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Target
von Hippel-Lindau disease tumor suppressor
Ligand
BDBM552715
Substrate
n/a
Meas. Tech.
VHL HEK-293 BRET Assay
IC50
5400±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:
BDBM552715
Synonyms:
(2S,4R)-N-((R)-3-([l,l'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)-4-hydroxy-l-((S)-3-methyl-2-(5-methyl-lH-l,2,3-triazol-l-yl)butanoyl)pyrrolidine-2-carboxamide (Compound 33) | WO2022103411, Compound 33 | WO2022103411, Example S32
Type:
Small organic molecule
Emp. Form.:
C28H34N6O4
Mol. Mass.:
518.6074
SMILES:
CC(C)[C@@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@H](Cc1ccc(cc1)-c1ccccc1)C(N)=O)n1nncc1C |r|
Structure:
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