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Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM50198811
Substrate
n/a
Meas. Tech.
ChEMBL_437736 (CHEMBL905921)
IC50
11±n/a nM
Citation
Noronha, G; Barrett, K; Boccia, A; Brodhag, T; Cao, J; Chow, CP; Dneprovskaia, E; Doukas, J; Fine, R; Gong, X; Gritzen, C; Gu, H; Hanna, E; Hood, JD; Hu, S; Kang, X; Key, J; Klebansky, B; Kousba, A; Li, G; Lohse, D; Mak, CC; McPherson, A; Palanki, MS; Pathak, VP; Renick, J; Shi, F; Soll, R; Splittgerber, U; Stoughton, S; Tang, S; Yee, S; Zeng, B; Zhao, N; Zhu, 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
More Info.:
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:
BDBM50198811
Synonyms:
4-(7-(2,6-dimethylphenyl)-6-methylbenzo[e][1,2,4]triazin-3-ylamino)-N-(2-(pyrrolidin-1-yl)ethyl)benzenesulfonamide | CHEMBL230816 | US8481536, 429 | US8481536, 590
Type:
Small organic molecule
Emp. Form.:
C28H32N6O2S
Mol. Mass.:
516.658
SMILES:
Cc1cccc(C)c1-c1cc2nnc(Nc3ccc(cc3)S(=O)(=O)NCCN3CCCC3)nc2cc1C |(-5.05,5.05,;-6.38,4.28,;-7.71,5.05,;-9.05,4.28,;-9.04,2.74,;-7.71,1.97,;-7.71,.43,;-6.38,2.75,;-5.05,1.97,;-3.72,2.74,;-2.39,1.98,;-1.05,2.77,;.3,1.99,;.31,.43,;1.65,-.33,;2.98,.44,;4.31,-.33,;5.64,.44,;5.63,1.99,;4.29,2.75,;2.96,1.97,;6.96,2.76,;6.19,4.09,;7.73,1.43,;8.3,3.53,;9.63,2.75,;10.97,3.52,;12.3,2.75,;12.46,1.23,;13.97,.91,;14.74,2.24,;13.71,3.39,;-1.03,-.34,;-2.38,.43,;-3.72,-.34,;-5.05,.43,;-6.38,-.34,)|