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