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Target
E3 ubiquitin-protein ligase XIAP [241-356]
Ligand
BDBM27940
Substrate
BDBM17342
Meas. Tech.
Fluorescence Polarization Affinity Measurements
Ki
3000±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 
Target
Name:
E3 ubiquitin-protein ligase XIAP [241-356]
Synonyms:
API3 | BIR3 domain of X-linked inhibitor of apoptosis protein | BIRC4 | E3 ubiquitin-protein ligase (XIAP-BIR3) | E3 ubiquitin-protein ligase XIAP BIR-3 | E3 ubiquitin-protein ligase XIAP BIR3 | IAP3 | X chromosome-linked inhibitor of apoptosis BIR3 domain (XIAP BIR3) | X-linked inhibitor of apoptosis protein BIR3 domain (XIAP BIR-3) | XIAP | XIAP-BIR3 | XIAP_HUMAN | baculovirus IAP repeat 3 (BIR3) domain of XIAP
Type:
Protein Binding Domain
Mol. Mass.:
13276.62
Organism:
Homo sapiens (Human)
Description:
BIR3 of XIAP: RESIDUES 241-356.
Residue:
116
Sequence:
SDAVSSDRNFPNSTNLPRNPSMADYEARIFTFGTWIYSVNKEQLARAGFYALGEGDKVKCFHCGGGLTDWKPSEDPWEQHAKWYPGCKYLLEQKGQEYINNIHLTHSLEECLVRTT
  
Inhibitor
Name:
BDBM27940
Synonyms:
(2S)-N-[(2S)-1-[(2S)-2-[(1,1-diphenylacetamido)methyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]-2-(methylamino)propanamide | butoxycarbonylpyrrolidine derivative, 15a
Type:
Small organic molecule
Emp. Form.:
C29H40N4O3
Mol. Mass.:
492.6529
SMILES:
CN[C@@H](C)C(=O)N[C@H](C(=O)N1CCC[C@H]1CNC(=O)C(c1ccccc1)c1ccccc1)C(C)(C)C |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM17342
Synonyms:
5-carboxyflourescein(5-FAM)-conjugated AVPFFAKK | AVP-diPhe-FAM
Type:
Fluorescent dye-conjugated peptide
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
n/a
Structure: