Ligand source activities (1 row/activity)





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CHEMBL3980643 219293 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 67020 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 67020 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 67020 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 116749 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 116749 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 217639 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 117381 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 117381 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 15536 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 15536 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 218113 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 218113 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 16125 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 16125 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 170158 0 None -1 4 Human 8.8 pIC50 = 8.8 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin 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 170158 0 None -1 4 Human 8.8 pIC50 = 8.8 Functional
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin 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 174682 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 174682 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 220765 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 118338 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 118338 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 118783 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 118783 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 114221 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 114221 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 214338 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 214338 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 168654 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 168654 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 105433 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 105433 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 15026 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 15026 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 214367 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 214367 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 7179 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 7179 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 7179 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 7179 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 7179 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 112980 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 112980 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 214378 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 214378 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 214299 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 214299 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 214601 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 214601 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 222699 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 214304 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 214304 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 170123 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 170123 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 114409 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 114409 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 214326 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 214326 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 16104 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 16104 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 214234 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 214234 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 219866 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 119097 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 119097 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 106614 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 106614 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 107076 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 107076 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 11929 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 11929 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 179504 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 179504 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 214569 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 214569 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 214164 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 214164 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 214213 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 214213 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 214570 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 214570 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 119467 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 119467 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 214681 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 214681 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 218095 0 None -1 4 Rat 7.7 pIC50 = 7.7 Functional
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL433406 220419 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 118317 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 118317 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 214578 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 214578 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 106578 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 106578 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 114024 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 114024 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 214645 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 214645 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 116599 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 116599 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 16104 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 16104 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 16131 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 16131 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 214574 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 214574 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 114017 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 114017 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 114197 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 114197 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 214328 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 214328 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 114118 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 114118 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 214667 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 214667 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 103669 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 103669 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 119443 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 119443 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 214692 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 214692 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 85439 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 85439 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 103831 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 103831 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 163089 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 163089 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 148190 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 148190 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 148567 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 148567 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 214624 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 214624 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 16131 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 16131 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 214608 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 214608 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 213860 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 213860 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 170435 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 170435 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 214278 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 214278 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 214684 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 214684 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 119442 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 119442 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 214363 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 214363 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 214633 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 214633 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 171658 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 171658 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 103538 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 103538 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 214706 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 214706 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 175947 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 175947 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 214339 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 214339 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 11513 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 11513 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 214286 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 214286 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 174660 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 174660 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 168454 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 168454 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 9803 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 9803 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 9803 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 9803 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 106840 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 106840 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 11513 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 11513 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 104910 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 104910 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 105011 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 105011 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 213867 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 213867 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 214377 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 214377 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 174946 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 174946 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 214715 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 214715 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 214638 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 214638 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 213493 38 None -1122 5 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 213493 38 None -1122 5 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 214390 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 214390 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 113699 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 113699 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 214050 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 214050 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 114106 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 114106 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 105011 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 105011 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 103831 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 103831 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 214280 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 214280 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 113725 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 113725 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 112978 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 112978 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 168562 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 168562 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 214614 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 214614 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 214613 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 214613 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 6982 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 6982 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 6982 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 119350 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 119350 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 119573 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 119573 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 214368 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 214368 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 114227 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 114227 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 214717 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 214717 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 174655 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 174655 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 119356 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 119356 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 113939 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 113939 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 119341 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 119341 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 170229 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 170229 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 12202 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 12202 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 119181 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 119181 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 214618 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 214618 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 107331 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 107331 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 214581 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 214581 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 214329 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 214329 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 219866 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 214126 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 214126 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 118285 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 118285 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 214603 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 214603 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 214610 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 214610 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 174710 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 174710 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 119081 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 119081 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 119325 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 119325 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 119139 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 119139 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 113954 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 113954 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 170262 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 170262 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 214606 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 214606 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 115075 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 115075 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 103226 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 103226 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 217998 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 114298 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 114298 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 168686 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 168686 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 219473 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 113985 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 113985 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 214648 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 214648 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 214305 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 214305 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 211188 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 211188 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 137340 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 137340 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 66471 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 66471 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 175022 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 175022 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 7493 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 7493 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 7493 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 7493 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 7493 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 214356 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 214356 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 138935 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 138935 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 211188 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 211188 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 138118 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 138118 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 66408 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 66408 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 68983 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 68983 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 106840 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 106840 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 68160 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 68160 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 66710 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 66710 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 66382 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 66382 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 105424 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 105424 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 137004 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 137004 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 136516 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 136516 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 136260 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 136260 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 105433 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 105433 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 106614 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 106614 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 68877 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 68877 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 66401 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 66401 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 136517 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 136517 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 7457 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 7457 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 7457 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 183799 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 183799 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 7237 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 7237 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 7237 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 7237 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 7493 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 7493 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 7493 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 7493 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 7493 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 10509 0 None 1 2 Rat 8.4 pA2 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7780649
5311469 10509 0 None 1 2 Rat 8.4 pA2 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7780649
104865 7493 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 7493 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 7493 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 7493 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 7493 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 7179 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 7179 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 7179 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 7179 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 7179 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 7237 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 7237 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 7237 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 7237 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 9232 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 9232 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 9232 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 9232 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 9232 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 10125 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 10125 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 10125 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 10090 0 None 501 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8183252
CHEMBL429908 10090 0 None 501 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8183252
9651 8955 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 8955 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 10267 23 None 1 2 Rat 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588
3528 10267 23 None 1 2 Rat 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588
CHEMBL8823 10267 23 None 1 2 Rat 9.4 pKB = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588




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DOI

4236 34869 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 34869 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 7493 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 7493 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 7493 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 7493 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 7493 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 211929 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 211929 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 216556 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 216557 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 217972 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 219430 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 219187 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 222668 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 217891 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 215662 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 215662 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 215662 0 None -1 3 Human 10.0 pIC50 = 10.0 Binding
Displacement of radiolabeled endothelin-3 from human endothelin ETB receptorDisplacement of radiolabeled endothelin-3 from human endothelin ETB receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm8007618
CHEMBL438733 220570 0 None - 0 Bovine 10.0 pIC50 = 10.0 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]2CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N2)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00077a013
44284481 220504 0 None - 5 Bovine 9.9 pIC50 = 9.9 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00077a013
CHEMBL437472 220504 0 None - 5 Bovine 9.9 pIC50 = 9.9 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00077a013
44284481 220504 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 220504 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 117381 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 117381 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL1790962 215689 0 None - 1 Bovine 9.8 pIC50 = 9.8 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
CHEMBL427748 220151 0 None - 0 Bovine 9.8 pIC50 = 9.8 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
10603409 117381 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 117381 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 170158 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 170158 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 220504 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 220504 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 216111 7 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm3009103
CHEMBL263855 217373 0 None - 0 Bovine 9.6 pIC50 = 9.6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CC(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)NCC(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N2CCC[C@@H]2C(=O)N1)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00296-5
CHEMBL2373292 217154 0 None - 1 Bovine 9.6 pIC50 = 9.6 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
10839947 124080 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 124080 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 16125 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 16125 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 16125 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 16125 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 116749 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 116749 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 170158 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 170158 0 None - 0 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
CHEMBL1790963 215690 0 None - 0 Bovine 9.5 pIC50 = 9.5 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
10210629 15536 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 15536 0 None - 0 Pig 9.5 pIC50 = 9.5 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL2373291 217153 0 None - 1 Bovine 9.4 pIC50 = 9.4 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00077a013
CHEMBL411171 219646 0 None - 1 Bovine 9.4 pIC50 = 9.4 Binding
Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptorTested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00077a013
10187997 116749 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 116749 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 15536 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 15536 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 18894 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 18894 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 18894 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 6982 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 6982 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 6982 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 121569 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 121569 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 211465 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 211465 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 217639 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 16125 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 16125 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 120106 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 120106 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 177448 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 177448 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 18223 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 18223 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 18223 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 170158 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 170158 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 116749 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 116749 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 117381 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 117381 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 18885 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 18885 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 18885 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 18891 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 18891 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 18891 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 211465 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 211465 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 120106 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 120106 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 116416 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 116416 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 167891 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 167891 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 167891 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 175294 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 175294 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 216648 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 183282 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 183282 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 183282 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 145555 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 145555 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 109922 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 109922 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 8853 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 8853 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 8853 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 124080 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 124080 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 15536 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 15536 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 170692 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 170692 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 116533 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 116533 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 110575 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 110575 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 220504 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 220504 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 168571 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 168571 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 18229 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 18229 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 18229 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 112766 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 112766 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 109608 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 109608 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 18734 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 18734 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 18734 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 211327 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 211327 0 None - 0 Pig 8.7 pIC50 = 8.7 Binding
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 679 14 5 5 5.1 CCCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL411057 219639 0 None - 0 Bovine 8.0 pIC50 = 8 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
CHEMBL384792 219114 0 None - 0 Bovine 8.0 pIC50 = 8 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/S0960-894X(97)00296-5
CHEMBL405599 219347 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 219866 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 23351 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 23351 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 107586 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 107586 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 181050 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 181050 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 138139 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 138139 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 11414 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 11414 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 107299 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 107299 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 66591 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 66591 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 7493 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 7493 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 7493 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 7493 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 7493 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
CHEMBL407188 219424 0 None - 0 Bovine 6.0 pIC50 = 6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
44284481 220504 0 None - 5 Bovine 6.0 pIC50 = 6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00296-5
CHEMBL437472 220504 0 None - 5 Bovine 6.0 pIC50 = 6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00296-5
10814440 104923 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 104923 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 106770 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 106770 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 16945 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 16945 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 21406 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 21406 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 21406 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 113616 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 113616 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 211486 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 211486 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 217566 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 105335 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 105335 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 116781 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 116781 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 209980 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 209980 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 217654 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 119088 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 119088 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 213840 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 213840 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 213940 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 213940 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 214038 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 214038 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 214051 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 214051 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 214083 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 214083 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 214152 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 214152 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 214157 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 214157 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 214224 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 214224 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 214599 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 214599 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 217654 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 166154 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 166154 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 135459 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 135459 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 19176 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 19176 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 19176 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 106249 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 106249 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 106249 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 106249 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 68983 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 68983 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 138935 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 138935 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 25176 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 25176 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 68055 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 68055 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 25176 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 25176 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 124584 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 124584 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 109003 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 109003 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 213731 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 213731 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 91448 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 91448 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 138146 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 138146 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 92616 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 92616 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 213918 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 213918 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 18900 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 18900 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 18900 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 103898 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 103898 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 88476 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 88476 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 216245 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 113833 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 113833 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 11408 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 11408 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 168026 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 168026 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 109980 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 109980 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 7310 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 7310 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 7310 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 7310 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 16945 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 16945 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 106578 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 106578 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 169170 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 169170 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 220575 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 212260 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 212260 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 107664 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 107664 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 174955 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 174955 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 211527 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 211527 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 175007 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 175007 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 11285 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 11285 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 111669 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 111669 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 15998 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 15998 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 117361 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 117361 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 202595 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 202595 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 113609 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 113609 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 216363 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 98726 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 98726 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 103876 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 103876 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 25608 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 25608 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 88444 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 88444 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 25171 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 25171 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 88444 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 88444 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 25171 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 25171 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 92130 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 92130 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 66838 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 66838 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 88461 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 88461 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 67009 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 67009 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 104883 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 104883 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 67247 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 67247 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 16386 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 16386 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 16386 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
CHEMBL263294 217343 0 None - 0 Bovine 7.9 pIC50 = 7.9 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
CHEMBL385492 219131 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 6982 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 6982 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 6982 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 16386 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 16386 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 16386 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 55909 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 55909 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 57656 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 57656 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 455 6 1 6 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL410321 219591 0 None - 0 Bovine 6.9 pIC50 = 6.9 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NCC(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
9825494 209389 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 209389 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 216242 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 180772 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 180772 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 181225 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 181225 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 213493 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 213493 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 210969 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 210969 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 7319 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 7319 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 7319 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 112002 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 112002 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 21401 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 21401 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 21401 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 105341 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 105341 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 210668 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 210668 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 109477 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 109477 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 62210 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 62210 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 214360 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 214360 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 25645 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 25645 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 104994 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 104994 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 113622 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 113622 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 68758 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 68758 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 11415 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 11415 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 137004 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 137004 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 108070 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 108070 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 177662 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 177662 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 137476 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 137476 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 211000 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 211000 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 134584 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 134584 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 103904 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 103904 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 52080 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 52080 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 88782 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 88782 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 213676 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 213676 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 61019 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 61019 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 110349 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 110349 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 211777 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 211777 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 138167 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 138167 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 21416 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 21416 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 21416 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 210002 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 210002 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 210160 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 210160 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 216250 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 21356 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 21356 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 21356 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 11323 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 11323 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 218095 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 57759 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 57759 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 124858 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 124858 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 168686 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 168686 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 219473 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 14942 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 14942 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 11532 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 11532 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 209664 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 209664 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 210098 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 210098 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 215560 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 182032 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 182032 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 203277 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 203277 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 70098 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 70098 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 55390 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 55390 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 111530 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 111530 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 112572 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 112572 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 170257 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 170257 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 212295 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 212295 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 219939 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 118086 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 118086 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 216432 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 16183 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 16183 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 16183 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 134974 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 134974 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 67919 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 67919 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 113762 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 113762 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 119119 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 119119 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 164005 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 164005 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 108224 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 108224 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 103898 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 103898 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 66950 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 66950 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 111853 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 111853 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 11178 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 11178 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 11424 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 11424 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 174891 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 174891 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 109940 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 109940 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 113876 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 113876 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 220419 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 211764 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 211764 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 202683 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 202683 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 216244 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 222671 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 174572 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 174572 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 220473 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 169474 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 169474 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 21514 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 21514 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 21514 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 136874 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 136874 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 105341 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 105341 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 103872 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 103872 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 111981 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 111981 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 212011 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 212011 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 212189 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 212189 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 220654 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 113629 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 113629 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 190699 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 190699 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 190699 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 190699 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 215697 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 213819 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 213819 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 11165 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 11165 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 105204 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 105204 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 15689 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 15689 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 105543 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 105543 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 105543 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 105543 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 181959 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 181959 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 124263 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 124263 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 163376 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 163376 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 109110 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 109110 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 187895 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 187895 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 88454 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 88454 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 12237 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 12237 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 25206 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 25206 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 88465 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 88465 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 88465 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 88465 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 213425 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 213425 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 88472 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 88472 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 88787 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 88787 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 103335 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 103335 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 216241 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 103300 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 103300 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 176506 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 176506 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 68877 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 68877 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 103335 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 103335 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 168026 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 168026 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 222695 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 209685 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 209685 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 209791 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 209791 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 7493 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 7493 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 7493 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 7493 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 7493 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 222680 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 218095 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 7493 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 7493 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 7493 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 7493 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 7493 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 105342 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 105342 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 103534 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 103534 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 86358 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 86358 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 21408 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 21408 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 21408 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 215711 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 107113 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 107113 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 212042 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 212042 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 212253 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 212253 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 104954 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 104954 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 219873 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 209762 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 209762 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 113634 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 113634 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 12147 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 12147 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 88449 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 88449 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 174885 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 174885 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 67198 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 67198 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 135250 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 135250 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 18007 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 18007 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 18007 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 16183 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 16183 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 16183 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 16104 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 16104 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 25245 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 25245 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 66534 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 66534 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 25245 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 25245 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 18815 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 18815 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 18815 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 138222 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 138222 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 138222 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 88786 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 88786 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 108020 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 108020 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 103982 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 103982 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 218000 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 120152 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 120152 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 8107 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 8107 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 8107 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 8107 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 66401 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 66401 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 209731 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 209731 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 21558 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 21558 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 21558 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 211024 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 211024 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 58249 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 58249 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 106580 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 106580 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 216592 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 12022 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 12022 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 13095 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 13095 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 209595 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 209595 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 209732 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 209732 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 21407 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 21407 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 21407 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 11285 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 11285 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 210618 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 210618 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 210706 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 210706 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 21631 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 21631 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 21631 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 63119 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 63119 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 212318 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 212318 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 16089 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 16089 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 118092 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 118092 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 120097 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 120097 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 165770 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 165770 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 88473 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 88473 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 88470 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 88470 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 136786 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 136786 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 16183 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 16183 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 16183 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 104077 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 104077 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 107949 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 107949 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 126517 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 126517 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 106614 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 106614 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 169233 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 169233 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 210020 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 210020 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 111654 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 111654 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 216249 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 210888 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 210888 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 219482 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 220469 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 214671 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 214671 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 212056 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 212056 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 15260 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 15260 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 16511 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 16511 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 113611 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 113611 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 66457 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 66457 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 189629 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 189629 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 7735 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 7735 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 7735 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 7735 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 11929 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 11929 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 88448 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 88448 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 173609 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 173609 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 188460 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 188460 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 113849 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 113849 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 68273 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 68273 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 18220 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 18220 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 18220 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 137475 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 137475 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 13929 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 13929 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 209605 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 209605 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 21405 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 21405 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 21405 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 15363 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 15363 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 114798 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 114798 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 220416 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 107560 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 107560 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 209643 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 209643 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 209768 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 209768 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 107560 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 107560 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 21562 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 21562 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 21562 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 21566 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 21566 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 21566 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 217976 15 None - 1 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
11798999 214364 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 214364 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 217696 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 13746 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 13746 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 105084 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 105084 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 217696 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 7498 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 7498 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 7498 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 7498 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 218353 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 15922 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 15922 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 186391 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 186391 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 103747 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 103747 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 124408 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 124408 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 66025 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 66025 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 119467 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 119467 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 103746 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 103746 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 217588 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 217588 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 106903 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 106903 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 136516 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 136516 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 210897 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 210897 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 88457 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 88457 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 103669 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 103669 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 209950 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 209950 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 168596 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 168596 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 116846 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 116846 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 56304 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 56304 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 217998 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 16520 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 16520 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 67083 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 67083 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 217965 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 21652 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 21652 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 21652 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 21360 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 21360 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 21360 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 60309 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 60309 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 51382 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 51382 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 15641 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 15641 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 67222 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 67222 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 219894 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 7310 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 7310 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 7310 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 7310 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 103951 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 103951 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 108232 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 108232 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 88475 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 88475 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 88466 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 88466 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 7179 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 7179 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 7179 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 7179 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 7179 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 66439 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 66439 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 177624 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 177624 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 136519 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 136519 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 124406 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 124406 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 18011 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 18011 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 18011 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 163676 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 163676 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 25183 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 25183 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 37644 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 37644 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 201665 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 201665 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 201665 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 201665 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 66471 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 66471 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 134595 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 134595 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 134595 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 110519 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 110519 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 18224 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 18224 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 18224 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 109694 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 109694 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 174660 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 174660 0 None - 0 Pig 8.6 pIC50 = 8.6 Binding
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 580 12 5 5 3.8 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL414047 219884 0 None - 0 Bovine 8.6 pIC50 = 8.6 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CC(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)NCC(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N2CCC[C@@H]2C(=O)N1)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00296-5
44314750 172431 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 172431 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 107093 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 107093 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 117224 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 117224 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 18218 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 18218 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 18218 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 213079 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 213079 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 211475 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 211475 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 16013 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 16013 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 109924 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 109924 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 211826 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 211826 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 18210 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 18210 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 18210 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 217977 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 201891 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 201891 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 175261 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 175261 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 217902 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 70103 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 70103 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 129101 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 129101 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 127020 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 127020 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 209389 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 209389 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 107383 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 107383 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 206788 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 206788 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 210835 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 210835 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 210902 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 210902 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 118221 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 118221 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 104976 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 104976 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 169709 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 169709 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 169939 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 169939 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 200522 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 182830 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 182830 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 222671 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 215698 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 66840 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 66840 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 171369 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 171369 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 211783 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 211783 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 211925 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 211925 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 168615 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 168615 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 88452 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 88452 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 181739 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 181739 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 172833 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 172833 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 105733 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 105733 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 113751 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 113751 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 67851 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 67851 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 138163 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human 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 138163 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human 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 88441 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 88441 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 136429 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 136429 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 66389 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 66389 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 209499 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 209499 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 11281 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 11281 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 12997 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 12997 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 217344 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 103335 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 103335 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 174953 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 174953 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 179926 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 179926 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 107845 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 107845 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 106700 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 106700 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 186150 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 186150 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 210815 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 210815 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 104873 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 104873 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 215494 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 66023 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 66023 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 214085 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 214085 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 138156 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human 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 138156 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human 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 118340 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 118340 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 123319 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 123319 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 164166 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 164166 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 88451 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 88451 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 88451 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 88451 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 92124 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 92124 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 92125 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 92125 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 216252 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 210072 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 210072 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 21535 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 21535 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 21535 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 16998 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 16998 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 16998 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 105298 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 105298 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 107732 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 107732 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 97008 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 97008 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 106013 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 106013 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 212003 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 212003 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 113613 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 113613 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 17865 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 17865 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 17865 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 17865 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 137454 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 137454 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 11273 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 11273 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 67187 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 67187 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 104953 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 104953 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 105389 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 105389 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 68050 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 68050 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 216243 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 146079 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 146079 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 107076 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 107076 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 106264 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 106264 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 105132 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 105132 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 109092 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 109092 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 209740 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 209740 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 109005 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 109005 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 212022 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 212022 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 7498 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 7498 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 7498 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 7498 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 138576 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 138576 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 103822 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 103822 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 105248 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 105248 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 103718 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 103718 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 137343 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 137343 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 68160 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 68160 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 137340 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 137340 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 175671 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 175671 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 175671 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 16569 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 16569 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 108332 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 108332 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 201777 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 201777 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 216253 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 92131 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 92131 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 16581 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 16581 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 16581 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 214317 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 214317 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 106720 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 106720 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 113772 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 113772 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 113409 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 113409 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 113614 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 113614 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 109647 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 109647 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 174976 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 174976 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 137491 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 137491 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 11815 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 11815 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 171339 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 171339 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 180252 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 180252 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 212025 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 212025 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 113619 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 113619 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 113632 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 113632 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 67188 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 67188 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 88443 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 88443 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 213672 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 213672 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 92121 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 92121 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 112960 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 112960 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 216558 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 88783 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 88783 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 88477 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 88477 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 107132 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 107132 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 134319 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 134319 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 210907 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 210907 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 210996 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 210996 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 222667 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 113967 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 113967 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 169785 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 169785 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 66043 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 66043 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 169589 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 169589 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 110886 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 110886 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 211759 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 211759 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 12882 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 12882 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 117356 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 117356 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 113610 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 113610 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 98015 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 98015 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 108128 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 108128 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 169889 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 169889 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 135432 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 135432 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 211864 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 211864 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 120769 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 120769 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 113126 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 113126 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 16208 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 16208 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 116599 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 116599 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 222699 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 11964 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 11964 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 12478 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 12478 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 124405 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 124405 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 21553 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 21553 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 21553 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 68544 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 68544 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 15968 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 15968 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 217968 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 222673 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 203285 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 203285 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 214312 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 214312 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 214694 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 214694 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 112183 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 112183 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 15689 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 15689 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 117236 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 117236 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 68051 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 68051 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 68551 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 68551 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 68070 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 68070 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 117445 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 117445 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 15968 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 15968 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 126717 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 126717 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 216246 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 216431 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 58209 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 58209 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 15909 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 15909 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 210263 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 210263 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 211558 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 211558 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 23174 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 23174 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 203191 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 203191 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 103590 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 211793 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 211793 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 212294 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 212294 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 103831 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 103831 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 108305 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 108305 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 18013 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 18013 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 18013 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 213827 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 213827 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 92002 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 92002 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 211818 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 211818 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 116558 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 116558 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 116558 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 103471 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 103471 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 105433 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 105433 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 113983 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 113983 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 7493 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 7493 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 7493 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 7493 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 7493 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 107844 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 107844 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 209691 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 209691 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 210285 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 210285 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 202456 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 202456 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 109904 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 109904 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 174911 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 174911 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 119579 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 119579 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 88438 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 88438 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 103983 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 103983 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 116445 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 116445 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 25257 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 25257 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 25257 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 25257 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 181859 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 181859 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 68380 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 68380 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 118412 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 118412 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 216241 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 216252 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 178382 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 178382 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 180705 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 180705 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 219381 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 21564 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 21564 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 21564 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 135287 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 135287 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 21561 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 21561 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 21561 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 119465 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 119465 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 103776 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 103776 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 106132 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 106132 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 211991 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 211991 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 113627 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 113627 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 113885 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 113885 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 182705 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 182705 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 174599 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 174599 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 135252 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 135252 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 213929 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 213929 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 67014 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 67014 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 210393 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 67183 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 67183 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 66657 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 66657 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 175284 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 175284 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 16624 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 16624 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 67838 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 67838 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 112750 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 112750 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 113733 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 113733 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 18222 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 18222 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 18222 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 18734 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 18734 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 18734 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 113777 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 113777 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 18902 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 18902 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 18902 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 19177 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 19177 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 19177 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 113578 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 113578 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 176348 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 176348 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 175022 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 175022 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 109608 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 109608 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 175294 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 175294 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 544 10 2 6 5.4 CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.1021/jm990170q
CHEMBL408437 219492 0 None - 0 Bovine 8.4 pIC50 = 8.4 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CC(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)NCC(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N2CCC[C@@H]2C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/S0960-894X(97)00296-5
10769177 119689 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 119689 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 19015 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 19015 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 19015 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 124243 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 124243 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 148190 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 148190 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 215554 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 11873 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 11873 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 56195 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 56195 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 26153 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 26153 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 107503 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 107503 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 113689 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 113689 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 174926 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 174926 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 206610 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 206610 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 210538 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 210538 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 213493 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 213493 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 175368 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 175368 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 126267 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 126267 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 425 5 1 5 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL414168 219895 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
CHEMBL436894 220472 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
CHEMBL437610 220506 0 None - 0 Bovine 5.5 pIC50 = 5.5 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
10767505 12072 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 12072 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 119581 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 119581 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 217671 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 212312 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 212312 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 16131 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 16131 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 168778 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 168778 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 67189 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 67189 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 218454 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 92002 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 92002 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 108048 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 108048 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 173688 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 173688 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 123764 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 123764 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 88442 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 88442 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 214013 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 214013 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 104037 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 104037 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 135802 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 135802 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 16851 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 16851 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 16851 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 18888 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 18888 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 18888 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 216248 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 113845 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 113845 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 7493 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 7493 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 7493 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 7493 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 7493 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 108325 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 108325 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 91678 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 91678 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 180193 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 180193 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 209445 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 209445 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 16032 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 16032 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 105365 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 105365 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 105365 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 105365 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 25251 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 25251 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 25251 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 25251 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 214055 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 214055 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 176937 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 176937 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 214350 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 214350 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 67136 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 67136 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 135825 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human 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 135825 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human 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 14048 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 14048 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 21404 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 21404 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 21404 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 113621 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 113621 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 176667 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 176667 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 15689 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 15689 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 88468 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 88468 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 68127 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 68127 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 135277 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 135277 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 106324 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 106324 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 179677 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 179677 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 173316 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 173316 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 113405 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 113405 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 172927 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 172927 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 216096 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 216598 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 137927 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 137927 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 222693 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 178263 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 178263 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 109783 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 109783 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 212290 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 212290 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 222671 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 113625 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 113625 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 222671 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 169146 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 169146 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 212220 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 212220 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 113620 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 113620 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 115316 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 115316 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 66750 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 66750 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 66568 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 66568 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 213854 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 213854 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 15272 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 15272 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 111142 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 111142 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 103300 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 103300 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 103553 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 103553 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 103553 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 103553 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 124409 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 124409 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 9803 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 9803 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 9803 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 9803 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 21402 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 21402 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 21402 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 21565 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 21565 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 21565 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 210806 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 210806 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 174615 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 174615 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 175349 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 175349 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 213024 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 213024 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 16323 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 16323 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 119875 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 119875 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 216433 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 67108 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 67108 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 67862 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 67862 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 67108 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 67108 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 88458 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 88458 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 80288 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 80288 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 92120 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 92120 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 88459 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 88459 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 67186 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 67186 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 209583 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 209583 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 218069 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 168562 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 168562 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 103602 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 103602 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 103602 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 210162 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 210162 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 55674 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 55674 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 107412 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 107412 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 209770 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 209770 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 168445 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 168445 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 220532 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 214356 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 214356 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 51423 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 51423 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 111193 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 111193 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 169814 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 169814 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 16481 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 16481 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 16626 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 16626 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 116499 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 116499 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 118131 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 118131 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 136597 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 136597 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 135249 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 135249 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 103745 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 103745 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 213454 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 213454 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 108209 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 108209 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 116446 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 116446 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 103719 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 103719 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 118114 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 118114 0 None - 0 Pig 7.4 pIC50 = 7.4 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 532 12 1 7 3.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC 10.1021/jm970101g
CHEMBL267754 217509 0 None - 0 Bovine 7.4 pIC50 = 7.4 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
CHEMBL327350 218069 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 209735 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 209735 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 16424 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 16424 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 115445 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 115445 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 113615 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 113615 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 68161 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 68161 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 135800 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 135800 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 220048 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 222690 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 212239 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 212239 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 136252 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 136252 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 108222 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 108222 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 213791 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 213791 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 88460 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 88460 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 213012 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 213012 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 16369 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 16369 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 16369 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 16369 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 16369 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 16369 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 106840 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 106840 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 212057 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 212057 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 212051 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 212051 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 213344 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 213344 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 103538 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 103538 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 14667 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 14667 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 108253 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 108253 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 112390 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 112390 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 113624 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 113624 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 9232 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 9232 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 9232 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 9232 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 9232 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 9232 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 9232 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 9232 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 9232 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 9232 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 91930 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 91930 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 91930 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 91930 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 66408 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 66408 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 213769 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 213769 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 15878 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 15878 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 213934 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 213934 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 213774 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 213774 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 109924 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 109924 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 170970 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 170970 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 136517 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 136517 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 212984 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 212984 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 66710 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 66710 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 105383 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 105383 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 136517 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 136517 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 170210 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 170210 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 211899 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 211899 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 213488 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 213488 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 213488 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 170160 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 170160 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 6982 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 6982 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 6982 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 109983 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 109983 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 104904 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 104904 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 109701 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 109701 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 213189 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 213189 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 113734 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 113734 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 106042 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 106042 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 215672 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 214085 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 214085 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 103226 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 103226 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 170019 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 170019 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 209578 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 209578 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 210288 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 210288 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 201730 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 201730 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 21560 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 21560 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 21560 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 209578 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 209578 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 211733 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 211733 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 209961 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 209961 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 216558 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 217965 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 213590 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 213590 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 104084 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 104084 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 103851 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 103851 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 78984 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 78984 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 186214 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 186214 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 165018 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 165018 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 126596 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 126596 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 175040 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 175040 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 16386 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 16386 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 16386 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 104085 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 104085 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 210156 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 210156 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 11384 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 11384 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 16541 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 16541 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 16011 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 16011 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 66023 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 66023 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 67840 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 67840 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 68059 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 68059 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 177197 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 177197 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 88453 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 88453 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 214333 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 214333 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 179243 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 179243 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 106334 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 106334 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 106357 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 106357 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 52580 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 52580 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 146353 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 146353 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 66509 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 66509 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 18005 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 18005 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 18005 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 115058 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 115058 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 213755 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 213755 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 70031 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 70031 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 116445 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 116445 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 92129 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 92129 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 88455 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 88455 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 172416 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 172416 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 66704 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 66704 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 209674 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 209674 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 210872 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 210872 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 106911 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 106911 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 143710 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 143710 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 210872 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 210872 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 56152 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 56152 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 201446 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 201446 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 148441 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 148441 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 220411 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 220411 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 173502 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 173502 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 209874 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 209874 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 14964 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 14964 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 186332 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 186332 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 213414 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 213414 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 25201 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 25201 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 120147 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 120147 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 112715 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 112715 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 66749 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 66749 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 182354 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 182354 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 213222 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 213222 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 211410 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 211410 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 25799 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 25799 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 148190 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 148190 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 11100 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 11100 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 88779 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 88779 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 88779 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 88779 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 169479 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 169479 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 136261 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 136261 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 179527 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 179527 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 136877 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 136877 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 456 6 1 6 4.8 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL407422 219440 0 None - 0 Bovine 7.4 pIC50 = 7.4 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
44284184 146778 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 146778 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 490 8 2 7 5.0 CCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL409433 219542 0 None - 0 Bovine 6.4 pIC50 = 6.4 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
44458399 105768 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 105768 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 217892 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 222672 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 108820 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 108820 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 106924 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 106924 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 11930 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 11930 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 210839 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 210839 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 214708 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 214708 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 212035 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 212035 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 173893 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 173893 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 124404 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 124404 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 15878 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 15878 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 105011 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 105011 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 17865 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 17865 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 17865 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 17865 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 17865 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 17865 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 17865 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 17865 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 88471 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 88471 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 88776 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 88776 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 103776 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 103776 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 67070 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 67070 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 210310 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 210310 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 23218 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 23218 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 88462 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 88462 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 21403 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 21403 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 21403 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 217974 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 211910 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 211910 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 88450 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 88450 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 88781 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 88781 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 88447 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 88447 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 88447 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 88447 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 67154 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 67154 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 88440 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 88440 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 160386 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 160386 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 173120 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 173120 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 173120 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 127840 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 127840 0 None - 0 Pig 6.3 pIC50 = 6.3 Binding
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 498 9 2 5 4.6 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL414131 219892 0 None - 0 Bovine 6.3 pIC50 = 6.3 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
11059249 109395 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 109395 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 209623 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 209623 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 220404 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 112180 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 112180 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 114155 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 114155 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 217697 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 211805 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 211805 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 15038 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 15038 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 16525 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 16525 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 56741 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 56741 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 94798 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 94798 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 115391 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 115391 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 107132 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 107132 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 213493 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 213493 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 209755 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 209755 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 21399 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 21399 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 21399 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 106886 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 106886 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 107794 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 107794 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 177402 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 177402 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 215494 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 16060 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 16060 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 115343 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 115343 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 16329 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 16329 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 175370 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 175370 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 68879 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 68879 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 209795 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 209795 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 138138 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 138138 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 210886 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 210886 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 107331 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 107331 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 169854 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 169854 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 170054 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 170054 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 51366 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 51366 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 104340 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 104340 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 212384 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 212384 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 168409 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 168409 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 105155 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 105155 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 18216 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 18216 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 18216 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 18906 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 18906 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 18906 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 109694 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 109694 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 162530 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 162530 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 106933 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 106933 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 211188 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 211188 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 16057 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 16057 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 16203 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 16203 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 109813 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 109813 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 168134 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 168134 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 107102 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 107102 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 106760 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 106760 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 120567 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 120567 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 217902 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 68540 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 68540 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 10966 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 10966 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 201367 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 201367 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 201778 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 201778 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 107495 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 107495 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 459 8 1 6 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
3911 10090 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
CHEMBL429908 10090 0 None - 0 Bovine 5.3 pIC50 = 5.3 Binding
Binding activity to ET-B receptor on bovine cerebellum membraneBinding activity to ET-B receptor on bovine cerebellum membrane
ChEMBL None None None None 10.1016/S0960-894X(97)00296-5
CHEMBL329609 218097 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 16404 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 16404 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 213580 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 213580 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 116550 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 116550 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 66676 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 66676 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 213181 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 213181 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 88780 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 88780 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 88778 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 88778 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 16433 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 16433 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 217999 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 106971 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 106971 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 16433 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 16433 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 21358 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 21358 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 21358 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 137669 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 137669 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 7310 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 7310 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 7310 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 7310 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 213422 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 213422 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 180527 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 180527 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 18001 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 18001 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 18001 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 222704 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 209896 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 209896 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 108570 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 108570 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 7310 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 7310 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 7310 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 7310 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 57684 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 57684 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 110953 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 110953 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 111655 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 111655 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 104022 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 104022 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 214320 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 214320 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 107580 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 107580 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 108868 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 108868 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 88437 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 88437 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 136873 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 136873 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 88775 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 88775 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 88775 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 88775 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 213896 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 213896 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 216251 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 11855 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 11855 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 116430 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 116430 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 112304 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 112304 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 210788 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 210788 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 214379 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 214379 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 68142 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 68142 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Tested for the inhibitory activity of cloned human ETB receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for the inhibitory activity of cloned human ETB receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 482 5 1 7 4.8 Cc1cc2c(cc1/C=C/c1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL409339 219540 0 None - 0 Bovine 7.3 pIC50 = 7.3 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
44284115 106971 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 106971 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 209599 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 209599 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 202459 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 202459 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 105634 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 105634 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 16512 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 16512 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 113623 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 113623 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 67218 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 67218 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 67106 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 67106 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 182112 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 182112 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 25179 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 25179 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 25179 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 25179 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 21398 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 21398 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 21398 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 214360 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 214360 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 50522 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 50522 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 188373 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 188373 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 128298 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 128298 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 111316 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 111316 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 67149 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 67149 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 138143 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 138143 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 219894 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 88464 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 88464 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 88464 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 88464 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 88478 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 88478 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 181748 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 181748 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 217414 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 202648 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 202648 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 104021 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 104021 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 137995 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 137995 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 88474 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 88474 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 165756 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 165756 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 119252 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 119252 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 88463 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 88463 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 137665 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 137665 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 182081 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 182081 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 182055 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 182055 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 182104 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 182104 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 16165 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 16165 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 23105 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 23105 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 107534 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 107534 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 214879 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 214879 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 103611 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 103611 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 21387 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 21387 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 92118 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 92118 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 107534 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 107534 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 213774 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 213774 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 210047 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 210047 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 109497 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 109497 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 209684 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 209684 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 212259 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 212259 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 63297 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 63297 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 107970 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 107970 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 216250 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 219347 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 162483 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 162483 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 103538 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 103538 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 209614 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 209614 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 182694 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 182694 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 212200 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 212200 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 119335 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 119335 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 127603 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 127603 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 213769 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 213769 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 106760 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 106760 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 18897 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 18897 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 18897 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 109802 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 109802 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 179451 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 179451 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 117148 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 117148 0 None - 0 Pig 8.2 pIC50 = 8.2 Binding
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 566 13 1 7 3.9 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL438745 220572 0 None - 0 Bovine 8.2 pIC50 = 8.2 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
44320783 113470 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 113470 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 6982 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 6982 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 6982 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 18215 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 18215 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 18215 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 121026 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 121026 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 16142 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 16142 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 219770 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 218095 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 220416 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 105549 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 105549 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 177147 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 177147 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 217902 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 215695 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 105549 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 105549 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 142196 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 142196 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 210921 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 210921 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 18892 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 18892 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 18892 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 148567 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 148567 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 109620 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 109620 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 120290 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 120290 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 7319 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 7319 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 7319 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 110369 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 110369 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 215709 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 217988 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 16213 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 16213 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 107731 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 107731 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 15924 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 15924 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 97074 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 97074 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 67223 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 67223 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 213479 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 213479 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 107079 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 107079 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 15028 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 15028 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 111678 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 111678 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 210094 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 210094 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 216597 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 108167 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 108167 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 218353 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 119154 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 119154 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 177895 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 177895 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 138577 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 138577 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 162720 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 162720 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 182198 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 182198 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 107900 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 107900 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 169937 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 169937 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 117010 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 117010 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 106913 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 106913 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 25799 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 25799 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 16439 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 16439 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 174911 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 174911 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 213480 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 213480 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 213614 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 213614 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 177716 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 177716 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 174601 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 174601 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 174779 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 174779 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 109076 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 109076 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 7310 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 7310 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 7310 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 7310 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 168454 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 168454 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 13668 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 13668 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 18779 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 18779 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 18779 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 12639 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 12639 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 128065 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 128065 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 56292 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 56292 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 210129 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 210129 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 16510 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 16510 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 214275 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 214275 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 117212 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 117212 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 213303 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 213303 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 115967 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 115967 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 92119 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 92119 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 219866 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 172565 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 172565 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 67954 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 67954 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 15922 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 15922 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 88467 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 88467 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 135463 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 135463 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 115641 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 115641 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 52139 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 52139 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 171644 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 171644 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 212226 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 212226 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 216435 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 51458 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 51458 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 137470 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 137470 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 138586 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 138586 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 68149 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 68149 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 104893 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 104893 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 51466 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 51466 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 106128 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 106128 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 212256 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 212256 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 16114 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 16114 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 68051 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 68051 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 138321 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 138321 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 190467 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 190467 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 190405 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 190405 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 180895 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 180895 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 25260 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 25260 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 15956 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 15956 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 201611 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 201611 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 21357 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 21357 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 21357 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 55638 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 55638 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 216596 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 107577 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 107577 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 92122 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 92122 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 109039 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 109039 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 176386 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 176386 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 10125 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 10125 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 10125 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 209966 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 209966 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 97008 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 97008 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 105978 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 105978 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 209642 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 209642 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 67197 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 67197 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 174930 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 174930 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 164429 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 164429 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 16083 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 16083 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 17031 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 17031 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 17031 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 105424 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 105424 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 211916 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 211916 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 18889 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 18889 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 18889 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 530 10 2 6 4.9 CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL384792 219114 0 None - 0 Bovine 8.1 pIC50 = 8.1 Binding
Binding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparationBinding activity against Endothelin B receptor expressed from bovine cerebellum membrane preparation
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)C[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(96)00127-8
44314658 211947 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 211947 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 217895 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 217895 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 211267 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 211267 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 210964 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 210964 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 211987 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 211987 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 118085 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 118085 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 106137 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 106137 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 222667 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 105009 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 105009 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 127175 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 127175 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 108946 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 108946 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 209754 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 209754 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 16346 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 16346 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 88777 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 88777 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 25183 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 25183 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 210179 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 210179 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 209602 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 209602 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 16422 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 16422 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 16324 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 16324 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 107944 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 107944 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 66845 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 66845 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 115986 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 115986 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 218106 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 222703 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 209759 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 209759 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 66676 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 66676 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 21228 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 21228 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 219736 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 106340 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 106340 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 112458 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 112458 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 186342 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 186342 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 107591 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 107591 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 19189 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 19189 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 19189 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 66836 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 66836 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 138155 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 138155 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 210148 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 210148 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 213402 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 213402 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 219355 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 138142 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 138142 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 163626 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 163626 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 19131 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 19131 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 19131 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 109633 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 109633 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 88446 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 88446 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 105288 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 105288 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 105006 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 105006 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 209698 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 209698 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 219353 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 209432 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 209432 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 127071 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 127071 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 14312 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 14312 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 137442 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 137442 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 209989 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 209989 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 210963 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 210963 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 26093 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 26093 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 214718 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 214718 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 116045 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 116045 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 105541 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 105541 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 180123 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 180123 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 180123 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 180123 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 210191 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 210191 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 107079 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 107079 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 213493 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 213493 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 169701 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 169701 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 213493 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 213493 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 216434 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 213493 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 213493 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 88439 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 88439 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 209621 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 209621 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 212300 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 212300 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 106790 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 106790 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 137940 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 137940 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 213545 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 213545 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 108981 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 108981 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 18230 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 18230 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 18230 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 16386 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 16386 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 16386 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 11306 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 11306 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 55367 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 55367 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 113338 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 113338 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 219113 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 210199 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 210199 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 216443 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 104983 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 104983 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 51350 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 51350 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 170135 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 170135 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 117031 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 117031 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 170135 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 170135 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 70100 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 70100 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 111979 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 111979 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 67044 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 67044 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 164189 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 164189 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 213125 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 213125 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 120346 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 120346 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 67220 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 67220 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 113851 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 113851 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 88784 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 88784 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 26233 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 26233 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 18004 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 18004 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 18004 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 119286 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 119286 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 22351 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 22351 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 23363 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 23363 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 178556 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 178556 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 21651 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 21651 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 21651 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 21359 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 21359 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 21359 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 68436 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 68436 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 188963 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 188963 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 67125 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 67125 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 213060 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 213060 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 105469 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 105469 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 120575 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 120575 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 88785 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 88785 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 215699 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 172961 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 172961 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 136450 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 136450 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 169938 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 169938 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 104044 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 104044 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 66382 0 None - 2 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human 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 66382 0 None - 2 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human 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 217890 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 113628 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 113628 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 114184 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 114184 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 105567 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 105567 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 16466 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 16466 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 210195 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 210195 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 201764 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 201764 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 16221 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 16221 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 105222 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 105222 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 10973 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 10973 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 11285 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 11285 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 177698 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 177698 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 15359 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 15359 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 25196 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 25196 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 216247 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 11377 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 11377 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 106044 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 106044 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 216240 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 176272 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 176272 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 66400 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 66400 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 107188 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 107188 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 7310 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 7310 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 7310 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 7310 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 12142 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 12142 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 209603 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 209603 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 112568 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 112568 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 214096 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 214096 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 138124 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 138124 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 113834 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 113834 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 106728 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 106728 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 136260 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 136260 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 115331 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 115331 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 15681 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 15681 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 106911 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 106911 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 113922 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 113922 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 112735 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 112735 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 213220 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 213220 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 179856 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 179856 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 105700 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 105700 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 217414 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 107275 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 107275 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 213488 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 213488 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 213488 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 16184 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 16184 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 211718 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 211718 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 137465 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 137465 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 67289 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 67289 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 213863 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 213863 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 66771 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 66771 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 92128 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 92128 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 188048 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 188048 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 217654 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 107935 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 107935 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 217654 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 108053 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 108053 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 25257 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 25257 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 181579 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 181579 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 68111 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 68111 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 113626 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 113626 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 107688 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 107688 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 18012 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 18012 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 18012 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 66963 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 66963 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 117108 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 117108 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 211988 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 211988 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 16554 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 16554 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 92615 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 92615 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 217970 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 217970 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 138118 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 138118 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 165037 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 165037 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 134528 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 134528 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 105828 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 105828 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 202630 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 202630 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 115402 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 115402 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 212052 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 212052 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 16216 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 16216 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 103988 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 103988 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 25685 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 25685 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 172961 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 172961 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 16085 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 16085 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 88445 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 88445 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 213034 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 213034 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 66795 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 66795 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 213711 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 213711 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 117723 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 117723 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 218095 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 117723 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 117723 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 66437 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 66437 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 163259 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 163259 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 66831 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 66831 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 169664 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 169664 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 213422 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 213422 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 217971 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 10382 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 10382 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 10382 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 10382 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 10382 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 10382 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 16554 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 16554 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 9232 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 9232 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 9232 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 9232 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 9232 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 7237 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 7237 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 7237 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 7237 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 7237 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 7237 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 7237 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 7237 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 110355 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 110355 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 67861 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 67861 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 67074 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 67074 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 220504 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 220504 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 10245 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 10245 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 10245 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 10245 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 10245 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 10245 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 10245 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 10245 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 10245 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 10245 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 220504 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 220504 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 180014 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 180014 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 215662 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 215662 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 180014 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 180014 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 215662 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 215662 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 220504 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 220504 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 173228 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 173228 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 173228 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 111130 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 111130 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 174935 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 174935 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 109599 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 109599 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 109943 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 109943 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 211333 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 211333 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 109795 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 109795 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 211248 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 211248 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 162500 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 162500 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 162500 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 111568 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 111568 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 211345 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 211345 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 211397 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 211397 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 109862 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 109862 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 109810 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 109810 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 109968 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 109968 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 109850 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 109850 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 109861 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 109861 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 211457 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 211457 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 210948 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 210948 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 211442 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 211442 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 168040 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 168040 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 168040 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 8853 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 8853 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 8853 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 168052 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 168052 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 8853 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 8853 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 8853 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 112190 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 112190 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 112190 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 112190 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 206563 0 None -1 2 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 206563 0 None -1 2 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 211228 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 211228 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 101575 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 101575 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 101575 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 101575 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 109013 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 109013 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 48225 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 48225 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 11609 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 11609 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 152214 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 152214 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 107439 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 107439 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 168501 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 168501 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 174730 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 174730 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 169996 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 169996 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 108859 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 108859 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 113752 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 113752 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 106544 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 106544 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 174730 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 174730 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 11233 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 11233 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 50827 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 50827 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 109807 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 109807 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 211243 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 211243 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 107628 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 107628 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 45874 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 45874 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 127892 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 127892 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 128045 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 128045 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 112770 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 112770 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 12088 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 12088 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 116455 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 116455 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 16369 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 16369 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 16369 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 105304 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 105304 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 50647 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 50647 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 109072 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 109072 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 209890 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 209890 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 210227 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 210227 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 106160 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 106160 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 16183 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 16183 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 16183 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 16183 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 16183 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 16183 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 213422 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 213422 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 213493 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 213493 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 9803 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 9803 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 9803 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 9803 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 190785 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 190785 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 114434 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 114434 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 10267 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 10267 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 10267 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 10267 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 10267 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 10267 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 7493 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 7493 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 7493 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 7493 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 7493 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 49841 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 49841 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 109388 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 109388 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 106121 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 106121 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 108685 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 108685 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 92120 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 92120 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 108273 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 108273 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 126429 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 126429 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 210308 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 210308 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 106640 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 106640 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 49255 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 49255 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 51317 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 51317 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 92122 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 92122 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 170089 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 170089 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 11392 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 11392 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 109564 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 109564 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 116521 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 116521 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 126287 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 126287 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 128770 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 128770 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 206613 0 None -707 2 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 206613 0 None -707 2 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 11438 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 11438 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 11854 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 11854 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 12081 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 12081 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 210395 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 210395 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 11854 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 11854 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 108000 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 108000 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 108245 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 108245 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 126069 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 126069 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 7735 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 7735 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 7735 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 7735 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 10267 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 10267 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 10267 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 167531 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 167531 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 167531 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 210476 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 210476 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 7457 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 7457 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 7457 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 7457 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 7457 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 7457 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 7457 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 7457 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 7457 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 109106 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 109106 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 51266 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 51266 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 128299 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 128299 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 109708 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 109708 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 7457 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 7457 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 7457 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 107573 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 107573 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 174684 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 174684 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 48390 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 48390 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 126633 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 126633 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 128271 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 128271 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 108957 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 108957 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 114138 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 114138 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 105182 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 105182 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 108929 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 108929 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 171666 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 171666 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 175081 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 175081 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 48483 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 48483 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 49044 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 49044 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 126333 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 126333 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 11744 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 11744 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 128750 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 128750 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 11502 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 11502 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 46079 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 46079 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 46338 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 46338 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 11303 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 11303 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 114076 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 114076 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 49100 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 49100 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 107875 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 107875 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 128074 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 128074 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 111567 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 111567 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 11509 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 11509 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 11126 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 11126 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 109678 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 109678 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 206642 0 None -218 2 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 206642 0 None -218 2 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 206642 0 None -218 2 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 206642 0 None -218 2 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 48652 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 48652 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 107169 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 107169 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 181458 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 181458 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 11381 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 11381 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 109483 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 109483 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 210369 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 210369 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 108150 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 108150 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 168039 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 168039 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 48308 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 48308 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 108521 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 108521 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 107746 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 107746 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 126452 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 126452 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 108079 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 108079 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 64841 0 None -74 2 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 64841 0 None -74 2 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 109106 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 109106 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 50817 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 50817 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 211249 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 211249 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 103378 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 103378 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 11439 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 11439 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 211350 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 211350 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 106339 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 106339 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 210437 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 210437 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 49848 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 49848 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 126288 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 126288 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 46255 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 46255 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 106065 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 106065 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 116180 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 116180 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 108761 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 108761 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 7498 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 7498 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 7498 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 7498 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 106010 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 106010 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 7493 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 7493 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 7493 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 7493 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 7493 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 115243 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 115243 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 173697 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 173697 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 209842 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 209842 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 175859 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 175859 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 175859 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 175859 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 106336 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 106336 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 64840 0 None -10 2 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 64840 0 None -10 2 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 45799 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 45799 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 101575 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 101575 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 8107 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 8107 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 8107 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 8107 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 105991 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 105991 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 126014 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 126014 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 48846 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 48846 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 210889 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 210889 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 114007 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 114007 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 114007 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 114007 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 114269 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 114269 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 21349 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 21349 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 21349 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 106479 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 106479 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 16386 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 16386 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 16386 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 128319 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 128319 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 64837 0 None -295 2 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 64837 0 None -295 2 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 50887 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 50887 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 108573 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 108573 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 107750 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 107750 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 107750 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 107750 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 49623 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 49623 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 106644 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 106644 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 100861 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 100861 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 210537 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 210537 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 106116 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 106116 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 46360 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 46360 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 166881 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 166881 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 109630 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 109630 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 163955 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 163955 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 163955 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 213488 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 213488 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 213488 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 162540 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 162540 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 162540 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 127846 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 127846 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 162536 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 162536 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 162536 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 49610 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 49610 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 64839 0 None -1230 2 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 64839 0 None -1230 2 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 49099 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 49099 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 47949 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 47949 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 11105 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 11105 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 107131 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 107131 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 108929 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 108929 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 128215 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 128215 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 109678 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 109678 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 126632 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 126632 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 106122 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 106122 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 115335 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 115335 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 127837 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 127837 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 113472 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 113472 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 109086 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 109086 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 212993 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 212993 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 128747 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 128747 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 11204 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 11204 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 48471 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 48471 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 105587 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 105587 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 64843 0 None -812 2 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 64843 0 None -812 2 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 48102 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 48102 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 126547 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 126547 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 11321 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 11321 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 7498 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 7498 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 7498 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 7498 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 212979 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 212979 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 114203 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 114203 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 208001 0 None -2 2 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 208001 0 None -2 2 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 106011 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 106011 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 48088 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 48088 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 127863 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 127863 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 148430 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 148430 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 85926 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 85926 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 12252 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 12252 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 107017 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 107017 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 7493 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 7493 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 7493 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 7493 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 7493 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 171191 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 171191 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 105030 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 105030 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 46467 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 46467 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 64838 0 None -3548 2 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 64838 0 None -3548 2 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 175986 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 175986 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 64842 0 None -123 2 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 64842 0 None -123 2 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 113722 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 113722 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 106716 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 106716 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 170104 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 170104 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 171641 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 171641 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 47766 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 47766 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 11590 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 11590 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 114437 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 114437 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 109300 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 109300 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 209321 0 None -263 2 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 209321 0 None -263 2 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 172116 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 172116 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 109471 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 109471 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 208111 0 None -39 2 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 208111 0 None -39 2 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 107821 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 107821 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 49617 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 49617 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 171962 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 171962 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 180252 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 180252 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 224518 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 10382 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 10382 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 10382 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 10382 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 10382 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 10382 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 9232 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 9232 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 9232 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 9232 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 9232 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 10413 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16130933 10413 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16133819 10413 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3886 10413 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
56947141 10413 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
CHEMBL3188091 10413 0 None -3 2 Human 10.0 pKd = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3887 8853 45 None -7 4 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
5311192 8853 45 None -7 4 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL72410 8853 45 None -7 4 Human 7.2 pKd = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1010 7500 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 7500 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 6982 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 6982 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 6982 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 7122 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1472961
1008 10246 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
1008 10246 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16132429 10246 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
16132429 10246 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL1790178 10246 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
CHEMBL1790178 10246 0 None -15 2 Human 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1007 10413 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16130933 10413 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16133819 10413 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3886 10413 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
56947141 10413 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
CHEMBL3188091 10413 0 None 3 2 Rat 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
1004 8346 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
1004 8346 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16219334 8346 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
16219334 8346 0 None -2 2 Rat 10.3 pKd None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1008 10246 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
1008 10246 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16132429 10246 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
16132429 10246 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL1790178 10246 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
CHEMBL1790178 10246 0 None 15 2 Rat 10.5 pKd None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1004 8346 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7524189
1004 8346 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8460684
1004 8346 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16219334 8346 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7524189
16219334 8346 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8460684
16219334 8346 0 None 2 2 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1010 7500 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 7500 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 109619 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 109619 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 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
1973 210262 15 125I-ENDOTHELIN -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 210262 15 125I-ENDOTHELIN -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 210262 15 125I-ENDOTHELIN -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
None 223272 0 125I-ENDOTHELIN -10471285 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 372 2 1 3 4.4 CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl None
104865 7493 99 125I-ENDOTHELIN -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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 7493 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 222855 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 7179 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 7179 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 7179 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 7179 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 7179 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 7493 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 7493 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 7493 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 7493 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 7493 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 7735 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 7735 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 7735 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 7735 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 7310 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 7310 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 7310 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 7310 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 7457 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 7457 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 7457 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 7493 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 7493 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 7493 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 7493 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 7493 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 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
1007 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16130933 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
16130933 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16133819 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
16133819 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
3886 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
3886 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
56947141 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
56947141 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
CHEMBL3188091 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
CHEMBL3188091 10413 0 None -3 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16133801 7499 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7733918
3859 7499 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7733918