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Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM17735
Substrate
biotinylated gastrin substrate
Meas. Tech.
HTRF Kinase Inhibition Assay
IC50
1±n/a nM
Citation
Martin, MW; Newcomb, J; Nunes, JJ; McGowan, DC; Armistead, DM; Boucher, C; Buchanan, JL; Buckner, W; Chai, L; Elbaum, D; Epstein, LF; Faust, T; Flynn, S; Gallant, P; Gore, A; Gu, Y; Hsieh, F; Huang, X; Lee, JH; Metz, D; Middleton, S; Mohn, D; Morgenstern, K; Morrison, MJ; Novak, PM; Oliveira-dos-Santos, A; Powers, D; Rose, P; Schneider, S; Sell, S; Tudor, Y; Turci, SM; Welcher, AA; White, RD; Zack, D; Zhao, H; Zhu, L; Zhu, X; Ghiron, C; Amouzegh, P; Ermann, M; Jenkins, J; Johnston, D; Napier, S; Power, E Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J Med Chem 49:4981-91 (2006) [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:
BDBM17735
Synonyms:
2,6-dimethylphenyl N-(2-{[3,5-dimethoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)-N-(2,4-dimethoxyphenyl)carbamate | 2-aminopyrimidine carbamate, 34
Type:
Small organic molecule
Emp. Form.:
C34H40N6O6
Mol. Mass.:
628.718
SMILES:
COc1ccc(N(C(=O)Oc2c(C)cccc2C)c2ccnc(Nc3cc(OC)c(N4CCN(C)CC4)c(OC)c3)n2)c(OC)c1
Substrate
Name:
biotinylated gastrin substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2100.22
Organism:
n/a
Description:
n/a
Residue:
17
Sequence:
ITINYLEEEEAYGWLDF