| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T92828 | ||||
| Target Name | Endothelin B receptor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Compound ET-3 | Drug Info | IC50 = 3000 nM | ||
| Linear peptide of RES-701-1 | Drug Info | IC50 = 5000 nM | |||
| W-F-F-N--Y-Y-W | Drug Info | IC50 = 15000 nM | |||
| BMS-193884 | Drug Info | Ki = 18700 nM | [525859] | ||
| Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Ser-Val-Tyr-Phe-Cys) | Drug Info | IC50 = 1700 nM | |||
| Compound RES-701-1(1-10)/[A15]ET-1 | Drug Info | IC50 = 0.24 nM | |||
| RES-701-1 | Drug Info | IC50 = 10 nM | |||
| Compound [S15]ET-1 | Drug Info | IC50 = 1000 nM | |||
| PD-155080 | Drug Info | IC50 = 4550 nM | |||
| Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Val-Tyr-Phe-Cys) | Drug Info | IC50 = 1700 nM | |||
| IRL-1722 | Drug Info | Ki = 16 nM | |||
| Bosentan | Drug Info | IC50 = 38~152 nM | |||
| Compound SRTX6b | Drug Info | IC50 = 3000 nM | |||
| PD-163140 | Drug Info | IC50 = 1800 nM | |||
| Bhg-F-N-Y-Y-W | Drug Info | IC50 = 13000 nM | |||
| IRL-2500 | Drug Info | Ki = 1 nM | |||
| Ac-w-F-F-N-Y-Y-W | Drug Info | IC50 = 14000 nM | |||
| Ac-bhg-F-N-Y-Y-W | Drug Info | IC50 = 4300 nM | |||
| Compound RES-701-1(1-10)/[A15]SRTX6b | Drug Info | IC50 = 3.8 nM | |||
| Compound RES-701-1(1-10)/[A15]ET-3 | Drug Info | IC50 = 2.5 nM | |||
| IRL-1841 | Drug Info | Ki = 36 nM | |||
| References | |||||
| Ref 525859 | J Med Chem. 2000 Aug 10;43(16):3111-7.Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists. | ||||
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