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Target
von Hippel-Lindau disease tumor suppressor
Ligand
BDBM552683
Substrate
n/a
Meas. Tech.
VHL HEK-293 BRET Assay
IC50
220±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:
BDBM552683
Synonyms:
(2S,4R)-N-((R)-3-([1,1'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)-l-((S)-2-(4-cyclopropyl-lH-l,2,3-triazol-l-yl)-3-methylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide ( Compound 1 ) | WO2022103411, Example S1
Type:
Small organic molecule
Emp. Form.:
C30H36N6O4
Mol. Mass.:
544.6446
SMILES:
CC(C)[C@@H](C(=O)N1C[C@H](O)CC1C(=O)N[C@H](Cc1ccc(cc1)-c1ccccc1)C(N)=O)n1cc(nn1)C1CC1 |r|
Structure:
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