 3 1 4 3.7 Cc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1I 10.1016/s0960-894x(00)00366-8
CHEMBL415942 161438 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 420 3 1 4 3.7 Cc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1I 10.1016/s0960-894x(00)00366-8
44386370 60079 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
CHEMBL342615 209919 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory effect against porcine Endothelin B receptorInhibitory effect against porcine Endothelin B 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
10347080 84789 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.5 pIC50 = 6.5 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
10576379 100788 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10790376 166345 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
11827489 116472 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
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 5.5 pIC50 = 5.5 Binding
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
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
9916121 81241 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.5 pIC50 = 5.5 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10792319 205494 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44265869 96800 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
23445457 128489 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 5.5 pIC50 = 5.5 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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
10962637 9969 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
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 Human 7.5 pIC50 = 7.5 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
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 Human 7.5 pIC50 = 7.5 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
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
10531506 11995 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 7.5 pIC50 = 7.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 7.5 pIC50 = 7.5 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
CHEMBL2304013 207714 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44320474 106572 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 7.5 pIC50 = 7.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
104865 697 94 None -6 4 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B 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 -6 4 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B 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 -6 4 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B 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 -6 4 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B 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 -6 4 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
44298330 101065 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
44458650 84465 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.5 pIC50 = 6.5 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
155544917 172832 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
11732155 200970 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 402 4 1 5 4.4 COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
10672060 9155 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
19385674 98124 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 4.5 pIC50 = 4.5 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 4.5 pIC50 = 4.5 Binding
Inhibitory concentration against endothelin receptor type BInhibitory concentration against endothelin receptor type B
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 4.5 pIC50 = 4.5 Binding
Inhibitory concentration against endothelin receptor type BInhibitory concentration against endothelin receptor type B
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
52943105 18278 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 5.5 pIC50 = 5.5 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
10744973 205535 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
155517241 169580 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
44265870 205827 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.5 pIC50 = 6.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44384715 60028 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10671928 7180 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.5 pIC50 = 5.5 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 467 5 1 7 4.4 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2nccc3ccccc23)cc1 10.1021/jm9606507
44295089 14448 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.5 pIC50 = 5.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.5 pIC50 = 5.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
15340613 106348 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
10837666 169310 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
9870959 8814 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 4.5 pIC50 = 4.5 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
71451529 81267 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.5 pIC50 = 6.5 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
18184228 61009 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.5 pIC50 = 6.5 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44384651 127964 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
10696210 99074 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
11795139 165973 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
23445516 106133 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 5.5 pIC50 = 5.5 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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
44384757 165584 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
CHEMBL216082 207562 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
CHEMBL2370255 208064 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
9830495 130614 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.5 pIC50 = 7.5 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
CHEMBL94907 214127 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
11505449 170908 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
44309814 102519 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
9909467 203790 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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 5.5 pIC50 = 5.5 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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
CHEMBL86814 214105 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
44213279 106352 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 5.5 pIC50 = 5.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
CHEMBL86814 214105 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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](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
44266549 161805 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
44316458 203720 2 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.5 pIC50 = 4.5 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
44277034 106347 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.5 pIC50 = 4.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
10576910 108039 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44384826 59646 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
22998456 59467 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 6.5 pIC50 = 6.5 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
10694547 205336 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10507467 8400 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.5 pIC50 = 7.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
44314660 103873 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 7.5 pIC50 = 7.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
22467235 96065 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 7.5 pIC50 = 7.5 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
10050696 96317 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 7.5 pIC50 = 7.5 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
73669992 117115 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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
23670447 2968 2 None - 2 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
10311570 14446 0 None - 1 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
44295206 14609 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.5 pIC50 = 6.5 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
9871348 202320 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
18617366 167262 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
11102609 167994 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10790183 204512 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10673715 9445 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10789715 112586 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
CHEMBL2369711 207899 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=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](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
10697633 60000 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
10415348 60747 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
10697633 60000 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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
71456862 81257 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.5 pIC50 = 6.5 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10274552 73151 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
9807200 84907 0 None -346 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.5 pIC50 = 6.5 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
71458720 81258 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.5 pIC50 = 5.5 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
23445533 60076 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.5 pIC50 = 5.5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
10896412 201107 0 None - 0 Pig 7.5 pIC50 = 7.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.5 pIC50 = 7.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
CHEMBL327350 209534 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
44327585 161222 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
44368824 96366 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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 6.5 pIC50 = 6.5 Binding
Binding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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 6.5 pIC50 = 6.5 Binding
Binding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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
10982740 201683 0 None - 0 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.5 pIC50 = 6.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44371429 48621 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
11762291 100156 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
9807178 201293 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.5 pIC50 = 5.5 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10648006 161105 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.5 pIC50 = 5.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
CHEMBL438194 211995 7 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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](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
9848132 205833 0 None - 2 Pig 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 - 2 Pig 5.5 pIC50 = 5.5 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
44368417 44382 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 4.5 pIC50 = 4.5 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
18617302 103924 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.5 pIC50 = 4.5 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccccc2F)c1Br 10.1016/0960-894X(96)00441-6
44298394 162473 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 340 4 1 5 3.8 CSc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)noc1C 10.1016/s0960-894x(00)00366-8
CHEMBL417595 162473 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 340 4 1 5 3.8 CSc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)noc1C 10.1016/s0960-894x(00)00366-8
10575356 9602 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10298764 9746 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10647182 109221 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10765567 110853 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.5 pIC50 = 4.5 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10415822 129284 0 None - 0 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
44384610 127936 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.5 pIC50 = 6.5 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10813822 96509 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
22998447 204938 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.5 pIC50 = 4.5 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 414 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2sccc2Oc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
10226215 100949 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.5 pIC50 = 4.5 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10648715 109168 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10598270 96483 0 None - 0 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.5 pIC50 = 5.5 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10302092 110836 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.4 pIC50 = 7.4 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
CHEMBL267754 208975 0 None - 0 Bovine 7.4 pIC50 = 7.4 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
CHEMBL327350 209534 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
10907399 201258 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.4 pIC50 = 5.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 516 11 1 6 6.8 CCCCOc1ccc(C2Oc3ccc(OCCCC)cc3C(c3ccc4c(c3)OCO4)=C2C(=O)O)cc1 10.1021/jm010382z
10577405 9546 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10767280 108168 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44277367 106342 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.4 pIC50 = 4.4 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
10168195 61043 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
18184179 128487 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.4 pIC50 = 5.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
CHEMBL421190 211511 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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
CHEMBL94525 214124 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCCN)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
18617322 203739 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.4 pIC50 = 4.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1Br 10.1016/0960-894X(96)00441-6
44385593 128939 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.4 pIC50 = 4.4 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
10839533 100962 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10742446 205274 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
71460535 81259 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10624915 204500 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
9938571 9491 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B 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 Human 7.4 pIC50 = 7.4 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B 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 Human 7.4 pIC50 = 7.4 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B 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 Human 7.4 pIC50 = 7.4 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B 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/jm0102304
CHEMBL112531 9491 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B 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/jm0102304
CHEMBL369489 9491 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B 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/jm0102304
9807691 99589 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
18617344 203557 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.4 pIC50 = 5.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
18617395 203551 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.4 pIC50 = 4.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10789279 204829 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44327347 96302 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
10765171 7798 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.4 pIC50 = 5.4 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)c(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10503921 100993 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
18617318 105121 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.4 pIC50 = 4.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2ccccc2Br)c1Br 10.1016/0960-894X(96)00441-6
44277245 106351 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 4.4 pIC50 = 4.4 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
16004692 2411 85 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
16004692 2411 85 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
9915510 84717 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.4 pIC50 = 6.4 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
9873255 59307 0 None - 2 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.4 pIC50 = 6.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10719598 205252 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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 6.4 pIC50 = 6.4 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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
44339655 9003 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 4.4 pIC50 = 4.4 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
23445254 205416 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.4 pIC50 = 4.4 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 412 5 1 5 4.2 Cc1noc(NS(=O)(=O)c2sccc2Cc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
10599230 205257 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.4 pIC50 = 6.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44314904 102659 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell 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 8.4 pIC50 = 8.4 Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell 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
10529868 163628 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
9917706 129204 0 None - 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
44320777 204473 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.4 pIC50 = 8.4 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
9897092 59606 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 8.4 pIC50 = 8.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9810400 98142 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 8.4 pIC50 = 8.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9917706 129204 0 None - 2 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 8.4 pIC50 = 8.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10209779 162867 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.4 pIC50 = 8.4 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
44314659 203400 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
9894460 204972 6 None -41 3 Human 8.4 pIC50 = 8.4 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 -41 3 Human 8.4 pIC50 = 8.4 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 -41 3 Human 8.4 pIC50 = 8.4 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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
10303555 162817 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.4 pIC50 = 8.4 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
1009 192 20 None - 1 Human 8.4 pIC50 = 8.4 Binding
Affinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRBAffinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRB
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 nan
5310991 192 20 None - 1 Human 8.4 pIC50 = 8.4 Binding
Affinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRBAffinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRB
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 nan
CHEMBL332794 192 20 None - 1 Human 8.4 pIC50 = 8.4 Binding
Affinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRBAffinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRB
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 nan
44315009 102718 0 None - 0 Pig 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.4 pIC50 = 8.4 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44314675 97663 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44314676 102438 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
17885919 204674 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.3 pIC50 = 8.3 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
44320171 106461 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.3 pIC50 = 8.3 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
10252787 98796 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 7.4 pIC50 = 7.4 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
CHEMBL1790519 207140 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar 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)[C@@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC 10.1021/jm970161m
10648937 205565 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44327466 95991 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
11103152 162677 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10364227 201102 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11059349 201806 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44298279 193272 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
10239569 14604 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.4 pIC50 = 6.4 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.4 pIC50 = 6.4 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
10364227 201102 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
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 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
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
18617355 203236 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.4 pIC50 = 5.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
11026419 201483 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.4 pIC50 = 5.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
CHEMBL2370070 208024 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
CHEMBL315047 209430 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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](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
10718385 205074 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10550844 96847 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 4.4 pIC50 = 4.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10553316 96616 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.4 pIC50 = 6.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10205245 71850 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
137642741 157682 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 5.4 pIC50 = 5.4 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
10005597 119300 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
10531650 167687 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.4 pIC50 = 7.4 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
9852318 9508 5 None - 2 Pig 7.4 pIC50 = 7.4 Binding
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 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 Pig 7.4 pIC50 = 7.4 Binding
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 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 Pig 7.4 pIC50 = 7.4 Binding
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 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
10578320 96848 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 7.4 pIC50 = 7.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10917653 201677 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
9821701 4529 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 6.4 pIC50 = 6.4 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
10767586 9662 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 5.4 pIC50 = 5.4 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10602183 9134 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44383537 58922 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Tested for binding affinity towards human Endothelin B receptorTested for binding affinity towards human Endothelin B 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 4.4 pIC50 = 4.4 Binding
Tested for binding affinity towards human Endothelin B receptorTested for binding affinity towards human Endothelin B 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
23445430 60725 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.4 pIC50 = 5.4 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44384652 60941 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.4 pIC50 = 5.4 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
155519384 169839 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
71458719 81252 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 7.4 pIC50 = 7.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10146640 205810 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10366278 171887 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.4 pIC50 = 7.4 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44278215 99084 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
18995986 99107 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.4 pIC50 = 6.4 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
44270522 45533 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 6.4 pIC50 = 6.4 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
44284183 139032 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 6.4 pIC50 = 6.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
44386069 59408 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.4 pIC50 = 6.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44291495 11114 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
44213923 107782 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
11799440 205238 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.4 pIC50 = 5.4 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10506868 62912 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.4 pIC50 = 4.4 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
10553384 109167 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 4.4 pIC50 = 4.4 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
76308472 84916 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
71451527 81254 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
23445313 165074 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 5.4 pIC50 = 5.4 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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
23445421 59600 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.4 pIC50 = 5.4 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
11005242 201197 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.4 pIC50 = 7.4 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44212539 202385 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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 7.4 pIC50 = 7.4 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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
44284288 99660 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.4 pIC50 = 7.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
44284266 136396 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.4 pIC50 = 7.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
44212539 202385 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 7.4 pIC50 = 7.4 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
44371449 49098 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
44298278 192991 0 None - 0 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.4 pIC50 = 6.4 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
44371670 141119 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) 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 5.4 pIC50 = 5.4 Binding
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) 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
CHEMBL432091 211874 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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](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
CHEMBL432091 211874 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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
10792785 166159 0 None - 0 Pig 4.4 pIC50 = 4.4 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.4 pIC50 = 4.4 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
23445221 201397 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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 4.4 pIC50 = 4.4 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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
10529742 8093 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10672494 178963 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.4 pIC50 = 5.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
23445354 204899 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.4 pIC50 = 4.4 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 426 5 1 5 4.8 CCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
52944276 18230 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
10674642 112858 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
44320291 105445 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 7.4 pIC50 = 7.4 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
10281573 59645 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9939960 174992 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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 6.4 pIC50 = 6.4 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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
44320444 204707 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
44309897 202915 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
9936145 18822 1 None - 1 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
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 5.4 pIC50 = 5.4 Binding
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
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
44327890 140868 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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 5.4 pIC50 = 5.4 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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
44266537 4247 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
71462320 81578 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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 6.4 pIC50 = 6.4 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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
71462320 81578 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.4 pIC50 = 6.4 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10674176 162138 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.4 pIC50 = 6.4 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
18184256 128948 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.4 pIC50 = 6.4 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10740439 172169 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.4 pIC50 = 4.4 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
23445379 129564 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 5.4 pIC50 = 5.4 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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
CHEMBL407422 210904 0 None - 0 Bovine 7.4 pIC50 = 7.4 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
44284184 139457 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.4 pIC50 = 7.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
CHEMBL409433 211006 0 None - 0 Bovine 6.4 pIC50 = 6.4 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
44458399 98522 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.4 pIC50 = 6.4 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
CHEMBL313382 209357 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
CHEMBL87243 214106 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
10288713 101560 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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
10160887 99673 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 5.4 pIC50 = 5.4 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
10600668 5074 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.4 pIC50 = 5.4 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1cc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc(OC)c1OC 10.1021/jm9606507
10840410 202353 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
44327237 206181 0 None - 0 Pig 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.4 pIC50 = 5.4 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
18617327 203535 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.4 pIC50 = 4.4 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1ccccc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
44439108 166550 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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
22010352 117110 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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
44339655 9003 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
11742628 97770 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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
9845967 10974 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.3 pIC50 = 5.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.3 pIC50 = 5.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 5.3 pIC50 = 5.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
71455064 81270 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
71460621 81575 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10527706 96540 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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 5.3 pIC50 = 5.3 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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
44386002 59963 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.3 pIC50 = 5.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
11015826 201828 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10626646 16254 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
10240093 81261 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44295224 14447 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
CHEMBL316092 209439 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
15453209 203411 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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 4.3 pIC50 = 4.3 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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
71451526 81249 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
67952994 81580 11 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10145418 81246 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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
10145418 81246 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44386163 60046 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
71453356 81239 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44439106 153061 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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
10579100 165777 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 7.3 pIC50 = 7.3 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 7.3 pIC50 = 7.3 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
10006086 120536 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 6.3 pIC50 = 6.3 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
CHEMBL414131 211355 0 None - 0 Bovine 6.3 pIC50 = 6.3 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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](C)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
11059249 102132 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 440 10 1 6 5.3 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCCC)cc21 10.1021/jm010382z
11733231 201147 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
CHEMBL431433 211867 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
18617340 104911 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
44279439 106881 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
CHEMBL303204 209163 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding activity against Endothelin B receptor 0f Porcine cerebellum membranesBinding activity against Endothelin B receptor 0f Porcine cerebellum 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
44317005 203307 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.3 pIC50 = 4.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10116355 8167 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
11799503 9646 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10095637 49682 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 4.3 pIC50 = 4.3 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
44459247 87581 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.3 pIC50 = 6.3 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
10649546 108114 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44284405 99879 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.3 pIC50 = 7.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
9870830 204977 34 None -66 2 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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 6.3 pIC50 = 6.3 Binding
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 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
10971938 201278 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44295156 14443 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
44284199 99635 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 6.3 pIC50 = 6.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
10961277 100535 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.3 pIC50 = 5.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10788494 170046 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.3 pIC50 = 5.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
CHEMBL133257 206963 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Inhibitory effect against porcine Endothelin B receptorInhibitory effect against porcine Endothelin B 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
44339840 9183 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10816110 108066 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10530156 9451 0 None - 0 Pig 4.3 pIC50 = 4.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.3 pIC50 = 4.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10579210 168015 0 None - 0 Pig 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
10673969 61761 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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
22998414 201318 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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 4.3 pIC50 = 4.3 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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
10231591 130825 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44311232 202399 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 7.3 pIC50 = 7.3 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
18995989 100076 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.3 pIC50 = 6.3 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
10426645 162513 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
11728313 162712 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.3 pIC50 = 5.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 368 6 1 5 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
44368396 44325 0 None - 0 Pig 4.3 pIC50 = 4.3 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 4.3 pIC50 = 4.3 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
10357554 97102 1 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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 4.3 pIC50 = 4.3 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1016/0960-894X(96)00441-6
44316973 203883 2 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.3 pIC50 = 4.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
44439114 161069 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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
10812400 97914 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10816667 11324 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.3 pIC50 = 8.3 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.3 pIC50 = 8.3 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
10768903 12013 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.3 pIC50 = 8.3 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.3 pIC50 = 8.3 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
44314579 102431 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell 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 8.3 pIC50 = 8.3 Binding
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell 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
44314722 155198 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44283421 99681 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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
9809919 202694 0 None - 2 Human 8.3 pIC50 = 8.3 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 8.3 pIC50 = 8.3 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
10209320 9180 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.3 pIC50 = 8.3 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10579303 9325 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.3 pIC50 = 8.3 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
44314864 102549 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44314751 160796 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.3 pIC50 = 8.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44283349 99849 0 None - 0 Pig 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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 8.3 pIC50 = 8.3 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum 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
44284437 99509 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 8.3 pIC50 = 8.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
10506430 113278 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
CHEMBL313984 209367 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
10188517 61422 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
9850566 4115 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
44298305 192980 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
44298277 193319 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
44298988 100239 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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
3911 3253 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
CHEMBL429908 3253 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
CHEMBL329609 209562 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)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
10649266 9526 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 5.3 pIC50 = 5.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
22010244 205064 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B 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 5.3 pIC50 = 5.3 Binding
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
10649585 109272 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.3 pIC50 = 4.3 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44383592 59573 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B receptor
ChEMBL 386 4 1 5 3.6 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
CHEMBL173059 59573 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B receptor
ChEMBL 386 4 1 5 3.6 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
44265853 204666 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
21979593 81579 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
71455139 81577 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.3 pIC50 = 5.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10391487 9555 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
CHEMBL319660 209464 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)C(c1ccccc1)c1ccccc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
44284115 99719 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.3 pIC50 = 7.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
10391487 9555 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 5.3 pIC50 = 5.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
44266903 14402 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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
44387124 130356 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
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 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
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
159594 518 38 None -4073 3 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 -4073 3 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 -4073 3 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 -4073 3 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
21041273 173166 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
10575845 11110 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.3 pIC50 = 4.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.3 pIC50 = 4.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
CHEMBL97470 214138 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)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
11732669 201418 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCC)cc21 10.1021/jm010382z
44298343 101310 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
159594 518 38 None - 3 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 - 3 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 - 3 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 - 3 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
44371420 50622 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 5.3 pIC50 = 5.3 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
9888574 103686 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10429404 104386 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10670372 96785 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)cc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44327423 205797 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.3 pIC50 = 5.3 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
10915215 100323 0 None - 0 Pig 4.3 pIC50 = 4.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 4.3 pIC50 = 4.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44305079 101608 0 None - 0 Pig 4.3 pIC50 = 4.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 4.3 pIC50 = 4.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
21041249 81236 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.3 pIC50 = 5.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44384656 129560 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.3 pIC50 = 5.3 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
21979601 81574 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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
21979601 81574 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10647372 205378 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
CHEMBL2304016 207717 0 None - 0 Pig 7.3 pIC50 = 7.3 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44333889 4999 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.3 pIC50 = 7.3 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44334084 109152 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 6.3 pIC50 = 6.3 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
18617333 105035 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.3 pIC50 = 5.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
44309488 202302 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B 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
10814655 205856 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.3 pIC50 = 6.3 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44385127 61024 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Tested for the inhibitory activity of cloned human ETB receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for the inhibitory activity of cloned human ETB 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 5.3 pIC50 = 5.3 Binding
Tested for the inhibitory activity of cloned human ETB receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for the inhibitory activity of cloned human ETB 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
CHEMBL409339 211004 0 None - 0 Bovine 7.3 pIC50 = 7.3 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
44284115 99719 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.3 pIC50 = 7.3 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
11826173 201123 1 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44298956 193997 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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
44270602 98389 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 6.3 pIC50 = 6.3 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
10553165 9633 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 492 7 1 6 5.4 O=C1OC(O)(c2ccc(OCc3ccccc3)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
44276946 106350 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 5.3 pIC50 = 5.3 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
10650062 60108 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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
18184206 59998 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
155564169 174751 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
42630655 18208 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
42630655 18208 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
17869231 14442 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
44327412 205837 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 6.3 pIC50 = 6.3 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
44367767 43486 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 469 9 2 6 4.5 COc1ccc(CN(Cc2cc3c(cc2Cl)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL151064 43486 0 None - 0 Pig 5.3 pIC50 = 5.3 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 469 9 2 6 4.5 COc1ccc(CN(Cc2cc3c(cc2Cl)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
10814746 181002 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.3 pIC50 = 5.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
44368481 120993 0 None - 0 Pig 4.3 pIC50 = 4.3 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 4.3 pIC50 = 4.3 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
9840391 104047 6 None - 1 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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 4.3 pIC50 = 4.3 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
10721386 60041 0 None - 0 Pig 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
44386535 130830 0 None - 0 Pig 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
CHEMBL414165 211357 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibitory effect against Human Endothelin B receptorInhibitory effect against Human Endothelin B 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
71451528 81263 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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
71451528 81263 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
71462248 81277 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
21041307 174387 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
CHEMBL265116 208880 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
44298324 194186 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 6.3 pIC50 = 6.3 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
9869444 96784 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 5.3 pIC50 = 5.3 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
10769045 130682 0 None - 0 Pig 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.3 pIC50 = 4.3 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
71455065 81273 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
137655285 158419 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.3 pIC50 = 6.3 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
23445219 111970 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.3 pIC50 = 4.3 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 428 5 1 6 4.3 COc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
10129267 81262 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44384723 130352 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.3 pIC50 = 5.3 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
58688008 174720 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
155563100 174694 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
10281929 9288 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10816152 16142 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.2 pIC50 = 7.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
9826741 100277 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 5.2 pIC50 = 5.2 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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
44327734 206350 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.2 pIC50 = 5.2 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
10265127 96375 2 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.2 pIC50 = 4.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10076527 14431 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 6.2 pIC50 = 6.2 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
22467237 84905 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
9826741 100277 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 ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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 5.2 pIC50 = 5.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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
10599230 205257 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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 6.2 pIC50 = 6.2 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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
11113541 201568 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11015023 102234 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 406 3 1 4 5.1 O=C(O)C1=C(c2ccc(Cl)cc2)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
11826259 201207 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44316527 203759 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.2 pIC50 = 4.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10211772 56214 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10815167 100710 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.2 pIC50 = 5.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
CHEMBL2304015 207716 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
CHEMBL405599 210811 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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
44328019 155151 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
44327347 96302 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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 5.2 pIC50 = 5.2 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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
10961510 201138 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10696788 175332 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro inhibitory activity against human Endothelin B receptor using radioligand binding assay.In vitro inhibitory activity against human Endothelin B 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 5.2 pIC50 = 5.2 Binding
In vitro inhibitory activity against human Endothelin B receptor using radioligand binding assay.In vitro inhibitory activity against human Endothelin B 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
44316526 203700 2 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.2 pIC50 = 4.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
23445506 112053 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.2 pIC50 = 4.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 428 5 1 6 4.3 COc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
23445227 120299 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 5.2 pIC50 = 5.2 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2ccsc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
10719598 205252 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44284437 99509 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 8.2 pIC50 = 8.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
10722389 12004 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.2 pIC50 = 8.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.2 pIC50 = 8.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
44314661 102538 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44314645 172093 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
10507211 109869 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.2 pIC50 = 8.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
CHEMBL438745 212035 0 None - 0 Bovine 8.2 pIC50 = 8.2 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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](Cc2ccc3ccccc3c2)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
44320783 106198 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.2 pIC50 = 8.2 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccnc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
1009 192 20 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
10841576 11323 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.2 pIC50 = 8.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.2 pIC50 = 8.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
10650477 113737 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
10209319 9265 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
CHEMBL412460 211234 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
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
CHEMBL328942 209560 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against endothelin B receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin B 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
CHEMBL433349 211879 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
9896251 98305 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Compound was evaluated for inhibitory activity against human Endothelin B receptor (ETB)Compound was evaluated for inhibitory activity against human Endothelin B receptor (ETB)
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 7.2 pIC50 = 7.2 Binding
Compound was evaluated for inhibitory activity against human Endothelin B receptor (ETB)Compound was evaluated for inhibitory activity against human Endothelin B receptor (ETB)
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
44213959 169789 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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 7.2 pIC50 = 7.2 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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
CHEMBL313984 209367 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
CHEMBL1791271 207163 2 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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
9896251 98305 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 7.2 pIC50 = 7.2 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against endothelin receptor type BInhibitory concentration against endothelin receptor type B
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 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against endothelin receptor type BInhibitory concentration against endothelin receptor type B
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
44311528 202432 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 7.2 pIC50 = 7.2 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
10650546 11999 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 6.2 pIC50 = 6.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 6.2 pIC50 = 6.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
44327656 141245 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
10918533 102357 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10674095 113001 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
8260 527 46 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
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 6.2 pIC50 = 6.2 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
10578853 103104 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
CHEMBL1793926 207177 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar 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)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
CHEMBL318020 209453 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
10504689 9335 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.2 pIC50 = 5.2 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
10895198 100473 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cccc(OCCC)c21 10.1021/jm010382z
10814318 9048 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44439102 89854 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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 5.2 pIC50 = 5.2 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB 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
10305181 60113 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
23445498 204963 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.2 pIC50 = 4.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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
44284041 99826 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.2 pIC50 = 7.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
11801523 8157 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 6.2 pIC50 = 6.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
15453170 104409 4 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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 6.2 pIC50 = 6.2 Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 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
10916597 201615 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
CHEMBL2370254 208063 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)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
44291583 100907 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
CHEMBL336033 209818 1 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibitory effect against Human Endothelin B receptorInhibitory effect against Human Endothelin B 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
23445285 111871 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 5.2 pIC50 = 5.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 454 7 1 5 5.6 CCCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
58688006 170540 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
10165809 131264 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
137637038 155388 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.2 pIC50 = 6.2 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
10577255 174836 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.2 pIC50 = 5.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10576378 100641 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10623888 162596 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.2 pIC50 = 5.2 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10230835 109731 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10344914 99662 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.2 pIC50 = 7.2 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
9936145 18822 1 None - 1 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
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 5.2 pIC50 = 5.2 Binding
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
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
10577829 9561 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10278777 167558 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44322947 204964 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.2 pIC50 = 4.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 428 5 1 6 4.3 COc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
11798998 205098 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.2 pIC50 = 6.2 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
21041284 170360 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
44334065 167248 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.2 pIC50 = 7.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44334146 167426 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.2 pIC50 = 7.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44311285 101816 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 7.2 pIC50 = 7.2 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
159594 518 38 None -4073 3 Human 7.2 pIC50 = 7.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 -4073 3 Human 7.2 pIC50 = 7.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 -4073 3 Human 7.2 pIC50 = 7.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 -4073 3 Human 7.2 pIC50 = 7.2 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
44327881 161114 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
10597575 6803 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 408 5 1 6 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCC2)cc1 10.1021/jm9606507
10576377 11887 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10503525 5775 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.2 pIC50 = 6.2 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44368414 120761 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 5.2 pIC50 = 5.2 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
44371396 49238 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
10992620 201650 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10766067 9631 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
44213924 205753 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.2 pIC50 = 5.2 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
10289311 109933 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
23445388 204788 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.2 pIC50 = 4.2 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2sccc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
44333598 108690 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.2 pIC50 = 7.2 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
22009947 84906 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
CHEMBL413825 211329 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) 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
10602726 165222 0 None - 0 Pig 4.2 pIC50 = 4.2 Binding
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar 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 Pig 4.2 pIC50 = 4.2 Binding
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar 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
10506524 60837 0 None - 0 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
9806559 9046 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
71456864 81266 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10233400 128150 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10651146 108364 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10415067 45094 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 6.2 pIC50 = 6.2 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
44371531 164302 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
10433234 203726 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.2 pIC50 = 5.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
CHEMBL2369714 207901 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
44368482 44417 0 None - 0 Pig 4.2 pIC50 = 4.2 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 4.2 pIC50 = 4.2 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
44386143 130157 0 None - 0 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
44385490 131273 0 None - 0 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
23445544 61031 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.2 pIC50 = 5.2 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44266640 97653 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
44368416 44425 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 5.2 pIC50 = 5.2 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
18996000 98880 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 5.2 pIC50 = 5.2 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
18617354 203756 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.2 pIC50 = 5.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10648135 9237 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
44386621 60933 0 None - 0 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
10768346 131008 0 None - 0 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
10527774 183096 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10718688 183034 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10548486 173534 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.2 pIC50 = 4.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
42630531 18287 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 6.2 pIC50 = 6.2 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
10650638 9079 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.2 pIC50 = 7.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
18738878 193154 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 7.2 pIC50 = 7.2 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
44266851 14401 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 7.2 pIC50 = 7.2 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 7.2 pIC50 = 7.2 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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
44371450 48585 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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 Human 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney 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
CHEMBL2370253 208062 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10151203 100320 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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
76312118 84909 0 None -691 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
23445412 101779 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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 4.2 pIC50 = 4.2 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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
21041297 169029 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
1011 3288 24 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
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 7.2 pIC50 = 7.2 Binding
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
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 7.2 pIC50 = 7.2 Binding
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
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
11015645 201488 0 None - 0 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.2 pIC50 = 7.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
18738879 89788 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 7.2 pIC50 = 7.2 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
18995996 98732 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.2 pIC50 = 6.2 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
10971076 201166 0 None - 0 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.2 pIC50 = 5.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 386 3 1 4 4.7 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
10627378 60087 0 None - 0 Pig 4.2 pIC50 = 4.2 Binding
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar 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 Pig 4.2 pIC50 = 4.2 Binding
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar 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
10815168 167577 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.2 pIC50 = 5.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
137647152 157096 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.2 pIC50 = 6.2 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
10745942 9206 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.2 pIC50 = 8.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
11050177 10147 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 8.2 pIC50 = 8.2 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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 Human 8.2 pIC50 = 8.2 Binding
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
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
9853680 98182 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 8.2 pIC50 = 8.2 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44314580 203417 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.2 pIC50 = 8.2 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
10697520 11996 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
CHEMBL384792 210578 0 None - 0 Bovine 8.1 pIC50 = 8.1 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
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[C@H](C(=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(96)00127-8
44314658 203447 0 None - 0 Pig 8.1 pIC50 = 8.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 8.1 pIC50 = 8.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
CHEMBL1788127 209360 8 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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 Rat 7.2 pIC50 = 7.2 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
19432649 202773 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 7.2 pIC50 = 7.2 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
44311321 202475 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 6.2 pIC50 = 6.2 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
18617284 203487 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.2 pIC50 = 5.2 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
44339714 110807 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10138169 98889 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.2 pIC50 = 5.2 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
CHEMBL85341 214101 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar 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](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
44266567 97768 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
44383536 119878 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B 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 4.2 pIC50 = 4.2 Binding
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B 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
11133491 101686 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 416 3 1 6 4.2 O=C(O)C1=C(c2ccc3c(c2)OCO3)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
11122785 201277 0 None - 0 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.2 pIC50 = 6.2 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10184817 9468 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
21041370 81576 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.2 pIC50 = 6.2 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
52949155 18212 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.2 pIC50 = 6.2 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
11070564 201700 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11058202 201126 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.1 pIC50 = 5.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
10696818 9544 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.1 pIC50 = 4.1 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10814222 9446 0 None - 0 Pig 4.1 pIC50 = 4.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.1 pIC50 = 4.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
44291775 100685 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 6.1 pIC50 = 6.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
23445538 59741 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 5.1 pIC50 = 5.1 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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
9808602 108709 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.1 pIC50 = 7.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
CHEMBL330144 209571 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)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
CHEMBL97431 214137 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)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
10993320 201282 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44383592 59573 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Tested for binding affinity towards human Endothelin B receptorTested for binding affinity towards human Endothelin B receptor
ChEMBL 386 4 1 5 3.6 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
CHEMBL173059 59573 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Tested for binding affinity towards human Endothelin B receptorTested for binding affinity towards human Endothelin B receptor
ChEMBL 386 4 1 5 3.6 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
10625269 14306 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
CHEMBL411797 211200 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)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
15289331 99090 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 5.1 pIC50 = 5.1 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
18617381 105188 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10504542 178973 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
22998396 100334 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.1 pIC50 = 4.1 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
10604167 12296 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 6.1 pIC50 = 6.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 6.1 pIC50 = 6.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
10185233 59732 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44385576 130842 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
11113473 201669 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
11798762 204887 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
CHEMBL405709 210819 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar 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)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
10792782 130829 0 None - 0 Pig 4.1 pIC50 = 4.1 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.1 pIC50 = 4.1 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
137638953 156293 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.1 pIC50 = 6.1 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
11798109 12238 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
44314610 102370 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 7.1 pIC50 = 7.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
71451525 81245 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 7.1 pIC50 = 7.1 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
18995999 98047 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.1 pIC50 = 6.1 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
10719367 97765 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
11826847 201221 1 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccccc1OC)O2 10.1021/jm010382z
CHEMBL405677 210817 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) 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
11103224 200957 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 5.1 pIC50 = 5.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44384177 119774 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 6.1 pIC50 = 6.1 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 506 6 1 8 4.6 Cc1noc(NS(=O)(=O)c2ccsc2COc2cc3c(cc2Cl)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
10721344 7444 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.1 pIC50 = 7.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10144334 130129 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.1 pIC50 = 7.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
11113542 201511 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44311288 202474 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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 membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
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
10918390 19110 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
44327714 206191 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.1 pIC50 = 5.1 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
10743478 108768 0 None - 0 Pig 4.1 pIC50 = 4.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 4.1 pIC50 = 4.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10029171 98297 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.1 pIC50 = 6.1 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
10503334 172762 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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 4.1 pIC50 = 4.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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 4.1 pIC50 = 4.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.1 pIC50 = 4.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
11080933 201712 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44284041 99826 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.1 pIC50 = 7.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
9870830 204977 34 None -66 2 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
11122784 162360 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
9870830 204977 34 None - 2 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL8981 204977 34 None - 2 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL2369713 207900 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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
9870830 204977 34 None -66 2 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
21041324 81238 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.1 pIC50 = 6.1 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10918216 201145 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
15453177 203800 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.1 pIC50 = 5.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
14041110 99539 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 5.1 pIC50 = 5.1 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
10626245 130627 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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 4.1 pIC50 = 4.1 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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
10647172 205029 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.1 pIC50 = 5.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
9803428 101721 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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 5.1 pIC50 = 5.1 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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
10793053 11338 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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
9852318 9508 5 None -2691 2 Human 8.1 pIC50 = 8.1 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
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 8.1 pIC50 = 8.1 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
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 8.1 pIC50 = 8.1 Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
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
44334150 4451 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 8.1 pIC50 = 8.1 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44371773 48314 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 562 8 1 8 4.6 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N(C)S(C)(=O)=O)ccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL155708 48314 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 562 8 1 8 4.6 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N(C)S(C)(=O)=O)ccc23)cc1 10.1016/s0960-894x(99)00040-2
44320590 106066 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.1 pIC50 = 8.1 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
CHEMBL384728 210577 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
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
11733450 201720 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
CHEMBL2369736 207909 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar 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)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
44270524 97742 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 6.1 pIC50 = 6.1 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
44368428 44309 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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 B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B 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
10505771 162792 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
10299975 109752 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
10505771 162792 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 5.1 pIC50 = 5.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
56678451 62981 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
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 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
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
3795752 104710 1 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10769025 59939 0 None - 0 Pig 4.1 pIC50 = 4.1 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.1 pIC50 = 4.1 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
137649592 156856 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.1 pIC50 = 6.1 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
10838921 204613 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
10744040 113057 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
9874379 60110 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44320419 106578 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 6.1 pIC50 = 6.1 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
21041267 81583 10 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.1 pIC50 = 6.1 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
10983992 19246 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
23445468 11113 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.1 pIC50 = 4.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.1 pIC50 = 4.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10275056 112004 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 5.1 pIC50 = 5.1 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 440 6 1 5 5.2 CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
10577388 15388 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
10602620 16399 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
21041278 171201 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
17869279 14695 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.1 pIC50 = 6.1 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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 Pig 6.1 pIC50 = 6.1 Binding
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B 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
10576428 14403 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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 5.1 pIC50 = 5.1 Binding
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 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
44385586 61318 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 ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10137382 181592 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
44385792 60017 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 5.1 pIC50 = 5.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10097589 204548 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 6.1 pIC50 = 6.1 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
10717923 98227 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 5.1 pIC50 = 5.1 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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
11799625 113286 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
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
71462322 81584 6 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.1 pIC50 = 6.1 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
CHEMBL1791280 207167 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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
44387111 165618 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 5.1 pIC50 = 5.1 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
10281606 129137 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10765750 162597 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44265906 96807 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.1 pIC50 = 5.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
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 ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
CHEMBL313056 209355 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
44276947 106355 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 5.1 pIC50 = 5.1 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
44327238 106910 0 None - 0 Pig 5.1 pIC50 = 5.1 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 Pig 5.1 pIC50 = 5.1 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
44458597 98322 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 6.1 pIC50 = 6.1 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
10817057 9587 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.1 pIC50 = 7.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10994374 201716 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
44298356 193305 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B 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
10791823 9343 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 6.1 pIC50 = 6.1 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
10601668 97981 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
44266594 4122 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
44266552 4431 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 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
9846065 170342 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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 5.1 pIC50 = 5.1 Binding
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta 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
10602267 8486 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.1 pIC50 = 4.1 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
52949197 18225 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.1 pIC50 = 6.1 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
CHEMBL2304012 207713 0 None - 0 Pig 7.1 pIC50 = 7.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
44333578 4522 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 7.1 pIC50 = 7.1 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
44278003 98798 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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 6.1 pIC50 = 6.1 Binding
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 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
CHEMBL2304005 207706 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
10625738 168915 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.1 pIC50 = 5.1 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
44385522 59299 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44284329 99933 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 7.1 pIC50 = 7.1 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
159594 518 38 None -4073 3 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B 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 -4073 3 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B 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 -4073 3 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B 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 -4073 3 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B 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
10576427 5283 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.1 pIC50 = 6.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
11037806 201127 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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 Pig 6.1 pIC50 = 6.1 Binding
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 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
3370402 105298 4 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 252 3 1 4 2.1 Cc1noc(NS(=O)(=O)c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
10670664 205576 0 None - 0 Pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 6.1 pIC50 = 6.1 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
23445304 130811 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.1 pIC50 = 5.1 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44320315 106561 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 7.1 pIC50 = 7.1 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
44279413 99477 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB 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
9831527 128947 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 8.1 pIC50 = 8.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44334129 108054 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 8.0 pIC50 = 8.0 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
10230836 8806 0 None - 0 Pig 8.0 pIC50 = 8.0 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 8.0 pIC50 = 8.0 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
44284288 99660 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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 8.0 pIC50 = 8.0 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B 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
44320375 106648 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.0 pIC50 = 8.0 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
44320480 105465 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.0 pIC50 = 8.0 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.0 pIC50 = 8 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 8.0 pIC50 = 8 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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
155542285 172498 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
44270498 98454 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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 B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) 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
CHEMBL265116 208880 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
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
10722385 100020 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B 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
9894460 204972 6 None - 3 Pig 6.1 pIC50 = 6.1 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 - 3 Pig 6.1 pIC50 = 6.1 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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 - 3 Pig 6.1 pIC50 = 6.1 Binding
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney 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
10410546 9307 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 5.1 pIC50 = 5.1 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
44316993 203221 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 4.1 pIC50 = 4.1 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10627398 130152 0 None - 0 Pig 4.1 pIC50 = 4.1 Binding
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar 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 Pig 4.1 pIC50 = 4.1 Binding
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar 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
9959298 60176 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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 4.1 pIC50 = 4.1 Binding
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B 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
10764220 205345 0 None - 0 Pig 5.0 pIC50 = 5.0 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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 Pig 5.0 pIC50 = 5.0 Binding
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
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
44384966 59667 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
22467234 84915 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
11799541 180677 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
CHEMBL289687 209120 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
10695071 100676 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
CHEMBL289687 209120 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
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
10599879 100793 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
25211074 18284 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
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
9871561 174218 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB 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
10168597 60993 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
44213278 106353 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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 5.0 pIC50 = 5.0 Binding
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
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
23445404 100431 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 ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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 5.0 pIC50 = 5.0 Binding
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB 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
10621170 11121 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.0 pIC50 = 4.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.0 pIC50 = 4.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
23445256 59858 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.0 pIC50 = 5.0 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44340049 109829 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 4.0 pIC50 = 4.0 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
10383884 203488 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 6.0 pIC50 = 6.0 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10673644 9674 0 None - 0 Pig 6.0 pIC50 = 6.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 6.0 pIC50 = 6.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
76324075 85399 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETB 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
CHEMBL315658 209435 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
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
CHEMBL315658 209435 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
9809270 130805 0 None - 2 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.0 pIC50 = 6.0 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
137643691 157701 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
23445272 127215 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.0 pIC50 = 5.0 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44458670 98582 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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 7.0 pIC50 = 7.0 Binding
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
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
10238141 194168 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
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
44333887 108125 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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 6.0 pIC50 = 6.0 Binding
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B 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
18617403 203552 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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 5.0 pIC50 = 5.0 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 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
10142669 9338 0 None - 0 Pig 7.0 pIC50 = 7.0 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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 Pig 7.0 pIC50 = 7.0 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
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
104865 697 94 None -6 4 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human ETB receptorBinding affinity to human ETB 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 -6 4 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human ETB receptorBinding affinity to human ETB 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 -6 4 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human ETB receptorBinding affinity to human ETB 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 -6 4 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human ETB receptorBinding affinity to human ETB 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 -6 4 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human ETB receptorBinding affinity to human ETB 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 -123 4 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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 -123 4 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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 -123 4 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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 -123 4 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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 -123 4 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB 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
10790757 96752 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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 6.0 pIC50 = 6.0 Binding
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 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
11027946 18710 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
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 6.0 pIC50 = 6.0 Binding
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
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
44387111 165618 0 None - 0 Pig 5.0 pIC50 = 5.0 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 5.0 pIC50 = 5.0 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
10289348 9208 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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 Human 4.0 pIC50 = 4.0 Binding
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
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
71458717 81244 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 5.0 pIC50 = 5.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44320432 204522 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
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 6.0 pIC50 = 6.0 Binding
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 442 6 1 7 3.6 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1OCCO1 10.1016/s0960-894x(00)00513-8
23445523 59691 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B 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 5.0 pIC50 = 5.0 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2sccc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
22998508 205195 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B 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 4.0 pIC50 = 4.0 Binding
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 412 4 1 5 4.6 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
10649321 110444 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
CHEMBL328942 209560 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B 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](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
10649321 110444 0 None - 0 Pig 6.0 pIC50 = 6.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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 Pig 6.0 pIC50 = 6.0 Binding
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 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
10602312 59336 0 None - 0 Pig 4.0 pIC50 = 4.0 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.0 pIC50 = 4.0 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
137633242 155927 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB 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
10189776 59727 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB 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
10766198 162323 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 4.0 pIC50 = 4.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
9914310 204907 3 None -1995 2 Human 7.0 pIC50 = 7.0 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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 7.0 pIC50 = 7.0 Binding
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B 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
CHEMBL315780 209436 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
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
11477084 3540 46 None - 2 Human 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 - 2 Human 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 - 2 Human 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 - 2 Human 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 - 2 Human 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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 - 2 Human 5.0 pIC50 = 5.0 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B 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
10673644 9674 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
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
16004692 2411 85 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB 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 6.0 pIC50 = 6.0 Binding
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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 6.0 pIC50 = 6.0 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB 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
44314906 103090 0 None - 0 Pig 7.0 pIC50 = 7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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 7.0 pIC50 = 7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum 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
10697377 60746 0 None - 0 Pig 4.0 pIC50 = 4 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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 Pig 4.0 pIC50 = 4 Binding
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
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+
23445458 59966 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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 5.0 pIC50 = 5 Binding
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor 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
44284481 211967 0 None 3 5 Rat 11.0 pKi = 11 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
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 3 5 Rat 11.0 pKi = 11 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
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
131845706 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
71308726 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
995 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL1222310 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL4524099 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
131845706 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
71308726 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
995 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL1222310 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL4524099 3403 6 None 11 2 Rat 10.9 pKi = 10.9 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
44284481 211967 0 None 3 5 Rat 10.8 pKi = 10.8 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
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 3 5 Rat 10.8 pKi = 10.8 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
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
155543936 172654 0 None 218776 2 Rat 10.8 pKi = 10.8 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
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 10.8 pKi = 10.8 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
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
CHEMBL1790180 207130 0 None -1 3 Human 10.8 pKi = 10.8 Binding
Binding affinity to human ETB receptor by radioligand displacement assayBinding affinity to human ETB 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]([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 10.1016/j.ejmech.2013.01.044
CHEMBL1790180 207130 0 None 1 3 Rat 10.7 pKi = 10.7 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
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
155543936 172654 0 None 218776 2 Rat 10.6 pKi = 10.6 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
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 10.6 pKi = 10.6 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
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
CHEMBL1790180 207130 0 None 1 3 Rat 10.4 pKi = 10.4 Binding
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
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
CHEMBL1790180 207130 0 None -1 3 Human 10.3 pKi = 10.3 Binding
Displacement of radiolabeled endothelin-3 from human endothelin ETB receptorDisplacement of radiolabeled endothelin-3 from human endothelin ETB 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]([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/jm8007618
44284481 211967 0 None -4 5 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETB 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 10.2 pKi = 10.2 Binding
Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETB 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
44314783 165885 0 None 7943 2 Pig 10.1 pKi = 10.1 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 10.1 pKi = 10.1 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 10.1 pKi = 10.1 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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
44311728 103861 0 None 13 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.9 pKi = 9.9 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311701 167582 1 None 213 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.7 pKi = 9.7 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311700 102336 0 None 234 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311692 102678 0 None 3 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311803 202838 0 None 26 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311804 102531 0 None 12 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311727 202754 0 None 9 2 Human 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.6 pKi = 9.6 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44314820 155168 0 None 380 2 Pig 9.6 pKi = 9.6 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 9.6 pKi = 9.6 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 9.6 pKi = 9.6 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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
44311915 104299 0 None 6 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.5 pKi = 9.5 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311805 202850 0 None 26 2 Human 9.4 pKi = 9.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.4 pKi = 9.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311838 202902 0 None 13 2 Human 9.4 pKi = 9.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.4 pKi = 9.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311726 102598 0 None 10 2 Human 9.4 pKi = 9.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.4 pKi = 9.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311772 102546 0 None 10 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.3 pKi = 9.3 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311850 102703 0 None 10 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.3 pKi = 9.3 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311849 102586 0 None 5 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.2 pKi = 9.2 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311852 102597 0 None 144 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.2 pKi = 9.2 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311773 202962 0 None 7 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.2 pKi = 9.2 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311699 202459 0 None 331 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.1 pKi = 9.1 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311851 202947 0 None 162 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 9.1 pKi = 9.1 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44314607 160702 0 None 1412 2 Pig 9.0 pKi = 9.0 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 9.0 pKi = 9.0 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 9.0 pKi = 9.0 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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
3887 2033 39 None 7 4 Pig 9.0 pKi = 9 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL None None None None 10.1016/0960-894X(96)00421-0
5311192 2033 39 None 7 4 Pig 9.0 pKi = 9 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL None None None None 10.1016/0960-894X(96)00421-0
CHEMBL72410 2033 39 None 7 4 Pig 9.0 pKi = 9 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL None None None None 10.1016/0960-894X(96)00421-0
44314832 160714 0 None 251 2 Pig 9.0 pKi = 9 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 9.0 pKi = 9 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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
3887 2033 39 None -7 4 Human 9.0 pKi = 9 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00387-4
5311192 2033 39 None -7 4 Human 9.0 pKi = 9 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00387-4
CHEMBL72410 2033 39 None -7 4 Human 9.0 pKi = 9 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00387-4
9938533 104921 1 None 1 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 8.9 pKi = 8.9 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
9938533 104921 1 None 1 2 Human 8.9 pKi = 8.9 Binding
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B 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 8.9 pKi = 8.9 Binding
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B 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
46228117 198092 0 None - 1 Mouse 8.9 pKi = 8.9 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 690 13 1 12 4.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOc3ccc(S(C)(=O)=O)cc3)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL593928 198092 0 None - 1 Mouse 8.9 pKi = 8.9 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 690 13 1 12 4.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOc3ccc(S(C)(=O)=O)cc3)c2)cc1 10.1016/j.bmc.2009.08.058
44311763 202734 0 None 6 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 8.9 pKi = 8.9 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
9953358 94346 9 None -102 2 Human 6.0 pKi = 6 Binding
Binding affinity against human Endothelin B receptor; orally active in vivo at 30 mg/kg, poBinding affinity against human Endothelin B 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 6.0 pKi = 6 Binding
Binding affinity against human Endothelin B receptor; orally active in vivo at 30 mg/kg, poBinding affinity against human Endothelin B 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
9953358 94346 9 None -102 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 6.0 pKi = 6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10599129 101753 0 None -5 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 6.0 pKi = 6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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
10737908 41195 0 None -102 2 Rat 4.0 pKi = 4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.0 pKi = 4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 370 6 1 4 4.6 Cc1cnoc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
10835335 4753 0 None -50118 2 Human 4.0 pKi = 4 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 4.0 pKi = 4 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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
10321341 144891 0 None -93 2 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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 6.0 pKi = 6.0 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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
11762890 100183 0 None -14791 2 Human 6.0 pKi = 6.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.0 pKi = 6.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
44314444 161161 0 None 457 2 Pig 8.0 pKi = 8.0 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 8.0 pKi = 8.0 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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
178103 167377 9 None -100 2 Human 7.0 pKi = 7.0 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 7.0 pKi = 7.0 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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
10763862 162654 0 None -1096 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 6.0 pKi = 6.0 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 406 9 1 5 4.0 CCc1cc(CC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10907333 101599 0 None -1819 2 Human 6.0 pKi = 6.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.0 pKi = 6.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
19934535 106479 0 None 7 2 Rat 5.0 pKi = 5.0 Binding
Affinity against ET B receptorAffinity against ET B 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 Rat 5.0 pKi = 5.0 Binding
Affinity against ET B receptorAffinity against ET B 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
11812665 99294 0 None -18197 2 Human 5.0 pKi = 5.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.0 pKi = 5.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
178103 167377 9 None -100 2 Human 7.0 pKi = 7.0 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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 7.0 pKi = 7.0 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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
10553793 4380 0 None -75 2 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 6.9 pKi = 6.9 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10813050 43788 0 None -602 2 Rat 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 9 2 5 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CNC=O)c1C 10.1021/jm970872k
9830098 102543 0 None 5 2 Human 5.9 pKi = 5.9 Binding
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B 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 5.9 pKi = 5.9 Binding
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B 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
44312023 202749 0 None 22 2 Human 5.9 pKi = 5.9 Binding
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B 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 5.9 pKi = 5.9 Binding
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B 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
10984658 100371 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 570 10 1 7 6.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CCc2ccccc2)c1C 10.1021/jm020289q
CHEMBL29346 100371 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 570 10 1 7 6.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CCc2ccccc2)c1C 10.1021/jm020289q
10812403 38848 0 None -120 2 Rat 4.9 pKi = 4.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.9 pKi = 4.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 7 2 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(N)=O)c1C 10.1021/jm970872k
10668819 120588 0 None -602 2 Rat 4.9 pKi = 4.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.9 pKi = 4.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 402 6 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2F)c1C 10.1021/jm970872k
10742502 120741 0 None -134 2 Rat 4.9 pKi = 4.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.9 pKi = 4.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 457 9 3 6 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCC(=O)O)c1C 10.1021/jm970872k
19934549 105500 0 None 3 2 Rat 4.9 pKi = 4.9 Binding
Affinity against ET B receptorAffinity against ET B 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 Rat 4.9 pKi = 4.9 Binding
Affinity against ET B receptorAffinity against ET B 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
10740953 5229 0 None -758 2 Human 4.9 pKi = 4.9 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 4.9 pKi = 4.9 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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
10740258 109177 0 None -1096 2 Human 4.9 pKi = 4.9 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 4.9 pKi = 4.9 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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
9938571 9491 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO 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/jm000538f
CHEMBL112531 9491 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO 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/jm000538f
CHEMBL369489 9491 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO 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/jm000538f
11801906 98063 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 6.9 pKi = 6.9 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10501931 43610 0 None -64 2 Rat 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CO)c1C 10.1021/jm970872k
10719157 101812 0 None -58 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.9 pKi = 5.9 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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
10552683 201412 0 None -5 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.9 pKi = 5.9 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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
10670662 201747 0 None -53 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.9 pKi = 5.9 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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
11103181 98912 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 507 7 1 7 4.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCN(C)C2=O)c1C 10.1021/jm020289q
CHEMBL282628 98912 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 507 7 1 7 4.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCN(C)C2=O)c1C 10.1021/jm020289q
9915028 9306 12 None -28183 2 Human 4.9 pKi = 4.9 Binding
Selectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRBSelectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRB
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 4.9 pKi = 4.9 Binding
Selectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRBSelectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRB
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 4.9 pKi = 4.9 Binding
Selectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRBSelectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRB
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 4.9 pKi = 4.9 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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 4.9 pKi = 4.9 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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 4.9 pKi = 4.9 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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
9914310 204907 3 None -1995 2 Human 6.9 pKi = 6.9 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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 6.9 pKi = 6.9 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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
9870830 204977 34 None -66 2 Human 6.9 pKi = 6.9 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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 6.9 pKi = 6.9 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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 6.9 pKi = 6.9 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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 6.9 pKi = 6.9 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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 6.9 pKi = 6.9 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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 6.9 pKi = 6.9 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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
9849547 183414 0 None -34 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]-ET-1 binding to CHO cells expressing human Endothelin B receptor at a concentration of 1 uMInhibition of [125I]-ET-1 binding to CHO cells expressing human Endothelin B receptor at a concentration of 1 uM
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 7.8 pKi = 7.8 Binding
Inhibition of [125I]-ET-1 binding to CHO cells expressing human Endothelin B receptor at a concentration of 1 uMInhibition of [125I]-ET-1 binding to CHO cells expressing human Endothelin B receptor at a concentration of 1 uM
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
10768897 107158 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.8 pKi = 7.8 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
108002 3425 14 None -56 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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 7.8 pKi = 7.8 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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 7.8 pKi = 7.8 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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 7.8 pKi = 7.8 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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 7.8 pKi = 7.8 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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 7.8 pKi = 7.8 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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
104865 697 94 None -6 4 Human 6.9 pKi = 6.9 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors 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 -6 4 Human 6.9 pKi = 6.9 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors 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 -6 4 Human 6.9 pKi = 6.9 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors 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 -6 4 Human 6.9 pKi = 6.9 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors 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 -6 4 Human 6.9 pKi = 6.9 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors 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
10741151 42806 0 None -223 2 Rat 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.9 pKi = 5.9 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 8 2 5 5.4 CCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10743346 102125 0 None -4 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.9 pKi = 5.9 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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
10941181 98873 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 624 9 1 7 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccc(C(F)(F)F)cc2)c1C 10.1021/jm020289q
CHEMBL282336 98873 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 624 9 1 7 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccc(C(F)(F)F)cc2)c1C 10.1021/jm020289q
11730445 101425 0 None -4677 2 Human 5.9 pKi = 5.9 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.9 pKi = 5.9 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2cccn2)c1C 10.1021/jm020289q
9807200 84907 0 None -346 2 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 5.8 pKi = 5.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
10918301 101013 0 None -7585 2 Human 6.8 pKi = 6.8 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.8 pKi = 6.8 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10620185 119133 0 None -89 2 Rat 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 386 6 1 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OC(C)C)cc2)c1C 10.1021/jm970872k
10814297 201826 0 None -17 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.8 pKi = 5.8 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 472 10 1 7 4.3 COc1cc(OC)nc(OC(C(=O)O)C(Oc2ccccc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
11124425 99389 0 None -75857 2 Human 5.8 pKi = 5.8 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.8 pKi = 5.8 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10595347 42221 0 None -537 2 Rat 4.8 pKi = 4.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.8 pKi = 4.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 370 6 1 4 4.7 CCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
10691439 44277 0 None -245 2 Rat 4.8 pKi = 4.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.8 pKi = 4.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 4 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)(C)C)cc2)c1C 10.1021/jm970872k
76312118 84909 0 None -691 2 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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 5.8 pKi = 5.8 Binding
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB 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
9863132 162747 0 None - 1 Pig 7.8 pKi = 7.8 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 348 6 3 2 3.1 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1CC1c1ccccc1 10.1016/0960-894X(96)00421-0
CHEMBL418898 162747 0 None - 1 Pig 7.8 pKi = 7.8 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 348 6 3 2 3.1 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1CC1c1ccccc1 10.1016/0960-894X(96)00421-0
10528863 4537 0 None -4 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.8 pKi = 7.8 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10786696 102301 0 None -223 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 6.8 pKi = 6.8 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 392 8 1 5 3.8 CCc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10603135 109243 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10503421 118991 0 None -245 2 Rat 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 443 9 3 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCCO)c1C 10.1021/jm970872k
9822616 121465 0 None -17782 2 Human 4.8 pKi = 4.8 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 4.8 pKi = 4.8 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
46228086 198142 0 None - 1 Mouse 6.8 pKi = 6.8 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 598 10 1 9 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCBr)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL594265 198142 0 None - 1 Mouse 6.8 pKi = 6.8 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 598 10 1 9 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCBr)c2)cc1 10.1016/j.bmc.2009.08.058
10505434 4583 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 6.8 pKi = 6.8 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10691437 4998 0 None -95 4 Rat 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 -95 4 Rat 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
9908909 5222 7 None -363 3 Rat 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 -363 3 Rat 5.8 pKi = 5.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C 10.1021/jm970872k
11797288 201913 0 None -89 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.8 pKi = 5.8 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 11 1 7 3.7 CCCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
10691437 4998 0 None -95 4 Human 5.8 pKi = 5.8 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 -95 4 Human 5.8 pKi = 5.8 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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
11081276 100740 0 None -2238 2 Human 5.8 pKi = 5.8 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.8 pKi = 5.8 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 476 7 1 8 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cc2ncco2)c1C 10.1021/jm020289q
10864118 100985 0 None -4265 2 Human 5.8 pKi = 5.8 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.8 pKi = 5.8 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10667808 118773 0 None -338 2 Rat 4.8 pKi = 4.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.8 pKi = 4.8 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 385 6 2 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(NC(C)C)cc2)c1C 10.1021/jm970872k
12286 933 30 None -1348 2 Human 6.8 pKi = 6.8 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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 6.8 pKi = 6.8 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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 6.8 pKi = 6.8 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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 6.8 pKi = 6.8 Binding
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 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
108002 3425 14 None -56 2 Human 7.8 pKi = 7.8 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 7.8 pKi = 7.8 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 7.8 pKi = 7.8 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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
44314884 160193 0 None - 1 Pig 6.8 pKi = 6.8 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 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](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](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
77282209 160193 0 None - 1 Pig 6.8 pKi = 6.8 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 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](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](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
CHEMBL411399 160193 0 None - 1 Pig 6.8 pKi = 6.8 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 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](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](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
10742005 201993 0 None -162 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.8 pKi = 5.8 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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
9843631 92766 9 None -13182 4 Human 4.7 pKi = 4.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 -13182 4 Human 4.7 pKi = 4.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 -13182 4 Human 4.7 pKi = 4.7 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 -13182 4 Human 4.7 pKi = 4.7 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 -13182 4 Human 4.7 pKi = 4.7 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 -13182 4 Human 4.7 pKi = 4.7 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2)c1C 10.1021/jm020289q
9865409 101846 0 None -199 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
10691438 44226 0 None -51 2 Rat 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 7 1 4 5.1 CCCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
10718666 120994 0 None -3 2 Rat 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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
5122650 102445 6 None -100 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.7 pKi = 5.7 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 364 7 1 5 3.2 COC(c1ccccc1)(c1ccccc1)C(Oc1nccc(C)n1)C(=O)O 10.1021/jm960274q
9843631 92766 9 None -1348 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETB receptor in rat cerebellum 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 -1348 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETB receptor in rat cerebellum 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
11113812 100316 0 None -1258 2 Human 5.7 pKi = 5.7 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.7 pKi = 5.7 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
11103326 167331 0 None -12589 2 Human 5.7 pKi = 5.7 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.7 pKi = 5.7 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10620897 41360 0 None -14 2 Rat 4.7 pKi = 4.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.7 pKi = 4.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 6 1 4 5.3 Cc1cccc(-c2ccc(CC(C)C)cc2)c1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10761688 119337 0 None -380 2 Rat 4.7 pKi = 4.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.7 pKi = 4.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 370 5 1 4 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)C)cc2)c1C 10.1021/jm970872k
10810897 120966 0 None -3801 2 Rat 4.7 pKi = 4.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.7 pKi = 4.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 6 1 4 5.3 Cc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
197712 101697 51 None -194 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 6.7 pKi = 6.7 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 378 7 1 5 3.5 COC(c1ccccc1)(c1ccccc1)C(Oc1nc(C)cc(C)n1)C(=O)O 10.1021/jm960274q
10721484 106864 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 6.7 pKi = 6.7 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10793160 97941 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.7 pKi = 7.7 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10432263 101669 0 None -85 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 7.7 pKi = 7.7 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 420 8 1 6 3.4 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2 10.1021/jm960274q
10549727 164324 0 None -125 2 Rat 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 1 5 5.0 COc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
10762600 167728 0 None -154 2 Rat 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 6 1 4 5.0 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10620958 41452 0 None -331 2 Rat 4.7 pKi = 4.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.7 pKi = 4.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 399 6 1 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C(C)C)cc2)c1C 10.1021/jm970872k
44365561 42010 0 None -524 2 Human 4.7 pKi = 4.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 4.7 pKi = 4.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 404 5 1 4 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
19085510 119037 0 None -6025 2 Human 4.7 pKi = 4.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 4.7 pKi = 4.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccnc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
11794992 4888 0 None -39810 2 Human 4.7 pKi = 4.7 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 4.7 pKi = 4.7 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cocn3)cc2)c1C 10.1021/jm000105c
10668636 121445 0 None -147 2 Rat 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccc(N)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10508342 4647 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 6.7 pKi = 6.7 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10740469 39053 0 None -154 2 Rat 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.7 pKi = 5.7 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 413 7 2 5 5.0 CNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
18660520 39311 0 None -3548 2 Human 4.7 pKi = 4.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 4.7 pKi = 4.7 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
11799974 4448 0 None -12 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.6 pKi = 7.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
3921421 106802 8 None -9 2 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 6.6 pKi = 6.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10670965 42066 0 None -851 2 Rat 5.6 pKi = 5.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.6 pKi = 5.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 444 9 2 6 4.3 Cc1noc(NS(=O)(=O)c2cccc(OCCO)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
11006149 100616 0 None -380 2 Human 5.6 pKi = 5.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.6 pKi = 5.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10521258 120770 0 None -416 2 Rat 4.6 pKi = 4.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.6 pKi = 4.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 342 4 1 4 4.1 Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
44311810 104298 0 None 35 2 Human 7.6 pKi = 7.6 Binding
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B 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 7.6 pKi = 7.6 Binding
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B 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
10555112 4654 0 None -12 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.6 pKi = 7.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10648996 4273 0 None -3 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.6 pKi = 7.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
9979632 102415 0 None -41 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 7.6 pKi = 7.6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 422 8 1 7 2.8 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2 10.1021/jm960274q
45257114 198171 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 538 10 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1 10.1021/jm101110w
CHEMBL594482 198171 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 538 10 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1 10.1021/jm101110w
45257114 198171 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 538 10 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL594482 198171 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 538 10 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1 10.1016/j.bmc.2009.08.058
10501166 41619 0 None -47 2 Rat 4.6 pKi = 4.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.6 pKi = 4.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cc(O)ccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10407051 99914 0 None -5 2 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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 5.6 pKi = 5.6 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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
9937336 174097 1 None -229 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 7.6 pKi = 7.6 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
11800649 4526 0 None -7 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.6 pKi = 7.6 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10693607 102220 0 None -354 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.6 pKi = 5.6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 424 10 1 7 3.3 CCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
10836754 201887 0 None -14 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.6 pKi = 5.6 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 11 1 7 3.7 CCOc1cc(OCC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
11124545 100890 0 None -4168 2 Human 5.6 pKi = 5.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.6 pKi = 5.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
44314445 160701 0 None - 1 Pig 6.6 pKi = 6.6 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1486 45 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)CNC(=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
CHEMBL412002 160701 0 None - 1 Pig 6.6 pKi = 6.6 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1486 45 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)CNC(=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
10670204 41278 0 None -17 2 Rat 4.6 pKi = 4.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.6 pKi = 4.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 428 7 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(=O)O)c1C 10.1021/jm970872k
11145758 101261 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C 10.1021/jm020289q
CHEMBL29972 101261 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C 10.1021/jm020289q
10973218 100487 0 None -3388 2 Human 5.6 pKi = 5.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.6 pKi = 5.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10525034 119156 0 None -89 2 Rat 5.6 pKi = 5.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.6 pKi = 5.6 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 7 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCC(C)C)cc2)c1C 10.1021/jm970872k
11734435 100819 0 None -6456 2 Human 5.6 pKi = 5.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.6 pKi = 5.6 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
51003354 57746 0 None - 1 Mouse 6.5 pKi = 6.5 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 920 24 1 17 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CN(C)S(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672884 57746 0 None - 1 Mouse 6.5 pKi = 6.5 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 920 24 1 17 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CN(C)S(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1 10.1021/jm101110w
9865409 101846 0 None -199 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 7.5 pKi = 7.5 Binding
Binding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 394 8 1 6 3.2 COc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10741834 43778 0 None -85 2 Rat 5.5 pKi = 5.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.5 pKi = 5.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 8 2 5 5.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC(C)C)c1C 10.1021/jm970872k
44311873 202755 0 None 2 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44311858 96142 0 None 2 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
10840560 4584 0 None -2 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 8.5 pKi = 8.5 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
44311989 202855 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 8.5 pKi = 8.5 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
44274960 99089 0 None -12 2 Human 5.5 pKi = 5.5 Binding
Binding affinity against human Endothelin B receptor showed weak activityBinding affinity against human Endothelin B receptor showed weak activity
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 5.5 pKi = 5.5 Binding
Binding affinity against human Endothelin B receptor showed weak activityBinding affinity against human Endothelin B receptor showed weak activity
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
44307412 201954 0 None -12 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 5.5 pKi = 5.5 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
10621777 42813 0 None -12 2 Rat 4.5 pKi = 4.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.5 pKi = 4.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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
10548904 118992 0 None -380 2 Rat 4.5 pKi = 4.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.5 pKi = 4.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 7 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CCC(C)C)cc2)c1C 10.1021/jm970872k
44213540 39229 0 None -831 2 Human 4.5 pKi = 4.5 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 4.5 pKi = 4.5 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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
11124821 98819 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 595 8 1 8 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2cc3ccccc3n2C)c1C 10.1021/jm020289q
CHEMBL281977 98819 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 595 8 1 8 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2cc3ccccc3n2C)c1C 10.1021/jm020289q
10505357 108902 0 None -10 2 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 6.5 pKi = 6.5 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10941084 101501 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 610 8 1 7 7.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2cc(Cl)cc(Cl)c2)c1C 10.1021/jm020289q
CHEMBL30150 101501 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 610 8 1 7 7.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2cc(Cl)cc(Cl)c2)c1C 10.1021/jm020289q
443289 702 40 None -831 3 Rat 4.5 pKi = 4.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL None None None None 10.1021/jm970872k
997 702 40 None -831 3 Rat 4.5 pKi = 4.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL None None None None 10.1021/jm970872k
CHEMBL314691 702 40 None -831 3 Rat 4.5 pKi = 4.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL None None None None 10.1021/jm970872k
DB12054 702 40 None -831 3 Rat 4.5 pKi = 4.5 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL None None None None 10.1021/jm970872k
10119517 98764 0 None -169824 2 Human 5.5 pKi = 5.5 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.5 pKi = 5.5 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
104865 697 94 None -6 4 Human 6.5 pKi = 6.5 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 -6 4 Human 6.5 pKi = 6.5 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 -6 4 Human 6.5 pKi = 6.5 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 -6 4 Human 6.5 pKi = 6.5 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B 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 -6 4 Human 6.5 pKi = 6.5 Binding
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
10669224 107967 0 None -1778 2 Human 4.5 pKi = 4.5 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 4.5 pKi = 4.5 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 6 1 6 4.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cc3ncco3)cc2)c1C 10.1021/jm000105c
44265871 166354 0 None -53 2 Human 6.5 pKi = 6.5 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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 6.5 pKi = 6.5 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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
10692125 201365 0 None -26 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.5 pKi = 5.5 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 396 8 2 7 2.3 COc1cc(OC)nc(OC(C(=O)O)C(O)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
9848710 168503 4 None -1 4 Pig 7.4 pKi = 7.4 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 -1 4 Pig 7.4 pKi = 7.4 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
11082049 99086 0 None -933 2 Human 6.4 pKi = 6.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.4 pKi = 6.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
51003353 57745 0 None - 1 Mouse 7.4 pKi = 7.4 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 886 26 1 17 5.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CCCCOc4cccnc4F)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672883 57745 0 None - 1 Mouse 7.4 pKi = 7.4 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 886 26 1 17 5.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CCCCOc4cccnc4F)nn3)c2)cc1 10.1021/jm101110w
10599293 38774 0 None -128 2 Rat 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 9 2 5 5.8 CCCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
9953358 94346 9 None -102 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 6.4 pKi = 6.4 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 -134 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 -134 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 -134 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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 -134 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB 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
11082168 98745 0 None -7585 2 Human 6.4 pKi = 6.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.4 pKi = 6.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10839202 118718 0 None -6 2 Rat 4.4 pKi = 4.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.4 pKi = 4.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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
22103537 41812 0 None -144 2 Human 4.4 pKi = 4.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 4.4 pKi = 4.4 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccno3)cc2)c1C 10.1016/s0960-894x(01)00791-0
44311698 202401 0 None 524 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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 8.4 pKi = 8.4 Binding
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B 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
9893800 106733 10 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]ET-3 from human ET-B receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodDisplacement of [125I]ET-3 from human ET-B 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 8.3 pKi = 8.3 Binding
Displacement of [125I]ET-3 from human ET-B receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodDisplacement of [125I]ET-3 from human ET-B 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 8.3 pKi = 8.3 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 8.3 pKi = 8.3 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10769887 106993 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10528341 14393 0 None -95 2 Rat 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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
10972867 99229 0 None -19952 2 Human 5.4 pKi = 5.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.4 pKi = 5.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
9852318 9508 5 None -2691 2 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors 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 7.4 pKi = 7.4 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors 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 7.4 pKi = 7.4 Binding
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors 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
10715881 121014 0 None -37 2 Rat 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.4 pKi = 5.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 5 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)(C)C)cc2)c1C 10.1021/jm970872k
51003306 57742 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 670 19 1 12 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCF)c2)cc1 10.1021/jm101110w
CHEMBL1672880 57742 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 670 19 1 12 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCF)c2)cc1 10.1021/jm101110w
10718053 43848 0 None -5 2 Rat 4.4 pKi = 4.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.4 pKi = 4.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 442 8 1 6 4.8 CCOC(=O)c1c(C)noc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
11123603 101313 0 None -14125 2 Human 5.4 pKi = 5.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.4 pKi = 5.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccnc2)c1C 10.1021/jm020289q
11754273 100491 0 None -21877 2 Human 5.4 pKi = 5.4 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 5.4 pKi = 5.4 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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
11754273 100491 0 None -21877 2 Human 5.4 pKi = 5.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.4 pKi = 5.4 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
11795351 42588 0 None -109 2 Rat 4.4 pKi = 4.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.4 pKi = 4.4 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 401 6 1 4 4.8 CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2ccc(Cl)nn2)cc1 10.1021/jm970872k
11103112 99393 0 None -4570 2 Human 5.3 pKi = 5.3 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.3 pKi = 5.3 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 501 8 1 7 6.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COc2ccccc2)c1C 10.1021/jm020289q
44274885 93639 0 None -29 2 Human 5.3 pKi = 5.3 Binding
Binding affinity against human Endothelin B receptor showed weak activityBinding affinity against human Endothelin B receptor showed weak activity
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 5.3 pKi = 5.3 Binding
Binding affinity against human Endothelin B receptor showed weak activityBinding affinity against human Endothelin B receptor showed weak activity
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 5.3 pKi = 5.3 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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 5.3 pKi = 5.3 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 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
11059912 98868 0 None -23988 2 Human 5.3 pKi = 5.3 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.3 pKi = 5.3 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
19085508 39333 0 None -218 2 Human 4.3 pKi = 4.3 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 4.3 pKi = 4.3 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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
10453858 159543 0 None -31 2 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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 6.3 pKi = 6.3 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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
9955561 102367 0 None - 1 Pig 8.3 pKi = 8.3 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 453 8 2 2 4.8 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)NCCc2c[nH]c3ccccc23)c1 10.1016/0960-894X(96)00421-0
CHEMBL305615 102367 0 None - 1 Pig 8.3 pKi = 8.3 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 453 8 2 2 4.8 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)NCCc2c[nH]c3ccccc23)c1 10.1016/0960-894X(96)00421-0
44314882 156622 0 None 380 2 Pig 8.3 pKi = 8.3 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 8.3 pKi = 8.3 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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 8.3 pKi = 8.3 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B 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
9894460 204972 6 None -41 3 Human 8.3 pKi = 8.3 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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 -41 3 Human 8.3 pKi = 8.3 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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 -41 3 Human 8.3 pKi = 8.3 Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B 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
44314883 155208 0 None - 1 Pig 8.2 pKi = 8.2 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=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
77282211 155208 0 None - 1 Pig 8.2 pKi = 8.2 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=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
CHEMBL405796 155208 0 None - 1 Pig 8.2 pKi = 8.2 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=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
10526510 120542 0 None -12 2 Rat 4.3 pKi = 4.3 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.3 pKi = 4.3 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 8 1 6 4.2 COc1cc(OC)nc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)n1 10.1021/jm970872k
44314819 155204 0 None - 1 Pig 5.3 pKi = 5.3 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -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](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)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
77282207 155204 0 None - 1 Pig 5.3 pKi = 5.3 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -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](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)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
CHEMBL405753 155204 0 None - 1 Pig 5.3 pKi = 5.3 Binding
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -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](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)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
22103743 42575 0 None -9332 2 Human 4.3 pKi = 4.3 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 4.3 pKi = 4.3 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 411 5 1 6 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccs3)cc2)c1C 10.1016/s0960-894x(01)00791-0
51003352 57744 0 None - 1 Mouse 5.3 pKi = 5.3 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 1020 35 1 21 4.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCOCc3cn(CCOCCOCCOCCOc4cccnc4F)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672882 57744 0 None - 1 Mouse 5.3 pKi = 5.3 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 1020 35 1 21 4.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCOCc3cn(CCOCCOCCOCCOc4cccnc4F)nn3)c2)cc1 10.1021/jm101110w
10647471 42065 0 None -125 2 Rat 5.3 pKi = 5.3 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.3 pKi = 5.3 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 456 7 3 5 4.7 CNC(=O)Nc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10597897 40919 0 None -724 2 Rat 4.3 pKi = 4.3 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 4.3 pKi = 4.3 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 1 5 5.0 COc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10624645 4252 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.3 pKi = 7.3 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10929533 99878 0 None -10964 2 Human 6.3 pKi = 6.3 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.3 pKi = 6.3 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10432263 101669 0 None -85 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 7.3 pKi = 7.3 Binding
Binding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 420 8 1 6 3.4 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2 10.1021/jm960274q
10643748 120910 0 None -29 2 Rat 5.3 pKi = 5.3 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.3 pKi = 5.3 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(CC(C)C)c2)c1C 10.1021/jm970872k
9979632 102415 0 None -41 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 7.2 pKi = 7.2 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 422 8 1 7 2.8 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2 10.1021/jm960274q
10501299 119336 0 None -147 2 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 402 6 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(SC(C)C)cc2)c1C 10.1021/jm970872k
11813553 98874 0 None -14454 2 Human 6.2 pKi = 6.2 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.2 pKi = 6.2 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10815239 108058 0 None -125 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.2 pKi = 7.2 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10690608 120533 0 None -112 2 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 371 5 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C)cc2)c1C 10.1021/jm970872k
19934534 106200 0 None 5 2 Rat 5.2 pKi = 5.2 Binding
Affinity against ET B receptorAffinity against ET B 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 Rat 5.2 pKi = 5.2 Binding
Affinity against ET B receptorAffinity against ET B 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
10837085 101826 0 None -39 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 5.2 pKi = 5.2 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2F)c2ccccc2F)n1 10.1021/jm960274q
19934546 204482 0 None -8 2 Rat 4.2 pKi = 4.2 Binding
Affinity against ET B receptorAffinity against ET B 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 Rat 4.2 pKi = 4.2 Binding
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 466 7 1 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(OCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
10693130 121442 0 None -16 2 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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
11799973 4351 0 None -31 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.2 pKi = 7.2 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
18660521 41440 0 None -2754 2 Human 5.2 pKi = 5.2 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 5.2 pKi = 5.2 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
11731054 98342 0 None -21379 2 Human 6.2 pKi = 6.2 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.2 pKi = 6.2 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
51002602 57748 0 None - 1 Mouse 5.2 pKi = 5.2 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 751 21 1 15 4.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CF)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672886 57748 0 None - 1 Mouse 5.2 pKi = 5.2 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 751 21 1 15 4.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CF)nn3)c2)cc1 10.1021/jm101110w
9864017 41072 0 None -194 2 Human 4.2 pKi = 4.2 Binding
Ability to inhibit ET-1 induced contractions in rabbit carotid artery rings (Endothelin B receptor) was determined in an in vitro functional assay.Ability to inhibit ET-1 induced contractions in rabbit carotid artery rings (Endothelin B receptor) 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 4.2 pKi = 4.2 Binding
Ability to inhibit ET-1 induced contractions in rabbit carotid artery rings (Endothelin B receptor) was determined in an in vitro functional assay.Ability to inhibit ET-1 induced contractions in rabbit carotid artery rings (Endothelin B receptor) 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
10741144 119251 0 None -407 2 Rat 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.2 pKi = 5.2 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 8 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC=O)c1C 10.1021/jm970872k
6433100 4466 6 None -2 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 8.2 pKi = 8.2 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
443289 702 40 None -831 3 Rat 5.2 pKi = 5.2 Binding
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
997 702 40 None -831 3 Rat 5.2 pKi = 5.2 Binding
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
CHEMBL314691 702 40 None -831 3 Rat 5.2 pKi = 5.2 Binding
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
DB12054 702 40 None -831 3 Rat 5.2 pKi = 5.2 Binding
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
19934544 204469 0 None 2 2 Rat 5.2 pKi = 5.2 Binding
Affinity against ET B receptorAffinity against ET B 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 Rat 5.2 pKi = 5.2 Binding
Affinity against ET B receptorAffinity against ET B 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
44333366 106929 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.2 pKi = 7.2 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
46228116 199527 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 598 10 1 9 4.6 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCBr)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
CHEMBL603635 199527 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 598 10 1 9 4.6 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCBr)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
11733544 98765 0 None -7244 2 Human 5.1 pKi = 5.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.1 pKi = 5.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10503999 41058 0 None -6 2 Rat 5.1 pKi = 5.1 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.1 pKi = 5.1 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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
22103385 120559 0 None -19054 2 Human 4.1 pKi = 4.1 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 4.1 pKi = 4.1 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 396 5 1 7 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nnco3)cc2)c1C 10.1016/s0960-894x(01)00791-0
10045790 141108 0 None -17 2 Human 6.1 pKi = 6.1 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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 6.1 pKi = 6.1 Binding
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B 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
9958321 78726 0 None -19498 2 Human 6.1 pKi = 6.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.1 pKi = 6.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10548722 5391 0 None -20892 2 Human 4.1 pKi = 4.1 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 4.1 pKi = 4.1 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnco3)cc2)c1C 10.1021/jm000105c
11027595 99764 0 None -19952 2 Human 6.1 pKi = 6.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.1 pKi = 6.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
104865 697 94 None -6 4 Human 7.1 pKi = 7.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 -6 4 Human 7.1 pKi = 7.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 -6 4 Human 7.1 pKi = 7.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 -6 4 Human 7.1 pKi = 7.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 -6 4 Human 7.1 pKi = 7.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
15297287 163849 0 None 3 2 Rat 5.1 pKi = 5.1 Binding
Affinity against ET B receptorAffinity against ET B 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 Rat 5.1 pKi = 5.1 Binding
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 424 5 2 4 5.2 O=C(O)CN1C(=O)c2ccccc2Nc2ccc(OCc3cccc4ccccc34)cc21 10.1016/0960-894X(95)00019-P
44277840 97789 0 None -81283 2 Human 6.1 pKi = 6.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.1 pKi = 6.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10836583 39440 0 None -43 2 Rat 5.1 pKi = 5.1 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.1 pKi = 5.1 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 434 7 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCc3ccccc3)cc2)c1C 10.1021/jm970872k
51003307 57743 0 None - 1 Mouse 5.1 pKi = 5.1 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 751 21 1 15 4.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCc3cn(CCOCCOCCOCCF)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672881 57743 0 None - 1 Mouse 5.1 pKi = 5.1 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 751 21 1 15 4.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCc3cn(CCOCCOCCOCCF)nn3)c2)cc1 10.1021/jm101110w
11071765 168630 0 None -8709 2 Human 7.1 pKi = 7.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 7.1 pKi = 7.1 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
51002601 57747 0 None - 1 Mouse 6.1 pKi = 6.1 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 906 24 2 17 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CNS(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672885 57747 0 None - 1 Mouse 6.1 pKi = 6.1 Binding
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 906 24 2 17 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CNS(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1 10.1021/jm101110w
9934204 106449 0 None 1 2 Rat 5.1 pKi = 5.1 Binding
Affinity against ET B receptorAffinity against ET B 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 Rat 5.1 pKi = 5.1 Binding
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 465 7 2 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
11049336 99465 0 None -3630 2 Human 5.0 pKi = 5.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 5.0 pKi = 5.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
10673091 162762 0 None -4 2 Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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 7.0 pKi = 7.0 Binding
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B 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
10621010 164299 0 None -186 2 Rat 6.0 pKi = 6.0 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 6.0 pKi = 6.0 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cccc(O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
22103787 40736 0 None -1380 2 Human 5.0 pKi = 5.0 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B 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 5.0 pKi = 5.0 Binding
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 394 5 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-n3cccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
10811477 4735 0 None -19952 2 Human 4.0 pKi = 4.0 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 4.0 pKi = 4.0 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncoc3C)cc2)c1C 10.1021/jm000105c
10813228 107161 0 None -46 2 Human 4.0 pKi = 4.0 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B 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 4.0 pKi = 4.0 Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 445 5 1 6 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nc4ccccc4o3)cc2)c1C 10.1021/jm000105c
10918368 102037 0 None -21379 2 Human 6.0 pKi = 6.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.0 pKi = 6.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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
46228118 200846 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 690 13 1 12 4.7 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCOc3ccc(S(C)(=O)=O)cc3)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
CHEMBL611626 200846 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 690 13 1 12 4.7 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCOc3ccc(S(C)(=O)=O)cc3)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
10573784 164774 0 None -95 2 Rat 5.0 pKi = 5.0 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.0 pKi = 5.0 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 413 7 2 5 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CN)c1C 10.1021/jm970872k
10671031 102208 0 None -29 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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 6.0 pKi = 6.0 Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
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
45257115 199637 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 538 10 1 9 4.2 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCF)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
CHEMBL604286 199637 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 538 10 1 9 4.2 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCF)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
10973161 100562 0 None -6456 2 Human 6.0 pKi = 6.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B 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 6.0 pKi = 6.0 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 502 8 2 9 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNc2ccncn2)c1C 10.1021/jm020289q
10741830 42582 0 None -3 2 Rat 5.0 pKi = 5.0 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.0 pKi = 5.0 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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
10668703 164620 0 None -1230 2 Rat 5.0 pKi = 5.0 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B 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 5.0 pKi = 5.0 Binding
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2O)c1C 10.1021/jm970872k
5344 172891 98 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
CHEMBL453 172891 98 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
6662 216009 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
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
11477084 3540 46 None - 2 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
216235 3540 46 None - 2 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
3548 3540 46 None - 2 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
3950 3540 46 None - 2 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
CHEMBL282724 3540 46 None - 2 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
DB06268 3540 46 None - 2 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
16004692 2411 85 None - 0 Human 8.2 pIC50 = 8.2 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
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 8.2 pIC50 = 8.2 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
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 8.2 pIC50 = 8.2 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
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 8.2 pIC50 = 8.2 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
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 8.2 pIC50 = 8.2 Binding
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
1007 3571 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16130933 3571 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16133819 3571 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3886 3571 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
56947141 3571 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
CHEMBL3188091 3571 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3887 2033 39 None -7 4 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
5311192 2033 39 None -7 4 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL72410 2033 39 None -7 4 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1010 704 0 None 2 2 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 641 11 3 8 4.9 CCCC[C@@H](N(C(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@H](C)CCC[C@@H]1C)C(=O)[C@@H](Cc1cn(c2c1cccc2)C(=O)OC)N)C(=O)O 8904635
3081333 704 0 None 2 2 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 641 11 3 8 4.9 CCCC[C@@H](N(C(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@H](C)CCC[C@@H]1C)C(=O)[C@@H](Cc1cn(c2c1cccc2)C(=O)OC)N)C(=O)O 8904635
1009 192 20 None - 1 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10479298
5310991 192 20 None - 1 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10479298
CHEMBL332794 192 20 None - 1 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 10479298
3837 331 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1472961
1008 3404 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
1008 3404 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16132429 3404 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
16132429 3404 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL1790178 3404 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
CHEMBL1790178 3404 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1007 3571 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16130933 3571 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16133819 3571 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3886 3571 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
56947141 3571 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
CHEMBL3188091 3571 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
1004 1529 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
1004 1529 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16219334 1529 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
16219334 1529 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1008 3404 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
1008 3404 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16132429 3404 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
16132429 3404 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL1790178 3404 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
CHEMBL1790178 3404 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1004 1529 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7524189
1004 1529 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8460684
1004 1529 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16219334 1529 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7524189
16219334 1529 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8460684
16219334 1529 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1010 704 0 None -2 2 Rat 7.5 pKd None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 641 11 3 8 4.9 CCCC[C@@H](N(C(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@H](C)CCC[C@@H]1C)C(=O)[C@@H](Cc1cn(c2c1cccc2)C(=O)OC)N)C(=O)O 8904635
3081333 704 0 None -2 2 Rat 7.5 pKd None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 641 11 3 8 4.9 CCCC[C@@H](N(C(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@H](C)CCC[C@@H]1C)C(=O)[C@@H](Cc1cn(c2c1cccc2)C(=O)OC)N)C(=O)O 8904635
186002 102356 19 125I-ENDOTHELIN -3 3 Human 10.0 pKi = 10 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 -3 3 Human 10.0 pKi = 10 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
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 -6 4 Human 7.0 pKi = 7.0 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 -6 4 Human 7.0 pKi = 7.0 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 -6 4 Human 7.0 pKi = 7.0 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 -6 4 Human 7.0 pKi = 7.0 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 -6 4 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 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 -6 4 Human 6.9 pKi = 6.9 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 -6 4 Human 6.9 pKi = 6.9 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 -6 4 Human 6.9 pKi = 6.9 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 -6 4 Human 6.9 pKi = 6.9 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 -6 4 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
None 214295 0 125I-ENDOTHELIN -52 2 Human 7.7 pKi = 7.7 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
3951 388 82 None 1 2 Human 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
104865 697 94 None -6 4 Human 8.2 pKi = 8.2 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
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 -6 4 Human 8.2 pKi = 8.2 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
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 -6 4 Human 8.2 pKi = 8.2 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
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 -6 4 Human 8.2 pKi = 8.2 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
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 -6 4 Human 8.2 pKi = 8.2 Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
12286 933 30 None -1348 2 Human 6.8 pKi = 6.8 Binding
Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</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 6.8 pKi = 6.8 Binding
Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</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 6.8 pKi = 6.8 Binding
Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</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 6.8 pKi = 6.8 Binding
Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</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 -4073 3 Human 6.9 pKi = 6.9 Binding
CHO cells expressing human ET<sub>B</sub> receptor.CHO cells expressing human ET<sub>B</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 -4073 3 Human 6.9 pKi = 6.9 Binding
CHO cells expressing human ET<sub>B</sub> receptor.CHO cells expressing human ET<sub>B</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 -4073 3 Human 6.9 pKi = 6.9 Binding
CHO cells expressing human ET<sub>B</sub> receptor.CHO cells expressing human ET<sub>B</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 -4073 3 Human 6.9 pKi = 6.9 Binding
CHO cells expressing human ET<sub>B</sub> receptor.CHO cells expressing human ET<sub>B</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
104865 697 94 None -6 4 Human 7.1 pKi = 7.1 Binding
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 -6 4 Human 7.1 pKi = 7.1 Binding
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 -6 4 Human 7.1 pKi = 7.1 Binding
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 -6 4 Human 7.1 pKi = 7.1 Binding
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 -6 4 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
1007 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
1007 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16130933 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
16130933 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16133819 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
16133819 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
3886 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
3886 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
56947141 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
56947141 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
CHEMBL3188091 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
CHEMBL3188091 3571 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16133801 703 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7733918
3859 703 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7733918