Target
Ribosomal protein S6 kinase alpha-1
Ligand
BDBM4779
Substrate
n/a
Meas. Tech.
ChEMBL_586995 (CHEMBL1062785)
Kd
6200±n/a nM
Citation
 Karaman, MWHerrgard, STreiber, DKGallant, PAtteridge, CECampbell, BTChan, KWCiceri, PDavis, MIEdeen, PTFaraoni, RFloyd, MHunt, JPLockhart, DJMilanov, ZVMorrison, MJPallares, GPatel, HKPritchard, SWodicka, LMZarrinkar, PP A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol 26:127-32 (2008) [PubMed]  Article 
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:
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:
Search PDB for entries with ligand similarity: