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Target
Ribosomal protein S6 kinase alpha-1
Ligand
BDBM2579
Substrate
n/a
Meas. Tech.
ChEMBL_498323 (CHEMBL973461)
IC50
<0.100000±n/a nM
Citation
 Hall, MD; Salam, NK; Hellawell, JL; Fales, HM; Kensler, CB; Ludwig, JA; Szakács, G; Hibbs, DE; Gottesman, MM Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. J Med Chem 52:3191-204 (2009) [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:
BDBM2579
Synonyms:
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US20240002365, Compound staurosporine | US9206188, Staurosporine | US9226923, Staurosporine
Type:
Small organic molecule
Emp. Form.:
C28H26N4O3
Mol. Mass.:
466.531
SMILES:
CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Structure:
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