Reaction Details Report a problem with these data
Target
Cellular tumor antigen p53
Ligand
BDBM50299819
Substrate
n/a
Meas. Tech.
ChEMBL_589609 (CHEMBL1052162)
IC50
44300±n/a nM
Citation
Allen, JG; Bourbeau, MP; Wohlhieter, GE; Bartberger, MD; Michelsen, K; Hungate, R; Gadwood, RC; Gaston, RD; Evans, B; Mann, LW; Matison, ME; Schneider, S; Huang, X; Yu, D; Andrews, PS; Reichelt, A; Long, AM; Yakowec, P; Yang, EY; Lee, TA; Oliner, JD Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction. J Med Chem 52:7044-53 (2009) [PubMed] Article
More Info.:
Target
Name:
Cellular tumor antigen p53
Synonyms:
Antigen NY-CO-13 | CREB-binding protein/p53 | GST-p53 | His6-p53 | P53 | P53_HUMAN | Phosphoprotein p53 | TP53 | Tumor Suppressor p53
Type:
fusion protein
Mol. Mass.:
43654.73
Organism:
Homo sapiens (Human)
Description:
The full-length His6-wt-p53 expressed in E. coli was used in assays.
Residue:
393
Sequence:
MEEPQSDPSVEPPLSQETFSDLWKLLPENNVLSPLPSQAMDDLMLSPDDIEQWFTEDPGPDEAPRMPEAAPPVAPAPAAPTPAAPAPAPSWPLSSSVPSQKTYQGSYGFRLGFLHSGTAKSVTCTYSPALNKMFCQLAKTCPVQLWVDSTPPPGTRVRAMAIYKQSQHMTEVVRRCPHHERCSDSDGLAPPQHLIRVEGNLRVEYLDDRNTFRHSVVVPYEPPEVGSDCTTIHYNYMCNSSCMGGMNRRPILTIITLEDSSGNLLGRNSFEVRVCACPGRDRRTEEENLRKKGEPHHELPPGSTKRALPNNTSSSPQPKKKPLDGEYFTLQIRGRERFEMFRELNEALELKDAQAGKEPGGSRAHSSHLKSKKGQSTSRHKKLMFKTEGPDSD
Inhibitor
Name:
BDBM50299819
Synonyms:
(+/-)-syn-6,7-Bis(4-bromophenyl)-2-fluoro-12-methyl-7,12-dihydro-6H-chromeno[4,3-d][1,2,4]triazolo[1,5-a]pyrimidine | CHEMBL567403
Type:
Small organic molecule
Emp. Form.:
C25H17Br2FN4O
Mol. Mass.:
568.235
SMILES:
CN1c2ncnn2C(C2=C1c1cc(F)ccc1OC2c1ccc(Br)cc1)c1ccc(Br)cc1 |c:9|