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Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM12228
Substrate
poly(E,Y)
Meas. Tech.
In Vitro Src Kinase Inhibition Test
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
10±n/a nM
Citation
Hennequin, LF; Allen, J; Breed, J; Curwen, J; Fennell, M; Green, TP; Lambert-van der Brempt, C; Morgentin, R; Norman, RA; Olivier, A; Otterbein, L; Ple, PA; Warin, N; Costello, G N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. J Med Chem 49:6465-88 (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:
BDBM12228
Synonyms:
AZD0530 analogue 6 | N-(5-chloro-2H-1,3-benzodioxol-4-yl)-7-methoxy-5-[(1-methylpiperidin-4-yl)oxy]quinazolin-4-amine
Type:
Small organic molecule
Emp. Form.:
C22H23ClN4O4
Mol. Mass.:
442.895
SMILES:
COc1cc(OC2CCN(C)CC2)c2c(Nc3c4OCOc4ccc3Cl)ncnc2c1
Substrate
Name:
poly(E,Y)
Synonyms:
n/a
Type:
Random Copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
A poly(Glu,Tyr) 4:1 random copolymer.
10 uM ATP was used as co-substrate
Residue:
3
Sequence:
NA