Reaction Details
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Proto-oncogene tyrosine-protein kinase LCK
Ligand
BDBM13228
Substrate
Enolase
Meas. Tech.
Lck Kinase Inhibition Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
24300±n/a nM
Citation
Das, J; Chen, P; Norris, D; Padmanabha, R; Lin, J; Moquin, RV; Shen, Z; Cook, LS; Doweyko, AM; Pitt, S; Pang, S; Shen, DR; Fang, Q; de Fex, HF; McIntyre, KW; Shuster, DJ; Gillooly, KM; Behnia, K; Schieven, GL; Wityak, J; Barrish, JC 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase i J Med Chem 49:6819-32 (2006) [PubMed] Article Target
Name:
Proto-oncogene tyrosine-protein kinase LCK
Synonyms:
LCK_MOUSE | LSK | Lck | Lsk-t | Lymphocyte cell-specific protein-tyrosine kinase | Proto-oncogene tyrosine-protein kinase LCK | Tyrosine-protein kinase LCK | p56-LCK
Type:
PROTEIN
Mol. Mass.:
57927.84
Organism:
Mus musculus
Description:
ChEMBL_806408
Residue:
509
Sequence:
MGCVCSSNPEDDWMENIDVCENCHYPIVPLDSKISLPIRNGSEVRDPLVTYEGSLPPASPLQDNLVIALHSYEPSHDGDLGFEKGEQLRILEQSGEWWKAQSLTTGQEGFIPFNFVAKANSLEPEPWFFKNLSRKDAERQLLAPGNTHGSFLIRESESTAGSFSLSVRDFDQNQGEVVKHYKIRNLDNGGFYISPRITFPGLHDLVRHYTNASDGLCTKLSRPCQTQKPQKPWWEDEWEVPRETLKLVERLGAGQFGEVWMGYYNGHTKVAVKSLKQGSMSPDAFLAEANLMKQLQHPRLVRLYAVVTQEPIYIITEYMENGSLVDFLKTPSGIKLNVNKLLDMAAQIAEGMAFIEEQNYIHRDLRAANILVSDTLSCKIADFGLARLIEDNEYTAREGAKFPIKWTAPEAINYGTFTIKSDVWSFGILLTEIVTHGRIPYPGMTNPEVIQNLERGYRMVRPDNCPEELYHLMMLCWKERPEDRPTFDYLRSVLDDFFTATEGQYQPQP
Inhibitor
Name:
BDBM13228
Synonyms:
2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-(2-methoxy-6-methylphenyl)-1,3-thiazole-5-carboxamide | BMS-354825 tert-Butoxycarbamate Analog 5i | CHEMBL132399 | tert-butyl N-{5-[(2-methoxy-6-methylphenyl)carbamoyl]-4-methyl-1,3-thiazol-2-yl}carbamate
Type:
Small organic molecule
Emp. Form.:
C18H23N3O4S
Mol. Mass.:
377.458
SMILES:
COc1cccc(C)c1NC(=O)c1sc(NC(=O)OC(C)(C)C)nc1C
Structure:
Substrate
Name:
Enolase
Synonyms:
Enolase 1
Type:
Other Protein Type
Mol. Mass.:
46670.83
Organism:
Saccharomyces cerevisiae
Description:
Acid denatured substrate.
Residue:
436
Sequence:
AVSKVYARSVYDSRGNPTVEVELTTEKGVFRSIVPSGASTGVHEALEMRDGDKSKWMGKGVLHAVKNVNDVIAPAFVKANIDVKDQKAVDDFLISLDGTANKSKLGANAILGVSLAASRAAAAEKNVPLYKHLADLSKSKTSPYVLPVPFLNVLNGGSHAGGALALQEFMIAPTGAKTFAEALRIGSEVYHNLKSLTKKRYGASAGNVGDEGGVAPNIQTAEEALDLIVDAIKAAGHDGKVKIGLDCASSEFFKDGKYDLDFKNPNSDKSKWLTGPQLADLYHSLMKRYPIVSIEDPFAEDDWEAWSHFFKTAGIQIVADDLTVTNPKRIATAIEKKAADALLLKVNQIGTLSESIKAAQDSFAAGWGVMVSHRSGETEDTFIADLVVGLRTGQIKTGAPARSERLAKLNQLLRIEEELGDNAVFAGENFHHGDKL