Ligand source activities (1 row/activity)





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CHEMBL3980643 212514 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 60246 33 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 60246 33 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 60246 33 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 109972 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 109972 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 210860 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 110604 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 110604 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 8764 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 8764 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 211334 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 211334 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 9353 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 9353 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 163379 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 163379 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 167903 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 167903 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
CHEMBL4533479 213986 1 None 1 2 Human 6.0 pIC50 = 6 Functional
Eurofins cellular functional assay - Antagonist (EDNRB)Eurofins cellular functional assay - Antagonist (EDNRB)
ChEMBL None None None CCCOc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.6019/CHEMBL4507261
11387205 111561 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 111561 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 112006 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 112006 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 107444 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 107444 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 207559 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 207559 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 161875 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 161875 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 98657 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 98657 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 8254 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 8254 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 207588 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 207588 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 391 86 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 391 86 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 391 86 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 391 86 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 391 86 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 106203 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 106203 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 207599 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 207599 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 207520 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 207520 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 207822 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 207822 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 215920 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 207525 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 207525 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 163344 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 163344 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 107632 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 107632 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 207547 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 207547 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 9332 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 9332 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 207455 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 207455 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 213087 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 112320 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 112320 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 99838 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 99838 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 100300 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 100300 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 5157 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 5157 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 172725 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 172725 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 207790 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 207790 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 207385 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 207385 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 207434 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 207434 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 207791 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 207791 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 112690 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 112690 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 207902 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 207902 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 211316 0 None -1 3 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 213640 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 111540 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 111540 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 207799 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 207799 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 99802 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 99802 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 107247 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 107247 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 207866 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 207866 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 109822 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 109822 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 9332 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 9332 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 9359 4 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 9359 4 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 207795 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 207795 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 107240 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 107240 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 107420 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 107420 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 207549 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 207549 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 107341 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 107341 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 207888 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 207888 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 96894 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 96894 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 112666 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 112666 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 207913 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 207913 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 78664 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 78664 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 97056 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 97056 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 156310 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 156310 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 141412 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 141412 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 141789 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 141789 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 207845 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 207845 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 9359 4 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 9359 4 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 207829 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 207829 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 207081 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 207081 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 163656 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 163656 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 207499 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 207499 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 207905 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 207905 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 112665 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 112665 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 207584 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 207584 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 207854 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 207854 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 164879 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 164879 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 96763 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 96763 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 207927 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 207927 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 169168 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 169168 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 207560 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 207560 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 4741 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 4741 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 207507 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 207507 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 167881 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 167881 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 161675 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 161675 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 3029 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 3029 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 3029 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 3029 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 100064 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 100064 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 4741 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 4741 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 98134 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 98134 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 98235 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 98235 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 207088 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 207088 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 207598 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 207598 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 168167 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 168167 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 207936 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 207936 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 207859 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 207859 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 206714 38 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 206714 38 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 207611 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 207611 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 106922 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 106922 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 207271 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 207271 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 107329 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 107329 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 98235 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 98235 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 97056 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 97056 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 207501 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 207501 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 106948 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 106948 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 106201 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 106201 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 161783 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 161783 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 207835 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 207835 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 207834 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 207834 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 194 25 None 1621 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 194 25 None 1621 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 194 25 None 1621 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 112573 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 112573 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 112796 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 112796 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 207589 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 207589 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 107450 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 107450 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 207938 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 207938 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 167876 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 167876 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 112579 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 112579 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 107162 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 107162 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 112564 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 112564 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 163450 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 163450 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 5430 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 5430 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 112404 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 112404 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 207839 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 207839 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 100555 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 100555 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 207802 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 207802 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 207550 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 207550 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 213087 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 207347 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 207347 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 111508 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 111508 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 207824 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 207824 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 207831 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 207831 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 167931 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 167931 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 112304 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 112304 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 112548 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 112548 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 112362 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 112362 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 107177 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 107177 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 163483 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 163483 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 207827 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 207827 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 108298 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 108298 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 96451 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 96451 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
CHEMBL319537 211219 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 107521 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 107521 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 161907 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 161907 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 212694 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 107208 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 107208 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 207869 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 207869 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 207526 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 207526 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 204409 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 204409 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 130562 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 130562 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 59697 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 59697 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 168243 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 168243 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 207577 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 207577 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 132157 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 132157 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 204409 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 204409 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 131340 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 131340 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 59634 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 59634 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 62209 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 62209 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 100064 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 100064 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 61386 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 61386 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 59936 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 59936 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 59608 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 59608 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 98648 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 98648 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 130226 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 130226 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 129738 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 129738 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 129482 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 129482 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 98657 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 98657 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 99838 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 99838 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 62103 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 62103 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 59627 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 59627 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 129739 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 129739 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
13016 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm030480f
9843631 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm030480f
CHEMBL24461 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm030480f
10096179 177020 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 177020 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 449 47 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 449 47 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 449 47 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 449 47 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 3737 0 None 1 2 Rat 8.4 pA2 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7780649
5311469 3737 0 None 1 2 Rat 8.4 pA2 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7780649
104865 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 391 86 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 391 86 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 391 86 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 391 86 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 391 86 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 449 47 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 449 47 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 449 47 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 449 47 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 3352 29 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 3352 29 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 3352 29 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 3317 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8183252
CHEMBL429908 3317 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8183252
9651 2174 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 2174 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 3494 23 None 1 2 Rat 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588
3528 3494 23 None 1 2 Rat 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588
CHEMBL8823 3494 23 None 1 2 Rat 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588




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DOI

4236 28096 66 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 273 5 1 2 2.0 NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1373 28096 66 None - 1 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 273 5 1 2 2.0 NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
104865 706 99 None -6 4 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
3494 706 99 None -6 4 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
392 706 99 None -6 4 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
CHEMBL957 706 99 None -6 4 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
DB00559 706 99 None -6 4 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
4020 205150 39 None - 1 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 10.1038/s41467-023-40064-9
CHEMBL781 205150 39 None - 1 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 10.1038/s41467-023-40064-9
CHEMBL2370066 209777 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 209778 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 211193 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 212651 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 212408 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 215889 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 211112 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 208883 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 208883 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 208883 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
44284481 213725 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 213725 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 110604 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 110604 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
10603409 110604 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 110604 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 163379 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 163379 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 213725 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 213725 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 209332 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
10839947 117302 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 117302 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 9353 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 9353 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 9353 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 9353 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 109972 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 109972 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 163379 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 163379 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
10210629 8764 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 8764 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
10187997 109972 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 109972 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 8764 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 8764 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 12122 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 12122 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 12122 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 194 25 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 10.6019/CHEMBL5210121
5310991 194 25 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 10.6019/CHEMBL5210121
CHEMBL332794 194 25 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 10.6019/CHEMBL5210121
10792711 114791 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 114791 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 204686 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 204686 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 210860 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 9353 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 9353 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 113329 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 113329 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 170669 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 170669 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 11451 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 11451 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 11451 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 163379 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 163379 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 109972 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 109972 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 110604 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 110604 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 12113 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 12113 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 12113 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 12119 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 12119 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 12119 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 204686 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 204686 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 113329 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 113329 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 109639 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 109639 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 161112 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 161112 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 161112 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 168515 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 168515 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 209869 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 176503 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 176503 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 176503 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 138777 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 138777 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 103145 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 103145 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 2072 45 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 2072 45 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 2072 45 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 117302 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 117302 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 8764 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 8764 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 163913 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 163913 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 109756 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 109756 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 103798 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 103798 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 213725 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 213725 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 161792 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 161792 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 11457 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 11457 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 11457 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 105989 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 105989 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 102831 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 102831 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 11962 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 11962 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 11962 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 204548 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 204548 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
CHEMBL405599 212568 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 213087 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 16579 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 16579 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 100809 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 100809 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 174271 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 174271 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 131361 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 131361 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 4642 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 4642 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 100523 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 100523 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 59817 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 59817 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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
10814440 98147 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 98147 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 99994 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 99994 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 10173 51 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 10173 51 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 14634 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 14634 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 14634 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 106839 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 106839 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 204707 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 204707 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 210787 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 98559 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 98559 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 110004 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 110004 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 203201 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 203201 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 210875 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 112311 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 112311 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 207061 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 207061 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 207161 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 207161 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 207259 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 207259 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 207272 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 207272 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 207304 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 207304 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 207373 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 207373 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 207378 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 207378 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 207445 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 207445 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 207820 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 207820 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 210875 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 159375 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 159375 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 128681 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 128681 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 12404 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 12404 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 12404 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 99473 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 99473 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 99473 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 99473 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 62209 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 62209 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 132157 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 132157 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 18404 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 18404 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 61281 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 61281 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 18404 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 18404 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 117806 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 117806 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 102226 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 102226 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 206952 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 206952 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 84673 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 84673 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 131368 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 131368 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 85841 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 85841 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 207139 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 207139 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 12128 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 12128 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 12128 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 97123 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 97123 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 81701 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 81701 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 209466 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 107056 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 107056 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 4636 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 4636 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 161247 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 161247 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 103203 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 103203 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 522 45 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 522 45 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 522 45 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 522 45 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 10173 51 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 10173 51 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 99802 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 99802 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 162391 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 162391 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 213796 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 205481 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 205481 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 100887 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 100887 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 168176 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 168176 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 204748 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 204748 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 168228 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 168228 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 4513 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 4513 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 104892 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 104892 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 9226 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 9226 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 110584 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 110584 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 195816 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 195816 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 106832 1 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 106832 1 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 209584 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 91951 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 91951 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 97101 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 97101 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 18836 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 18836 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 81669 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 81669 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 18399 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 18399 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 81669 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 81669 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 18399 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 18399 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 85355 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 85355 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 60064 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 60064 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 81686 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 81686 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 60235 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 60235 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 98107 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 98107 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 60473 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 60473 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 9614 8 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 9614 8 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 9614 8 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
CHEMBL385492 212352 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 194 25 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 194 25 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 194 25 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 9614 8 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 9614 8 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 9614 8 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 49135 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 49135 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 50882 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 50882 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
9825494 202610 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 202610 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 209463 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 173993 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 173993 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 174446 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 174446 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 206714 38 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 206714 38 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 204190 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 204190 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 531 54 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 531 54 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 531 54 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 105225 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 105225 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 14629 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 14629 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 14629 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 98565 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 98565 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 203889 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 203889 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 102700 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 102700 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 55436 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 55436 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 207581 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 207581 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 18873 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 18873 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 98218 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 98218 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 106845 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 106845 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 61984 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 61984 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 4643 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 4643 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 130226 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 130226 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 101293 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 101293 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 170883 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 170883 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 130698 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 130698 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 204221 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 204221 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 127806 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 127806 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 97129 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 97129 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 45306 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 45306 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 82007 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 82007 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 206897 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 206897 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 54245 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 54245 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 103572 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 103572 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 204998 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 204998 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 131389 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 131389 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 14644 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 14644 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 14644 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 203223 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 203223 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 203381 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 203381 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 209471 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 14584 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 14584 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 14584 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 4551 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 4551 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 211316 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 50985 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 50985 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 118080 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 118080 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 161907 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 161907 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 212694 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 8170 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 8170 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 4760 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 4760 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 202885 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 202885 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 203319 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 203319 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 208781 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 175253 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 175253 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 196498 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 196498 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 63324 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 63324 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 48616 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 48616 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 104753 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 104753 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 105795 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 105795 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 163478 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 163478 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 205516 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 205516 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 213160 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 111309 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 111309 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 209653 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 9411 18 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 9411 18 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 9411 18 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 128196 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 128196 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 61145 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 61145 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 106985 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 106985 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 112342 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 112342 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 157226 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 157226 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 101447 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 101447 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 97123 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 97123 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 60176 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 60176 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 105076 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 105076 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 4406 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 4406 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 4652 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 4652 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 168112 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 168112 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 103163 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 103163 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 107099 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 107099 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 213640 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 204985 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 204985 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 195904 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 195904 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 209465 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 215892 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 167793 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 167793 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 213694 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 162695 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 162695 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 14742 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 14742 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 14742 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 130096 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 130096 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 98565 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 98565 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 97097 31 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 97097 31 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 105204 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 105204 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 205232 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 205232 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 205410 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 205410 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 213875 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 106852 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 106852 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 183920 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 183920 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 183920 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 183920 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 208918 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 207040 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 207040 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 4393 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 4393 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 98428 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 98428 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 8917 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 8917 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 98767 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 98767 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 98767 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 98767 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 175180 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 175180 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 117485 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 117485 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 156597 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 156597 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 102333 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 102333 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 181116 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 181116 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 81679 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 81679 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 5465 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 5465 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 18434 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 18434 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 81690 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 81690 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 81690 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 81690 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 206646 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 206646 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 81697 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 81697 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 82012 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 82012 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 96560 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 96560 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 209462 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 96525 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 96525 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 169727 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 169727 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 62103 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 62103 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 96560 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 96560 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 161247 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 161247 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 215916 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 202906 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 202906 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 203012 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 203012 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 215901 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 211316 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 98566 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 98566 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 96759 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 96759 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 79583 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 79583 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 14636 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 14636 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 14636 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 208932 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 100337 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 100337 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 205263 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 205263 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 205474 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 205474 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 98178 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 98178 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 213094 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 202983 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 202983 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 106857 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 106857 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 5375 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 5375 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 81674 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 81674 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 168106 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 168106 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 60424 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 60424 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 128472 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 128472 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 11235 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 11235 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 11235 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 9411 18 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 9411 18 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 9411 18 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 9332 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 9332 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 18473 3 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 18473 3 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 59760 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 59760 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 18473 3 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 18473 3 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 12043 1 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 12043 1 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 12043 1 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 131444 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 131444 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 131444 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 82011 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 82011 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 101243 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 101243 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 97207 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 97207 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 211221 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 113375 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 113375 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 1325 45 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 1325 45 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 1325 45 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 1325 45 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 59627 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 59627 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 202952 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 202952 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 14786 2 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 14786 2 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 14786 2 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 204245 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 204245 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 51475 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 51475 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 99804 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 99804 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 209813 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 5250 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 5250 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 6323 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 6323 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 202816 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 202816 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 202953 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 202953 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 14635 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 14635 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 14635 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 4513 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 4513 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 203839 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 203839 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 203927 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 203927 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 14859 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 14859 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 14859 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 56345 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 56345 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 205539 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 205539 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 9317 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 9317 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 111315 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 111315 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 113320 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 113320 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 158991 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 158991 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 81698 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 81698 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 81695 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 81695 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 130008 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 130008 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 9411 18 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 9411 18 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 9411 18 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 97302 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 97302 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 101172 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 101172 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 119739 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 119739 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 99838 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 99838 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 162454 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 162454 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 203241 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 203241 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 104877 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 104877 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 209470 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 204109 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 204109 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 212703 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 213690 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 207892 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 207892 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 205277 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 205277 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 8488 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 8488 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 9739 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 9739 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 106834 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 106834 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 59683 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 59683 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 182850 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 182850 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 948 36 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 948 36 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 948 36 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 948 36 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 5157 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 5157 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 81673 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 81673 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 166830 11 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 166830 11 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 181681 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 181681 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 107072 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 107072 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 61499 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 61499 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 11448 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 11448 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 11448 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 130697 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 130697 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 7157 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 7157 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 202826 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 202826 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 14633 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 14633 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 14633 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 8591 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 8591 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 108021 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 108021 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 213637 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 100783 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 100783 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 202864 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 202864 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 202989 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 202989 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 100783 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 100783 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 14790 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 14790 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 14790 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 14794 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 14794 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 14794 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 211197 15 None - 0 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 207585 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 207585 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 210917 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 6974 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 6974 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 98308 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 98308 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 210917 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 711 47 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
997 711 47 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 711 47 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 711 47 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 211574 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 9150 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 9150 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 179612 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 179612 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 96972 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 96972 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 117630 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 117630 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 59251 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 59251 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 112690 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 112690 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 96971 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 96971 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 210809 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 210809 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 100127 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 100127 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 129738 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 129738 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 204118 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 204118 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 81682 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 81682 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 96894 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 96894 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 203171 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 203171 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 161817 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 161817 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 110069 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 110069 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 49530 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 49530 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 211219 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 9748 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 9748 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 60309 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 60309 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 211186 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 14880 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 14880 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 14880 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 14588 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 14588 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 14588 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 53535 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 53535 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 44608 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 44608 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 8869 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 8869 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 60448 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 60448 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 213115 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 522 45 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 522 45 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 522 45 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 522 45 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 97176 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 97176 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 101455 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 101455 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 81700 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 81700 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 81691 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 81691 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 391 86 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 391 86 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 391 86 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 391 86 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 391 86 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 59665 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 59665 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 170845 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 170845 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 129741 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 129741 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 117628 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 117628 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 11239 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 11239 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 11239 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 156897 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 156897 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 18411 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 18411 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 30871 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 30871 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 194886 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 194886 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 194886 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 194886 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 59697 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 59697 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 127817 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 127817 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 127817 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 103742 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 103742 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 11452 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 11452 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 11452 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 102917 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 102917 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 167881 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 167881 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
44314750 165652 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 165652 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 100317 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 100317 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 110447 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 110447 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 11446 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 11446 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 11446 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 206300 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 206300 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 204696 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 204696 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 9241 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 9241 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 103147 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 103147 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 205047 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 205047 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 11438 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 11438 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 11438 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 211198 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 195112 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 195112 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 168482 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 168482 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 211123 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 63329 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 63329 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 122323 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 122323 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 120242 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 120242 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 202610 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 202610 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 100607 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 100607 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 200009 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 200009 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 204056 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 204056 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 204123 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 204123 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 111444 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 111444 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 98200 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 98200 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 162930 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 162930 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 163160 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 163160 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
CHEMBL5272983 193743 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to human placenta ETBBinding affinity to human placenta ETB
ChEMBL 439 7 2 6 3.3 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccccc1)c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.0c01093
19735343 176051 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 176051 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 215892 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 208919 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 60066 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 60066 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 164590 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 164590 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 205004 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 205004 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 205146 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 205146 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 161836 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 161836 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 81677 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 81677 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 174960 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 174960 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 166054 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 166054 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 98957 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 98957 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 106974 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 106974 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 61077 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 61077 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 131385 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 131385 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 81666 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 81666 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 129651 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 129651 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 59615 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 59615 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 202720 45 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 202720 45 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 4509 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 4509 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 6225 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 6225 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 210565 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 96560 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 96560 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 168174 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 168174 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 173147 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 173147 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 101068 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 101068 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 99924 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 99924 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 179371 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 179371 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 204036 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 204036 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 98097 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 98097 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 208715 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 59249 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 59249 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 207306 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 207306 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 131378 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 131378 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 111563 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 111563 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 116541 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 116541 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 157387 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 157387 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 81676 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 81676 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 81676 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 81676 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 85349 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 85349 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 85350 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 85350 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 209473 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 203293 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 203293 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 14763 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 14763 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 14763 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 10226 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 10226 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 10226 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 98522 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 98522 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 100955 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 100955 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 90233 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 90233 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 99237 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 99237 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 205224 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 205224 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 106836 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 106836 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 11093 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 11093 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 11093 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 11093 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 130676 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 130676 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 4501 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 4501 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 60413 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 60413 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 98177 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 98177 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 98613 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 98613 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 61276 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 61276 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 209464 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 139301 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 139301 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 100300 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 100300 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 99488 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 99488 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 98356 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 98356 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 102315 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 102315 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 202961 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 202961 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 102228 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 102228 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 205243 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 205243 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 711 47 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
997 711 47 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 711 47 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 711 47 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 131798 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 131798 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 97047 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 97047 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 98472 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 98472 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 96943 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 96943 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 130565 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 130565 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 61386 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 61386 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 130562 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 130562 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 168892 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 168892 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 168892 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 9797 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 9797 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 101555 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 101555 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 194998 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 194998 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 209474 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 85356 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 85356 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 9809 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 9809 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 9809 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 207538 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 207538 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 99944 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 99944 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 106995 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 106995 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 106632 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 106632 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 106837 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 106837 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 102870 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 102870 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 168197 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 168197 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 130713 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 130713 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 5043 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 5043 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 164560 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 164560 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 173473 101 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 173473 101 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 205246 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 205246 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 106842 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 106842 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 106855 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 106855 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 60414 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 60414 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 81668 27 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 81668 27 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 206893 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 206893 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 85346 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 85346 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 106183 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 106183 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 209779 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 82008 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 82008 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 81702 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 81702 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 100356 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 100356 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 127541 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 127541 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 204128 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 204128 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 204217 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 204217 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 215888 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 107190 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 107190 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 163006 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 163006 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 59269 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 59269 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 162810 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 162810 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 104109 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 104109 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 204980 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 204980 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 6110 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 6110 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 110579 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 110579 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 106833 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 106833 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 91240 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 91240 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 101351 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 101351 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 163110 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 163110 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 128654 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 128654 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 205085 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 205085 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 113992 1 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 113992 1 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 106349 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 106349 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 9436 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 9436 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 109822 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 109822 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 215920 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 5192 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 5192 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 5706 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 5706 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 117627 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 117627 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 14781 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 14781 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 14781 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 61770 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 61770 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 9196 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 9196 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 211189 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 215894 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 196506 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 196506 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 207533 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 207533 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 207915 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 207915 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 105406 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 105406 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 8917 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 8917 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 110459 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 110459 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 61277 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 61277 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 61777 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 61777 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 61296 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 61296 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 110668 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 110668 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 9196 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 9196 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 119939 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 119939 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 209467 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 209652 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 51435 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 51435 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 9137 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 9137 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 203484 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 203484 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 204779 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 204779 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 16402 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 16402 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 196412 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 196412 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 96815 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 205014 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 205014 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 205515 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 205515 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 97056 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 97056 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 101528 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 101528 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 11241 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 11241 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 11241 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 207048 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 207048 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 85227 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 85227 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 205039 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 205039 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 109781 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 109781 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 109781 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 96696 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 96696 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 98657 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 98657 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 107206 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 107206 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 101067 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 101067 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 202912 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 202912 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 203506 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 203506 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 195677 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 195677 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 103127 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 103127 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 168132 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 168132 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 112802 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 112802 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 81663 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 81663 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 97208 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 97208 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 109668 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 109668 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 18485 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 18485 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 18485 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 18485 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 175080 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 175080 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 61606 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 61606 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 111635 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 111635 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 209462 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 209473 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 171603 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 171603 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 173926 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 173926 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 212602 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 14792 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 14792 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 14792 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 128509 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 128509 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 14789 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 14789 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 14789 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 112688 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 112688 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 97001 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 97001 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 99356 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 99356 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 205212 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 205212 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 106850 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 106850 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 107108 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 107108 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 175926 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 175926 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 167820 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 167820 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 128474 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 128474 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 207150 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 207150 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 60240 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 60240 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 203614 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 60409 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 60409 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 59883 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 59883 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 168505 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 168505 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 9852 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 9852 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 61064 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 61064 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 105973 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 105973 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 106956 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 106956 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 11450 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 11450 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 11450 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 11962 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 11962 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 11962 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 107000 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 107000 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 12130 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 12130 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 12130 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 12405 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 12405 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 12405 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 106801 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 106801 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 169569 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 169569 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 168243 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 168243 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 102831 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 102831 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 168515 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 168515 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
10769177 112912 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 112912 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 12243 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 12243 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 12243 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 117465 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 117465 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 141412 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 141412 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 208775 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 5101 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 5101 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 49421 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 49421 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 19381 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 19381 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 100727 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 100727 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 106912 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 106912 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 168147 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 168147 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 199831 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 199831 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 203759 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 203759 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 206714 38 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 206714 38 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 168589 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 168589 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 119489 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 119489 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
10767505 5300 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 5300 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 112804 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 112804 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 210892 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 205533 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 205533 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 9359 4 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 9359 4 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 161999 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 161999 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 60415 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 60415 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 211675 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 85227 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 85227 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 101271 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 101271 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 166909 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 166909 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 116986 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 116986 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 81667 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 81667 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 207234 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 207234 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 97262 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 97262 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 129024 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 129024 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 10079 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 10079 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 10079 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 12116 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 12116 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 12116 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 209469 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 107068 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 107068 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 101548 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 101548 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 84903 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 84903 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 173414 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 173414 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 202666 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 202666 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 9260 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 9260 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 98589 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 98589 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 98589 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 98589 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 18479 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 18479 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 18479 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 18479 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 207276 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 207276 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 170158 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 170158 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 207571 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 207571 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 60362 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 60362 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 129047 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 129047 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 7276 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 7276 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 14632 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 14632 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 14632 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 106844 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 106844 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 169888 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 169888 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 8917 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 8917 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 81693 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 81693 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 61353 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 61353 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 128499 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 128499 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 99548 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 99548 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 172898 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 172898 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 166537 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 166537 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 106628 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 106628 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 166148 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 166148 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 209317 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 209819 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 131149 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 131149 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 215914 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 171484 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 171484 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 103006 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 103006 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 205511 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 205511 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 215892 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 106848 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 106848 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 215892 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 162367 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 162367 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 205441 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 205441 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 106843 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 106843 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 108539 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 108539 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 59976 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 59976 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 59794 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 59794 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 207075 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 207075 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 8500 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 8500 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 104365 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 104365 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 96525 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 96525 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 96778 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 96778 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 96778 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 96778 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 117631 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 117631 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 3029 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 3029 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 3029 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 3029 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 14630 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 14630 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 14630 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 14793 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 14793 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 14793 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 204027 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 204027 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 167836 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 167836 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 168570 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 168570 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 206245 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 206245 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 9551 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 9551 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 113098 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 113098 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 209654 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 60334 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 60334 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 61088 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 61088 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 60334 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 60334 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 81683 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 81683 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 73513 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 73513 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 85345 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 85345 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 81684 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 81684 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 60412 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 60412 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 202804 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 202804 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 211290 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 161783 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 161783 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 96827 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 96827 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 96827 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 203383 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 203383 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 48900 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 48900 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 100636 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 100636 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 202991 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 202991 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 161666 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 161666 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 213753 14 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 207577 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 207577 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 44649 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 44649 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 104416 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 104416 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 163035 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 163035 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 9709 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 9709 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 9854 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 9854 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 109722 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 109722 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 111354 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 111354 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 129819 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 129819 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 128471 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 128471 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 96970 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 96970 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 206675 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 206675 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 101432 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 101432 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 109669 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 109669 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 96944 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 96944 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 111337 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 111337 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
CHEMBL327350 211290 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 202956 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 202956 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 9652 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 9652 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 108668 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 108668 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 106838 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 106838 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 61387 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 61387 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 129022 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 129022 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 213269 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 215911 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 205460 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 205460 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 129474 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 129474 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 101445 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 101445 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 207012 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 207012 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 81685 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 81685 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 206233 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 206233 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 9597 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 9597 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 9597 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 9597 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 9597 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 9597 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 100064 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 100064 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 205278 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 205278 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 205272 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 205272 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 206565 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 206565 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 96763 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 96763 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 7895 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 7895 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 101476 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 101476 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 105613 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 105613 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 106847 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 106847 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 85155 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 85155 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 85155 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 85155 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 59634 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 59634 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 206990 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 206990 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 9106 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 9106 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 207155 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 207155 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 206995 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 206995 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 103147 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 103147 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 164191 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 164191 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 129739 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 129739 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 206205 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 206205 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 59936 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 59936 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 98607 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 98607 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 129739 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 129739 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 163431 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 163431 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 205120 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 205120 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 206709 9 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 206709 9 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 206709 9 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 163381 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 163381 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 194 25 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 10.6019/CHEMBL5210307
5310991 194 25 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 10.6019/CHEMBL5210307
CHEMBL332794 194 25 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 10.6019/CHEMBL5210307
44315009 103206 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 103206 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 98128 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 98128 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 102924 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 102924 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 206410 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 206410 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 106957 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 106957 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 99266 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 99266 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 208893 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 207306 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 207306 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 96451 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 96451 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 163240 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 163240 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 202799 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 202799 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 203509 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 203509 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 194951 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 194951 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 14788 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 14788 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 14788 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 202799 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 202799 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 204954 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 204954 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 203182 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 203182 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 209779 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 211186 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 206811 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 206811 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 97309 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 97309 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 97076 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 97076 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 72209 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 72209 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 179435 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 179435 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 158239 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 158239 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 119818 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 119818 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 168261 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 168261 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 9614 8 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 9614 8 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 9614 8 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 97310 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 97310 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 203377 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 203377 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 4612 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 4612 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 9769 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 9769 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 9239 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 9239 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 59249 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 59249 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 61066 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 61066 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 61285 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 61285 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 170418 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 170418 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 81678 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 81678 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 207554 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 207554 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 172464 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 172464 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 99558 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 99558 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 99581 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 99581 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 45806 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 45806 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 139575 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 139575 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 59735 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 59735 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 11233 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 11233 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 11233 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 108281 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 108281 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 206976 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 206976 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 63257 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 63257 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 109668 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 109668 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 85354 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 85354 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 81680 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 81680 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 165637 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 165637 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 59930 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 59930 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 202895 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 202895 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 204093 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 204093 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 100135 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 100135 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 136932 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 136932 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 204093 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 204093 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 49378 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 49378 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 194667 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 194667 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 141663 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 141663 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 213632 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 213632 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 166723 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 166723 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 203095 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 203095 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 8192 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 8192 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 179553 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 179553 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 206635 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 206635 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 18429 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 18429 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 113370 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 113370 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 105938 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 105938 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 59975 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 59975 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 175575 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 175575 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 206443 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 206443 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 204631 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 204631 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 19027 2 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 19027 2 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 141412 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 141412 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 4328 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 4328 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 82004 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 82004 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 82004 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 82004 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 162700 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 162700 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 129483 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 129483 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 172748 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 172748 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 130099 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 130099 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
44284184 140000 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 140000 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
44458399 98992 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 98992 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 211113 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 215893 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 102043 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 102043 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 100148 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 100148 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 5158 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 5158 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 204060 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 204060 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 207929 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 207929 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 205256 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 205256 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 167114 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 167114 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 117626 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 117626 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 9106 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 9106 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 98235 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 98235 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 11093 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 11093 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 11093 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 11093 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 11093 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 11093 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 11093 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 11093 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 81696 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 81696 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 82001 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 82001 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 97001 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 97001 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 60296 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 60296 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 203531 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 203531 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 16446 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 16446 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 81687 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 81687 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 14631 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 14631 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 14631 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 211195 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 205131 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 205131 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 81675 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 81675 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 82006 14 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 82006 14 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 81672 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 81672 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 81672 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 81672 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 60380 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 60380 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 81665 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 81665 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 153607 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 153607 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 166341 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 166341 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 166341 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 121062 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 121062 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
11059249 102618 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 102618 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 202844 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 202844 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 213625 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 105403 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 105403 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 107378 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 107378 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 210918 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 205026 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 205026 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 8266 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 8266 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 9753 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 9753 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 49967 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 49967 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 88023 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 88023 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 108614 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 108614 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 100356 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 100356 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 206714 38 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 206714 38 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 202976 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 202976 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 14627 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 14627 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 14627 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 100110 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 100110 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 101017 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 101017 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 170623 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 170623 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 208715 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 9288 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 9288 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 108566 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 108566 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 9557 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 9557 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 168591 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 168591 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 62105 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 62105 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 203016 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 203016 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 131360 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 131360 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 204107 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 204107 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 100555 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 100555 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 163075 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 163075 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 163275 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 163275 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 44592 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 44592 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 97564 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 97564 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 205605 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 205605 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 161630 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 161630 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 98379 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 98379 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 11444 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 11444 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 11444 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 12134 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 12134 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 12134 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 102917 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 102917 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 155751 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 155751 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 100157 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 100157 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 204409 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 204409 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 9285 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 9285 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 9431 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 9431 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 103036 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 103036 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 161355 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 161355 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 100326 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 100326 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 99984 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 99984 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 113790 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 113790 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 211123 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 61766 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 61766 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 4194 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 4194 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 194588 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 194588 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 194999 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 194999 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 100719 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 100719 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
CHEMBL329609 211318 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 9632 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 9632 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 206801 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 206801 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 109773 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 109773 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 59902 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 59902 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 206402 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 206402 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 82005 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 82005 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 82003 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 82003 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 9661 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 9661 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 211220 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 100195 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 100195 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 9661 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 9661 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 14586 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 14586 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 14586 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 130891 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 130891 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 522 45 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 522 45 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 522 45 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 522 45 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 206643 8 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 206643 8 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 173748 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 173748 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 11229 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 11229 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 11229 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 215925 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 203117 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 203117 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 101793 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 101793 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 522 45 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 522 45 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 522 45 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 522 45 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 50910 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 50910 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 104176 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 104176 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 104878 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 104878 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 97247 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 97247 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 207541 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 207541 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 100803 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 100803 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 102091 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 102091 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 81662 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 81662 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 130095 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 130095 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 82000 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 82000 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 82000 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 82000 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 207117 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 207117 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 209472 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 5083 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 5083 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 109653 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 109653 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 105527 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 105527 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 204009 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 204009 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 207600 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 207600 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 61368 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 61368 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
44284115 100195 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 100195 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 202820 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 202820 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 195680 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 195680 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 98858 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 98858 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 9740 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 9740 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 106846 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 106846 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 60444 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 60444 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 60332 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 60332 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 175333 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 175333 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 18407 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 18407 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 18407 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 18407 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 14626 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 14626 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 14626 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 207581 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 207581 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 43748 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 43748 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 181594 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 181594 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 121520 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 121520 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 104539 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 104539 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 60375 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 60375 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 131365 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 131365 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 213115 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 81689 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 81689 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 81689 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 81689 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 81703 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 81703 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 174969 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 174969 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 210635 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 195869 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 195869 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 97246 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 97246 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 131217 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 131217 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 81699 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 81699 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 158977 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 158977 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 112475 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 112475 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 81688 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 81688 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 130887 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 130887 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 175302 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 175302 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 175276 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 175276 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 175325 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 175325 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 9393 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 9393 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 16333 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 16333 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 100758 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 100758 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 208100 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 208100 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 96836 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 96836 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 14615 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 14615 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 85343 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 85343 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 100758 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 100758 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 206995 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 206995 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 203268 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 203268 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 102720 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 102720 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 202905 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 202905 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 205480 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 205480 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 56523 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 56523 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 101193 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 101193 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 209471 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 212568 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 155704 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 155704 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 96763 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 96763 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 202835 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 202835 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 175915 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 175915 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 205421 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 205421 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 112558 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 112558 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 120825 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 120825 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 206990 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 206990 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 99984 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 99984 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 12125 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 12125 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 12125 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 103025 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 103025 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 172672 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 172672 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 110371 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 110371 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
44320783 106693 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 106693 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 194 25 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 194 25 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 194 25 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 11443 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 11443 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 11443 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 114249 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 114249 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 9370 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 9370 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 212991 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 211316 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 213637 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 98773 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 98773 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 170368 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 170368 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 211123 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 208916 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 98773 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 98773 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 135418 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 135418 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 204142 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 204142 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 12120 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 12120 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 12120 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 141789 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 141789 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 102843 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 102843 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 113513 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 113513 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 531 54 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 531 54 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 531 54 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 103592 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 103592 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 208930 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 211209 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 9441 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 9441 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 100954 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 100954 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 9152 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 9152 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 90299 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 90299 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 60449 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 60449 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 206700 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 206700 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 100303 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 100303 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 8256 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 8256 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 104901 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 104901 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 203315 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 203315 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 209818 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 101390 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 101390 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 211574 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 112377 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 112377 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 171116 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 171116 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 131799 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 131799 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 155941 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 155941 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 175419 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 175419 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 101123 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 101123 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 163158 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 163158 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 110233 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 110233 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 100137 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 100137 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 19027 2 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 19027 2 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 9667 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 9667 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 168132 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 168132 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 206701 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 206701 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 206835 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 206835 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 170937 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 170937 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 167822 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 167822 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 168000 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 168000 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 102299 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 102299 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 522 45 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 522 45 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 522 45 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 522 45 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 161675 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 161675 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 6896 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 6896 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 12007 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 12007 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 12007 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 5867 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 5867 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 121287 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 121287 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 49518 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 49518 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 203350 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 203350 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 9738 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 9738 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 207496 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 207496 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 110435 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 110435 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 206524 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 206524 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 109190 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 109190 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 85344 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 85344 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 213087 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 165786 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 165786 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 61180 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 61180 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 9150 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 9150 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 81692 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 81692 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 128685 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 128685 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 108864 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 108864 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 45365 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 45365 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 164865 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 164865 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 205447 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 205447 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 209656 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 44684 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 44684 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 130692 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 130692 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 131808 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 131808 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 61375 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 61375 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 98117 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 98117 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 44692 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 44692 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 99352 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 99352 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 205477 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 205477 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 9342 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 9342 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 61277 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 61277 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 131543 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 131543 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 183688 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 183688 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 183626 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 183626 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 174116 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 174116 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 18488 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 18488 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 9184 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 9184 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 194832 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 194832 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 14585 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 14585 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 14585 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 48864 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 48864 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 209817 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 100800 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 100800 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 85347 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 85347 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 102262 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 102262 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 169607 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 169607 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 3352 29 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 3352 29 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 3352 29 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 203187 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 203187 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 90233 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 90233 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 99202 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 99202 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 202863 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 202863 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 60423 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 60423 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 168151 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 168151 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 157650 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 157650 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 9311 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 9311 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 10259 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 10259 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 10259 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 98648 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 98648 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 205137 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 205137 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 12117 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 12117 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 12117 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
44314658 205168 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 205168 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 211116 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 211116 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 204488 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 204488 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 204185 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 204185 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 205208 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 205208 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 111308 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 111308 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 99361 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 99361 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 215888 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 98233 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 98233 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 120397 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 120397 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 102169 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 102169 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 202975 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 202975 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 9574 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 9574 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 82002 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 82002 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 18411 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 18411 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 203400 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 203400 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 202823 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 202823 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 9650 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 9650 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 9552 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 9552 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 101167 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 101167 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 60071 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 60071 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 109209 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 109209 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 211327 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 215924 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 202980 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 202980 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 59902 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 59902 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 14456 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 14456 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 212957 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 99564 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 99564 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 105681 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 105681 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 179563 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 179563 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 100814 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 100814 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 12417 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 12417 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 12417 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 60062 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 60062 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 131377 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 131377 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 203369 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 203369 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 206623 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 206623 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 212576 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 131364 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 131364 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 156847 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 156847 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 12359 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 12359 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 12359 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 102856 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 102856 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 81671 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 81671 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 98512 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 98512 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 98230 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 98230 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 202919 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 202919 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 212574 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 202653 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 202653 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 120293 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 120293 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 7540 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 7540 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 130664 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 130664 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 203210 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 203210 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 204184 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 204184 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 19321 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 19321 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 207939 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 207939 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 109268 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 109268 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 98765 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 98765 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 173344 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 173344 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 173344 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 173344 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 203412 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 203412 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 100303 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 100303 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 206714 38 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 206714 38 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 162922 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 162922 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 206714 38 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 206714 38 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 209655 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 206714 38 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 206714 38 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 81664 5 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 81664 5 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 202842 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 202842 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 205521 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 205521 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 100014 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 100014 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 131162 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 131162 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 206766 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 206766 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 102204 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 102204 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 11458 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 11458 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 11458 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 9614 8 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 9614 8 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 9614 8 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 4534 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 4534 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 48593 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 48593 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 106561 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 106561 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 212334 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 203420 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 203420 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 209664 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 98207 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 98207 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 44576 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 44576 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 163356 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 163356 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 110254 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 110254 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 163356 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 163356 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 63326 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 63326 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 105202 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 105202 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 60270 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 60270 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 157410 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 157410 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 206346 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 206346 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 113569 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 113569 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 60446 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 60446 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 107074 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 107074 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 82009 13 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 82009 13 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 19461 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 19461 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 11232 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 11232 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 11232 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 112509 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 112509 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 15579 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 15579 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 16591 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 16591 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 171777 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 171777 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 14879 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 14879 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 14879 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 14587 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 14587 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 14587 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 61662 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 61662 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 182184 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 182184 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 60351 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 60351 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 206281 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 206281 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 98693 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 98693 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 113798 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 113798 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 82010 11 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 82010 11 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 208920 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 166182 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 166182 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 129672 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 129672 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 163159 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 163159 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 97269 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 97269 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 59608 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 59608 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 211111 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 106851 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 106851 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 107407 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 107407 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 98791 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 98791 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 9694 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 9694 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 203416 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 203416 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 194985 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 194985 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 9449 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 9449 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 98446 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 98446 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 4201 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 4201 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 4513 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 4513 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 170919 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 170919 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 8587 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 8587 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 18424 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 18424 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 209468 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 4605 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 4605 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 99268 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 99268 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 209461 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 169493 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 169493 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 59626 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 59626 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 100412 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 100412 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 522 45 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 522 45 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 522 45 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 522 45 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 5370 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 5370 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 202824 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 202824 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 105791 5 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 105791 5 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 207317 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 207317 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 131346 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 131346 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 107057 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 107057 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 99952 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 99952 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 129482 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 129482 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 108554 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 108554 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 8909 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 8909 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 100135 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 100135 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 107145 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 107145 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 105958 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 105958 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 206441 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 206441 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 173077 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 173077 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 98924 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 98924 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 210635 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 100499 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 100499 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 206709 9 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 206709 9 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 206709 9 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 9412 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 9412 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 204939 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 204939 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 130687 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 130687 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 60515 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 60515 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 207084 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 207084 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 59997 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 59997 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 85353 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 85353 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 181269 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 181269 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 210875 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 101158 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 101158 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 210875 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 101276 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 101276 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 18485 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 18485 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 174800 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 174800 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 61337 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 61337 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 106849 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 106849 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 100911 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 100911 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 11240 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 11240 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 11240 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 60189 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 60189 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 110331 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 110331 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 205209 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 205209 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 9782 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 9782 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 85840 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 85840 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 211191 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 211191 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 131340 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 131340 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 158258 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 158258 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 127750 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 127750 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 99052 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 99052 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 195851 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 195851 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 108625 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 108625 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 205273 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 205273 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 9444 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 9444 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 97213 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 97213 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 18913 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 18913 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 166182 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 166182 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 9313 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 9313 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 81670 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 81670 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 206255 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 206255 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 60021 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 60021 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 206932 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 206932 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 110946 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 110946 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 211316 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 110946 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 110946 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 59663 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 59663 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 156480 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 156480 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 60057 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 60057 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 162885 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 162885 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 206643 8 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 206643 8 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 211192 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 3610 53 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 3610 53 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 3610 53 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 3610 53 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 3610 53 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 3610 53 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 9782 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 9782 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 449 47 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 449 47 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 449 47 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 449 47 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 449 47 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 449 47 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 449 47 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 449 47 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 103578 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 103578 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 61087 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 61087 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 60300 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 60300 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 213725 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 213725 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 3472 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 3472 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 3472 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 3472 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 3472 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 3472 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 3472 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 3472 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 3472 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 3472 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 213725 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 213725 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 173235 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 173235 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 208883 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 208883 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 173235 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 173235 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 208883 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 208883 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 213725 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 213725 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 166449 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 166449 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 166449 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 104353 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 104353 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 168156 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 168156 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 102822 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 102822 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 103166 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 103166 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 204554 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 204554 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 103018 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 103018 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 204469 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 204469 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 155721 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 155721 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 155721 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 104791 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 104791 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 204566 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 204566 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 204618 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 204618 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 103085 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 103085 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 103033 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 103033 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 103191 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 103191 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 103073 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 103073 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 103084 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 103084 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 204678 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 204678 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 204169 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 204169 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 204663 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 204663 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 161261 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 161261 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 161261 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 2072 45 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 2072 45 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 2072 45 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 161273 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 161273 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 2072 45 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 2072 45 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 2072 45 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 105413 4 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 105413 4 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 105413 4 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 105413 4 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 199784 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 199784 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 204449 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 204449 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 94800 13 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 94800 13 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 94800 13 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 94800 13 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 102236 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 102236 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 41451 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 41451 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 4837 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 4837 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 145436 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 145436 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 100663 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 100663 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 161722 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 161722 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 167951 14 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 167951 14 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 163217 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 163217 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 102082 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 102082 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 106975 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 106975 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 99768 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 99768 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 167951 14 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 167951 14 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 4461 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 4461 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 44053 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 44053 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 103030 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 103030 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 204464 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 204464 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 100851 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 100851 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 39100 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 39100 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 121114 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 121114 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 121267 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 121267 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 105993 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 105993 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 5316 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 5316 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 109678 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 109678 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 9597 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 9597 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 9597 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 98528 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 98528 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 43873 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 43873 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 102295 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 102295 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 203111 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 203111 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 203448 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 203448 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 99384 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 99384 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 9411 18 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 10.6019/CHEMBL5212743
CHEMBL111612 9411 18 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 10.6019/CHEMBL5212743
CHEMBL4761843 9411 18 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 10.6019/CHEMBL5212743
9915028 9411 18 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 9411 18 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 9411 18 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 206643 8 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 206643 8 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 206714 38 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 206714 38 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 3029 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 3029 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 3029 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 3029 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 184006 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 184006 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 107657 1 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 107657 1 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 3494 23 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 3494 23 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 3494 23 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 3494 23 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 3494 23 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 3494 23 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 43067 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 43067 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 102611 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 102611 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 99345 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 99345 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 101908 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 101908 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 85345 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 85345 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 101496 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 101496 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 119651 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 119651 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 203529 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 203529 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 99864 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 99864 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 42481 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 42481 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 44543 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 44543 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 85347 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 85347 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 163310 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 163310 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 4620 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 4620 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 102787 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 102787 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 109744 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 109744 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 119509 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 119509 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 121992 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 121992 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 199834 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 199834 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 4666 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 4666 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 5082 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 5082 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 5309 11 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 5309 11 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 203616 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 203616 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 5082 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 5082 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 101223 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 101223 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 101468 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 101468 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 119291 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 119291 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 948 36 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 948 36 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 948 36 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 948 36 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 3494 23 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 3494 23 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 3494 23 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 160752 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 160752 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 160752 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 203697 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 203697 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
13016 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/s0960-894x(01)00791-0
9843631 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/s0960-894x(01)00791-0
CHEMBL24461 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/s0960-894x(01)00791-0
13016 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm000105c
9843631 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm000105c
CHEMBL24461 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm000105c
13016 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm020289q
9843631 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm020289q
CHEMBL24461 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm020289q
9865409 102329 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 102329 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 44492 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 44492 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 121521 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 121521 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 102931 5 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 102931 5 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
13016 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/j.bmcl.2016.06.014
9843631 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/j.bmcl.2016.06.014
CHEMBL24461 670 13 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 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/j.bmcl.2016.06.014
11113812 100796 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 100796 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 167905 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 167905 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 41616 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 41616 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 119855 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 119855 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 121493 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 121493 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 102180 57 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 102180 57 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 107361 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 107361 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 98406 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 98406 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 102152 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 102152 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 164887 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 164887 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 168302 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 168302 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 41709 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 41709 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 42270 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 42270 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 119555 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 119555 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 4972 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 4972 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 121972 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 121972 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 4730 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 4730 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 39305 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 39305 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 39564 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 39564 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 4531 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 4531 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 107299 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 107299 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 42326 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 42326 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 101098 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 101098 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 121296 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 121296 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 104790 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 104790 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 4737 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 4737 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 4354 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 4354 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 102901 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 102901 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 199863 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 199863 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 199863 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 199863 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 41878 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 41878 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 100393 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 100393 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 174679 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 174679 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 4609 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 4609 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 102706 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 102706 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 203590 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 203590 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 101373 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 101373 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 161260 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 161260 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 41534 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 41534 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 101744 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 101744 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 100969 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 100969 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 119674 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 119674 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 101302 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 101302 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 58067 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 58067 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 102329 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 102329 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 44043 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 44043 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 204470 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 204470 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 96603 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 96603 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 4667 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 4667 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 204571 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 204571 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 99563 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 99563 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 203658 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 203658 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 43074 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 43074 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 119510 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 119510 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 39481 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 39481 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 99289 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 99289 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 109403 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 109403 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 101984 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 101984 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 711 47 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
997 711 47 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 711 47 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 711 47 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 99234 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 99234 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 108466 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 108466 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 166918 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 166918 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 203063 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 203063 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 169080 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 169080 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 169080 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 169080 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 99560 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 99560 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 58066 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 58066 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 39025 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 39025 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 94800 13 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 94800 13 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 1325 45 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 1325 45 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 1325 45 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 1325 45 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 99215 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 99215 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 119236 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 119236 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 42072 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 42072 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 204110 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 204110 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 107230 12 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 107230 12 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 107230 12 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 107230 12 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 107492 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 107492 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 14577 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 14577 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 14577 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 99703 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 99703 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 9614 8 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 9614 8 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 9614 8 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 121541 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 121541 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 58063 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 58063 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 44113 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 44113 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 101796 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 101796 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 100973 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 100973 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 100973 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 100973 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 42849 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 42849 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 99868 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 99868 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 94086 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 94086 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 203758 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 203758 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 99340 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 99340 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 39586 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 39586 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 160102 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 160102 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 102853 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 102853 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 157176 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 157176 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 157176 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 206709 9 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 206709 9 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 206709 9 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 155761 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 155761 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 155761 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 121068 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 121068 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 155757 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 155757 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 155757 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 42836 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 42836 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 58065 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 58065 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 42325 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 42325 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 41175 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 41175 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 4333 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 4333 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 100355 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 100355 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 102152 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 102152 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 121437 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 121437 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 102901 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 102901 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 119854 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 119854 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 99346 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 99346 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 108558 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 108558 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 121059 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 121059 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 106695 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 106695 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 102309 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 102309 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 206214 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 206214 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 121969 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 121969 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 4432 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 4432 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 41697 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 41697 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 98811 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 98811 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 58069 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 58069 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 41328 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 41328 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 119769 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 119769 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 4549 7 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 4549 7 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 711 47 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
997 711 47 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 711 47 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 711 47 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 206200 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 206200 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 107426 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 107426 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 201222 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 201222 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 99235 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 99235 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 41314 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 41314 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 121085 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 121085 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 141652 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 141652 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 79151 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 79151 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 5480 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 5480 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 100241 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 100241 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 164412 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 164412 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 98254 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 98254 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 39693 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 39693 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 58064 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 58064 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 169207 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 169207 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 58068 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 58068 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 106945 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 106945 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 99940 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 99940 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 163325 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 163325 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 164862 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 164862 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 40992 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 40992 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 4818 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 4818 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 107660 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 107660 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 102523 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 102523 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 202542 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 202542 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 165337 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 165337 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 102694 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 102694 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 201332 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 201332 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 101044 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 101044 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 42843 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 42843 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 165183 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 165183 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 173473 101 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 173473 101 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 217739 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 3610 53 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 3610 53 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 3610 53 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 3610 53 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 3610 53 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 3610 53 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 2454 91 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 3641 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16130933 3641 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16133819 3641 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3886 3641 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
56947141 3641 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
CHEMBL3188091 3641 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3887 2072 45 None -7 4 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
5311192 2072 45 None -7 4 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL72410 2072 45 None -7 4 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1010 713 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 713 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 194 25 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 194 25 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 194 25 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 334 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1472961
1008 3473 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
1008 3473 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16132429 3473 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
16132429 3473 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL1790178 3473 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
CHEMBL1790178 3473 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1007 3641 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16130933 3641 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16133819 3641 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3886 3641 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
56947141 3641 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
CHEMBL3188091 3641 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
1004 1565 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
1004 1565 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16219334 1565 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
16219334 1565 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1008 3473 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
1008 3473 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16132429 3473 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
16132429 3473 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL1790178 3473 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
CHEMBL1790178 3473 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1004 1565 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7524189
1004 1565 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8460684
1004 1565 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16219334 1565 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7524189
16219334 1565 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8460684
16219334 1565 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1010 713 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 713 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 102842 23 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 102842 23 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 140707 7 UNDEFINED -89125 36 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 140707 7 UNDEFINED -89125 36 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 203483 15 125I-ENDOTHELIN -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 203483 15 125I-ENDOTHELIN -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 203483 15 125I-ENDOTHELIN -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
None 216493 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 216076 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 391 86 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 391 86 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 391 86 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 391 86 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 391 86 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 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 948 36 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 948 36 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 948 36 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 948 36 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 522 45 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 522 45 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 522 45 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 522 45 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
13016 670 13 None -13182 4 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10956219
9843631 670 13 None -13182 4 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10956219
CHEMBL24461 670 13 None -13182 4 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10956219
104865 706 99 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 706 99 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
392 706 99 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 706 99 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 706 99 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 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
1007 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16130933 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
16130933 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16133819 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
16133819 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
3886 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
3886 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
56947141 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
56947141 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
CHEMBL3188091 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
CHEMBL3188091 3641 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16133801 712 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7733918
3859 712 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7733918