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TargetTyrosine-protein kinase Lck
LigandBDBM13273
Substrate/CompetitorEnolase
Meas. Tech.Lck Kinase Inhibition Assay
IC50<0.5±n/a nM
Citation Das, JChen, PNorris, DPadmanabha, RLin, JMoquin, RVShen, ZCook, LSDoweyko, AMPitt, SPang, SShen, DRFang, Qde Fex, HFMcIntyre, KWShuster, DJGillooly, KMBehnia, KSchieven, GLWityak, JBarrish, 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 Chem49:6819-32 (2006) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Tyrosine-protein kinase Lck
Name:Tyrosine-protein kinase Lck
Synonyms:2.7.10.2 | LCK | 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 | T cell-specific protein-tyrosine kinase
Type:n/a
Mol. Mass.:57987.83
Organism:Homo sapiens (Human)
Description:n/a
Residue:509
Sequence:
MGCGCSSHPEDDWMENIDVCENCHYPIVPLDGKGTLLIRNGSEVRDPLVTYEGSNPPASP
LQDNLVIALHSYEPSHDGDLGFEKGEQLRILEQSGEWWKAQSLTTGQEGFIPFNFVAKAN
SLEPEPWFFKNLSRKDAERQLLAPGNTHGSFLIRESESTAGSFSLSVRDFDQNQGEVVKH
YKIRNLDNGGFYISPRITFPGLHELVRHYTNASDGLCTRLSRPCQTQKPQKPWWEDEWEV
PRETLKLVERLGAGQFGEVWMGYYNGHTKVAVKSLKQGSMSPDAFLAEANLMKQLQHQRL
VRLYAVVTQEPIYIITEYMENGSLVDFLKTPSGIKLTINKLLDMAAQIAEGMAFIEERNY
IHRDLRAANILVSDTLSCKIADFGLARLIEDNEYTAREGAKFPIKWTAPEAINYGTFTIK
SDVWSFGILLTEIVTHGRIPYPGMTNPEVIQNLERGYRMVRPDNCPEELYQLMRLCWKER
PEDRPTFDYLRSVLEDFFTATEGQYQPQP
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BDBM13273
NameBDBM13273
Synonyms:2-(6-(3-(1H-Imidazol-1-yl)propylamino)pyridin-2-ylamino)-N-(2-chloro-6-methylphenyl)-1,3-thiazole-5-carboxamide | BMS-354825 2-Heteroarylamino-thiazole Analog 12r | N-(2-chloro-6-methylphenyl)-2-[(6-{[3-(1H-imidazol-1-yl)propyl]amino}pyridin-2-yl)amino]-1,3-thiazole-5-carboxamide
TypeSmall organic molecule
Emp. Form.C22H22ClN7OS
Mol. Mass.467.974
SMILESCc1cccc(Cl)c1NC(=O)c1cnc(Nc2cccc(NCCCn3ccnc3)n2)s1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
Enolase
Name:Enolase
Synonyms:Enolase 1
Type:Other Protein Type
Mol. Mass.:46670.83
Organism:Saccharomyces cerevisiae
Description:Acid denatured substrate.
Residue:436
Sequence:
AVSKVYARSVYDSRGNPTVEVELTTEKGVFRSIVPSGASTGVHEALEMRDGDKSKWMGKG
VLHAVKNVNDVIAPAFVKANIDVKDQKAVDDFLISLDGTANKSKLGANAILGVSLAASRA
AAAEKNVPLYKHLADLSKSKTSPYVLPVPFLNVLNGGSHAGGALALQEFMIAPTGAKTFA
EALRIGSEVYHNLKSLTKKRYGASAGNVGDEGGVAPNIQTAEEALDLIVDAIKAAGHDGK
VKIGLDCASSEFFKDGKYDLDFKNPNSDKSKWLTGPQLADLYHSLMKRYPIVSIEDPFAE
DDWEAWSHFFKTAGIQIVADDLTVTNPKRIATAIEKKAADALLLKVNQIGTLSESIKAAQ
DSFAAGWGVMVSHRSGETEDTFIADLVVGLRTGQIKTGAPARSERLAKLNQLLRIEEELG
DNAVFAGENFHHGDKL
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