Reaction Details |
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Target | Cyclin-dependent kinase 8 |
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Ligand | BDBM13534 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_587069 (CHEMBL1051283) |
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Kd | >10000±n/a nM |
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Citation | Karaman, MW; Herrgard, S; Treiber, DK; Gallant, P; Atteridge, CE; Campbell, BT; Chan, KW; Ciceri, P; Davis, MI; Edeen, PT; Faraoni, R; Floyd, M; Hunt, JP; Lockhart, DJ; Milanov, ZV; Morrison, MJ; Pallares, G; Patel, HK; Pritchard, S; Wodicka, LM; Zarrinkar, PP A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol26:127-32 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Cyclin-dependent kinase 8 |
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Name: | Cyclin-dependent kinase 8 |
Synonyms: | CDK8 | CDK8_HUMAN | Cell division protein kinase 8 | Cyclin-Dependent Kinase 8 (CDK8) | Mediator complex subunit CDK8 | Mediator of RNA polymerase II transcription subunit CDK8 | Protein kinase K35 |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 53300.21 |
Organism: | Homo sapiens (Human) |
Description: | P49336 |
Residue: | 464 |
Sequence: | MDYDFKVKLSSERERVEDLFEYEGCKVGRGTYGHVYKAKRKDGKDDKDYALKQIEGTGIS
MSACREIALLRELKHPNVISLQKVFLSHADRKVWLLFDYAEHDLWHIIKFHRASKANKKP
VQLPRGMVKSLLYQILDGIHYLHANWVLHRDLKPANILVMGEGPERGRVKIADMGFARLF
NSPLKPLADLDPVVVTFWYRAPELLLGARHYTKAIDIWAIGCIFAELLTSEPIFHCRQED
IKTSNPYHHDQLDRIFNVMGFPADKDWEDIKKMPEHSTLMKDFRRNTYTNCSLIKYMEKH
KVKPDSKAFHLLQKLLTMDPIKRITSEQAMQDPYFLEDPLPTSDVFAGCQIPYPKREFLT
EEEPDDKGDKKNQQQQQGNNHTNGTGHPGNQDSSHTQGPPLKKVRVVPPTTTSGGLIMTS
DYQRSNPHAAYPNPGPSTSQPQSSMGYSATSQQPPQYSHQTHRY
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BDBM13534 |
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n/a |
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Name | BDBM13534 |
Synonyms: | CHEMBL572878 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | N-[4-[[4-(4-methylpiperazino)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]thio]phenyl]cyclopropanecarboxamide | VX-680 | VX680 | cyclopropane carboxylic acid {4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino)-pyrimidin-2ylsulphanyl]-phenyl}-amide |
Type | Small organic molecule |
Emp. Form. | C23H28N8OS |
Mol. Mass. | 464.586 |
SMILES | CN1CCN(CC1)c1cc(Nc2cc(C)n[nH]2)nc(Sc2ccc(NC(=O)C3CC3)cc2)n1 |
Structure |
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