Ki Summary

Reaction Details

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Target

Complex of Baculoviral IAP repeat-containing protein 7 [1-159,S150G] and E3 ubiquitin-protein ligase XIAP [336-348]

Ligand

BDBM17346

Substrate/Competitor

BDBM17342

Meas. Tech.

Fluorescence Polarization Affinity Measurements.

7.2±n/a

Temperature

295.15±n/a K

190±n/a nM

Citation

Zobel, K; Wang, L; Varfolomeev, E; Franklin, MC; Elliott, LO; Wallweber, HJ; Okawa, DC; Flygare, JA; Vucic, D; Fairbrother, WJ; Deshayes, K Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs. ACS Chem Biol1:525-33 (2006) [PubMed] Article

More Info.:

Get all data from this article, Solution Info, Assay Method

Complex of Baculoviral IAP repeat-containing protein 7 [1-159,S150G] and E3 ubiquitin-protein ligase XIAP [336-348]

Name:

Complex of Baculoviral IAP repeat-containing protein 7 [1-159,S150G] and E3 ubiquitin-protein ligase XIAP [336-348]

Synonyms:

Chimeric protein of melanoma inhibitor of apoptosis protein and XIAP-BIR3 | ML-IAP-BIR | MLXBIR3SG

Type:

Chimeric Protein

Mol. Mass.:

19011.07

Organism:

Homo sapiens (Human)

Description:

Amino acids 160-179 of MLBIR were replaced with amino acids 336-348 of XIAP-BIR3, and Ser150 of MLBIR was mutated to glycine to give MLXBIR3SG.

Residue:

172

Sequence:

MGPKDSAKCLHRGPQPSHWAAGDGPTQERCGPRSLGSPVLGLDTCRAWDHVDGQILGQLR
PLTEEEEEEGAGATLSRGPAFPGMGSEELRLASFYDWPLTAEVPPELLAAAGFFHTGHQD
KVRCFFCYGGLQSWKRGDDPWTEHAKWFPGCQFLLRSKGQEYINNIHLTHSL

BDBM17346

BDBM17342

Name

BDBM17346

Synonyms:

(3R,6S,9aS)-2,2-dimethyl-N-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-6-[(2S)-2-(methylamino)propanamido]-5-oxo-octahydroazepino[2,1-b][1,3]thiazole-3-carboxamide | peptide isostere, 9

Type

Small organic molecule

Emp. Form.

C25H34N6O3S

Mol. Mass.

498.641

SMILES

[H][C@]12CCC[C@H](NC(=O)[C@H](C)NC)C(=O)N1[C@H](C(=O)Nc1cc(C)nn1-c1ccccc1)C(C)(C)S2 |r|

Structure