Reaction Details
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E3 ubiquitin-protein ligase XIAP [241-356]
Ligand
BDBM27919
Substrate
BDBM17342
Meas. Tech.
Fluorescence Polarization Affinity Measurements
Ki
140±n/a nM
Citation
Cohen, F; Alicke, B; Elliott, LO; Flygare, JA; Goncharov, T; Keteltas, SF; Franklin, MC; Frankovitz, S; Stephan, JP; Tsui, V; Vucic, D; Wong, H; Fairbrother, WJ Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold. J Med Chem 52:1723-30 (2009) [PubMed] Article More Info.:
Target
Name:
E3 ubiquitin-protein ligase XIAP [241-356]
Synonyms:
baculovirus IAP repeat 3 (BIR3) domain of XIAP | X-linked inhibitor of apoptosis protein BIR3 domain (XIAP BIR-3) | XIAP_HUMAN | XIAP | API3 | BIRC4 | IAP3 | XIAP-BIR3 | E3 ubiquitin-protein ligase XIAP BIR-3 | X chromosome-linked inhibitor of apoptosis BIR3 domain (XIAP BIR3) | BIR3 domain of X-linked inhibitor of apoptosis protein | E3 ubiquitin-protein ligase XIAP BIR3 | E3 ubiquitin-protein ligase (XIAP-BIR3)
Type:
Protein Binding Domain
Mol. Mass.:
13276.62
Organism:
Human
Description:
BIR3 of XIAP: RESIDUES 241-356.
Residue:
116
Sequence:
SDAVSSDRNFPNSTNLPRNPSMADYEARIFTFGTWIYSVNKEQLARAGFYALGEGDKVKCFHCGGGLTDWKPSEDPWEQHAKWYPGCKYLLEQKGQEYINNIHLTHSLEECLVRTT
Inhibitor
Name:
BDBM27919
Synonyms:
N-[(3aR,6S,6aS)-1-[(2S)-3,3-dimethyl-2-[(2S)-2-(methylamino)propanamido]butanoyl]-octahydrocyclopenta[b]pyrrol-6-yl]naphthalene-1-carboxamide | Azabicyclooctane scaffold, 14b
Type:
Small organic molecule
Emp. Form.:
C28H38N4O3
Mol. Mass.:
478.29
SMILES:
C[C@@H](C(=O)N[C@H](C(=O)N1CC[C@@H]2[C@H]1[C@H](CC2)NC(=O)c3cccc4c3cccc4)C(C)(C)C)NC

