Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM50198819
Substrate
n/a
Meas. Tech.
ChEMBL_437736 (CHEMBL905921)
IC50
10±n/a nM
Citation
 Noronha, GBarrett, KBoccia, ABrodhag, TCao, JChow, CPDneprovskaia, EDoukas, JFine, RGong, XGritzen, CGu, HHanna, EHood, JDHu, SKang, XKey, JKlebansky, BKousba, ALi, GLohse, DMak, CCMcPherson, APalanki, MSPathak, VPRenick, JShi, FSoll, RSplittgerber, UStoughton, STang, SYee, SZeng, BZhao, NZhu, H Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. Bioorg Med Chem Lett 17:602-8 (2007) [PubMed]  Article 
Target
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:
MGSNKSKPKDASQRRRSLEPAENVHGAGGGAFPASQTPSKPASADGHRGPSAAFAPAAAEPKLFGGFNSSDTVTSPQRAGPLAGGVTTFVALYDYESRTETDLSFKKGERLQIVNNTEGDWWLAHSLSTGQTGYIPSNYVAPSDSIQAEEWYFGKITRRESERLLLNAENPRGTFLVRESETTKGAYCLSVSDFDNAKGLNVKHYKIRKLDSGGFYITSRTQFNSLQQLVAYYSKHADGLCHRLTTVCPTSKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGSLLDFLKGETGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKEPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
  
Inhibitor
Name:
BDBM50198819
Synonyms:
4-(6-methyl-7-o-tolylbenzo[e][1,2,4]triazin-3-ylamino)-N-(2-(pyrrolidin-1-yl)ethyl)benzenesulfonamide | CHEMBL231237 | US8481536, 431 | US8481536, 591
Type:
Small organic molecule
Emp. Form.:
C27H30N6O2S
Mol. Mass.:
502.631
SMILES:
Cc1ccccc1-c1cc2nnc(Nc3ccc(cc3)S(=O)(=O)NCCN3CCCC3)nc2cc1C
Structure:
Search PDB for entries with ligand similarity: