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Target
Ribosomal protein S6 kinase alpha-2
Ligand
BDBM4779
Substrate
n/a
Meas. Tech.
ChEMBL_586996 (CHEMBL1062786)
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
Target
Name:
Ribosomal protein S6 kinase alpha-2
Synonyms:
90 kDa ribosomal protein S6 kinase 2 | 90 kDa ribosomal protein S6 kinase 2 (RSK2) | KS6A2_HUMAN | MAP kinase-activated protein kinase 1c | MAPKAPK1C | RPS6KA2 | RPS6KA2(Kin.Dom.1 - N-terminal) | RSK3 | Ribosomal S6 Kinase 3 (RSK-3) | Ribosomal protein S6 kinase alpha 2 | Ribosomal protein S6 kinase alpha 2 (RSK2) | Ribosomal protein S6 kinase alpha-2 | p90-RSK 2 | p90RSK | pp90RSK3
Type:
Serine/threonine-protein kinase
Mol. Mass.:
83259.46
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
733
Sequence:
MDLSMKKFAVRRFFSVYLRRKSRSKSSSLSRLEEEGVVKEIDISHHVKEGFEKADPSQFELLKVLGQGSYGKVFLVRKVKGSDAGQLYAMKVLKKATLKVRDRVRSKMERDILAEVNHPFIVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALALDHLHSLGIIYRDLKPENILLDEEGHIKITDFGLSKEAIDHDKRAYSFCGTIEYMAPEVVNRRGHTQSADWWSFGVLMFEMLTGSLPFQGKDRKETMALILKAKLGMPQFLSGEAQSLLRALFKRNPCNRLGAGIDGVEEIKRHPFFVTIDWNTLYRKEIKPPFKPAVGRPEDTFHFDPEFTARTPTDSPGVPPSANAHHLFRGFSFVASSLIQEPSQQDLHKVPVHPIVQQLHGNNIHFTDGYEIKEDIGVGSYSVCKRCVHKATDTEYAVKIIDKSKRDPSEEIEILLRYGQHPNIITLKDVYDDGKFVYLVMELMRGGELLDRILRQRYFSEREASDVLCTITKTMDYLHSQGVVHRDLKPSNILYRDESGSPESIRVCDFGFAKQLRAGNGLLMTPCYTANFVAPEVLKRQGYDAACDIWSLGILLYTMLAGFTPFANGPDDTPEEILARIGSGKYALSGGNWDSISDAAKDVVSKMLHVDPHQRLTAMQVLKHPWVVNREYLSPNQLSRQDVHLVKGAMAATYFALNRTPQAPRLEPVLSSNLAQRRGMKRLTSTRL
  
Inhibitor
Name:
BDBM4779
Synonyms:
CHEMBL31965 | CHEMBL545315 | CI-1033 | Canertinib | N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide | PD0183805 | US10507209, Compound CI-1033 | US9730934, CI-1033 | cid_156414
Type:
Small organic molecule
Emp. Form.:
C24H25ClFN5O3
Mol. Mass.:
485.938
SMILES:
Fc1ccc(Nc2ncnc3cc(OCCCN4CCOCC4)c(NC(=O)C=C)cc23)cc1Cl
Structure:
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