Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetProto-oncogene tyrosine-protein kinase Src
LigandBDBM50151366
Substrate/Competitorn/a
Meas. Tech.ChEMBL_305893 (CHEMBL832908)
IC50>4±n/a nM
Citation Chen, PDoweyko, AMNorris, DGu, HHSpergel, SHDas, JMoquin, RVLin, JWityak, JIwanowicz, EJMcIntyre, KWShuster, DJBehnia, KChong, Sde Fex, HPang, SPitt, SShen, DRThrall, SStanley, PKocy, ORWitmer, MRKanner, SBSchieven, GLBarrish, JC Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity. J Med Chem47:4517-29 (2004) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Proto-oncogene tyrosine-protein kinase Src
Name:Proto-oncogene tyrosine-protein kinase Src
Synonyms:Calmodulin/Proto-oncogene tyrosine-protein kinase Src | Protein cereblon/Tyrosine-protein kinase SRC | Proto-oncogene c-Src | Proto-oncogene tyrosine-protein kinase Src (c-Src) | SRC | SRC1 | SRC_HUMAN | Tyrosine-protein kinase Src (SRC) | V-src sarcoma (Schmidt-Ruppin A-2) viral oncogene homolog (avian) | c-Src | p60-Src | pp60c-src
Type:Protein
Mol. Mass.:59838.60
Organism:Homo sapiens (Human)
Description:P12931
Residue:536
Sequence:
MGSNKSKPKDASQRRRSLEPAENVHGAGGGAFPASQTPSKPASADGHRGPSAAFAPAAAE
PKLFGGFNSSDTVTSPQRAGPLAGGVTTFVALYDYESRTETDLSFKKGERLQIVNNTEGD
WWLAHSLSTGQTGYIPSNYVAPSDSIQAEEWYFGKITRRESERLLLNAENPRGTFLVRES
ETTKGAYCLSVSDFDNAKGLNVKHYKIRKLDSGGFYITSRTQFNSLQQLVAYYSKHADGL
CHRLTTVCPTSKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTL
KPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGSLLDFLKGETGKY
LRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYT
ARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVER
GYRMPCPPECPESLHDLMCQCWRKEPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50151366
n/a
NameBDBM50151366
Synonyms:(2-Chloro-6-methyl-phenyl)-[8-((S)-3-methyl-piperazin-1-yl)-2,5,9,9b-tetraaza-cyclopenta[a]naphthalen-4-yl]-amine | BMS-279700 | CHEMBL189338
TypeSmall organic molecule
Emp. Form.C21H22ClN7
Mol. Mass.407.899
SMILESC[C@H]1CN(CCN1)c1ccc2nc(Nc3c(C)cccc3Cl)c3cncn3c2n1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: