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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