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Target
von Hippel-Lindau disease tumor suppressor
Ligand
BDBM552687
Substrate
n/a
Meas. Tech.
VHL HEK-293 BRET Assay
IC50
20±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:
BDBM552687
Synonyms:
(2S,4R)-l-((S)-2-(4-benzyl-lH-l,2,3-triazol-l-yl)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (Compound 27) | WO2022103411, Example S27
Type:
Small organic molecule
Emp. Form.:
C31H36N6O3S
Mol. Mass.:
572.721
SMILES:
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](n2cc(Cc3ccccc3)nn2)C(C)(C)C)cc1 |r|
Structure:
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