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Target
von Hippel-Lindau disease tumor suppressor
Ligand
BDBM552725
Substrate
n/a
Meas. Tech.
VHL HEK-293 BRET Assay
IC50
80±n/a nM
Citation
 Jakob, F; Hao, W; J., FW 1-(2-(4-CYCLOPROPYL-1H-1,2,3-TRIAZOL-1-YL)ACETYL)-4-HYDROXY-N-(BENZYL)PYRROLIDIN E-2-CARBOXAMIDE DERIVATIVES AS VHL INHIBITORS FOR THE TREATMENT OF ANEMIA AND CANCER WIPO 0:0 (2022) [PubMed] 
Target
Name:
von Hippel-Lindau disease tumor suppressor
Synonyms:
Protein G7 | VHL | VHL_HUMAN | Von Hippel-Lindau disease tumor suppressor | Von Hippel-Lindau disease tumor suppressor protein (VBC) | pVHL
Type:
Protein
Mol. Mass.:
24136.87
Organism:
Homo sapiens (Human)
Description:
P40337
Residue:
213
Sequence:
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
  
Inhibitor
Name:
BDBM552725
Synonyms:
(2S, 4R)-l-((S)-2-(4-cyclopropyl-lH-l,2,3-triazol-l-yl)-3,3-dimethylbutanoyl)-4-hydroxy-N-((R)-2,2,2-trifluoro-l-(4-(4-methylthiaz,ol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide ( Compound 46) | WO2022103411, Compound 46 | WO2022103411, Example S40
Type:
Small organic molecule
Emp. Form.:
C28H33F3N6O3S
Mol. Mass.:
590.66
SMILES:
Cc1ncsc1-c1ccc(cc1)[C@@H](NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](n1cc(nn1)C1CC1)C(C)(C)C)C(F)(F)F |r|
Structure:
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