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Target
Ribosomal protein S6 kinase alpha-1
Ligand
BDBM13534
Substrate
n/a
Meas. Tech.
ChEMBL_586995 (CHEMBL1062785)
Kd
>10000±n/a nM
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 Biotechnol 26:127-32 (2008) [PubMed] Article
More Info.:
Target
Name:
Ribosomal protein S6 kinase alpha-1
Synonyms:
90 kDa ribosomal protein S6 kinase 1 | KS6A1_HUMAN | MAP kinase-activated protein kinase 1a | MAPKAPK1A | RPS6KA1 | RPS6KA1(Kin.Dom.1 - N-terminal) | RPS6KA1(Kin.Dom.2 - C-terminal) | RSK-1 | RSK1 | Ribosomal S6 Kinase 1 (RSK-1) | Ribosomal S6 kinase 1 | Ribosomal S6 kinase 1 (RSK1) | Ribosomal protein S6 kinase alpha 1 | Ribosomal protein S6 kinase alpha-1 | Ribosomal protein S6 kinase alpha-1 (RSK1) | S6K-alpha 1 | p90-RSK 1 | p90RSK | p90S6K | pp90RSK1
Type:
Serine/threonine-protein kinase
Mol. Mass.:
82736.10
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
735
Sequence:
MPLAQLKEPWPLMELVPLDPENGQTSGEEAGLQPSKDEGVLKEISITHHVKAGSEKADPSHFELLKVLGQGSFGKVFLVRKVTRPDSGHLYAMKVLKKATLKVRDRVRTKMERDILADVNHPFVVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALGLDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKEAIDHEKKAYSFCGTVEYMAPEVVNRQGHSHSADWWSYGVLMFEMLTGSLPFQGKDRKETMTLILKAKLGMPQFLSTEAQSLLRALFKRNPANRLGSGPDGAEEIKRHVFYSTIDWNKLYRREIKPPFKPAVAQPDDTFYFDTEFTSRTPKDSPGIPPSAGAHQLFRGFSFVATGLMEDDGKPRAPQAPLHSVVQQLHGKNLVFSDGYVVKETIGVGSYSECKRCVHKATNMEYAVKVIDKSKRDPSEEIEILLRYGQHPNIITLKDVYDDGKHVYLVTELMRGGELLDKILRQKFFSEREASFVLHTIGKTVEYLHSQGVVHRDLKPSNILYVDESGNPECLRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDEGCDIWSLGILLYTMLAGYTPFANGPSDTPEEILTRIGSGKFTLSGGNWNTVSETAKDLVSKMLHVDPHQRLTAKQVLQHPWVTQKDKLPQSQLSHQDLQLVKGAMAATYSALNSSKPTPQLKPIESSILAQRRVRKLPSTTL
Inhibitor
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