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Target
Tyrosine-protein kinase Lck
Ligand
BDBM13278
Substrate
Enolase
Meas. Tech.
Lck Kinase Inhibition Assay
IC50
0.7±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
More Info.:
Target
Name:
Tyrosine-protein kinase Lck
Synonyms:
2.7.10.2 | LCK | LCK_HUMAN | LSK | Leukocyte C-terminal Src kinase | Lymphocyte cell-specific protein-tyrosine kinase | Lymphocyte-specific protein tyrosine kinase | P56-LCK | Protein YT16 | Proto-oncogene Lck | Proto-oncogene tyrosine-protein kinase LCK | Src/Lck kinase | T cell-specific protein-tyrosine kinase
Type:
n/a
Mol. Mass.:
57987.83
Organism:
Homo sapiens (Human)
Description:
P06239
Residue:
509
Sequence:
MGCGCSSHPEDDWMENIDVCENCHYPIVPLDGKGTLLIRNGSEVRDPLVTYEGSNPPASPLQDNLVIALHSYEPSHDGDLGFEKGEQLRILEQSGEWWKAQSLTTGQEGFIPFNFVAKANSLEPEPWFFKNLSRKDAERQLLAPGNTHGSFLIRESESTAGSFSLSVRDFDQNQGEVVKHYKIRNLDNGGFYISPRITFPGLHELVRHYTNASDGLCTRLSRPCQTQKPQKPWWEDEWEVPRETLKLVERLGAGQFGEVWMGYYNGHTKVAVKSLKQGSMSPDAFLAEANLMKQLQHQRLVRLYAVVTQEPIYIITEYMENGSLVDFLKTPSGIKLTINKLLDMAAQIAEGMAFIEERNYIHRDLRAANILVSDTLSCKIADFGLARLIEDNEYTAREGAKFPIKWTAPEAINYGTFTIKSDVWSFGILLTEIVTHGRIPYPGMTNPEVIQNLERGYRMVRPDNCPEELYQLMRLCWKERPEDRPTFDYLRSVLEDFFTATEGQYQPQP
Inhibitor
Name:
BDBM13278
Synonyms:
BMS-354825 2-Heteroarylamino-thiazole Analog 12w | N-(2-Chloro-6-methylphenyl)-2-(6-(4-(hydroxymethyl)piperidin-1-yl)-2-methylpyrimidin-4-ylamino)-1,3-thiazole-5-carboxamide | N-(2-chloro-6-methylphenyl)-2-({6-[4-(hydroxymethyl)piperidin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
Type:
Small organic molecule
Emp. Form.:
C22H25ClN6O2S
Mol. Mass.:
472.991
SMILES:
Cc1nc(Nc2ncc(s2)C(=O)Nc2c(C)cccc2Cl)cc(n1)N1CCC(CO)CC1
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