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Target
Ribosomal protein S6 kinase alpha-3
Ligand
BDBM286078
Substrate
n/a
Meas. Tech.
Radioisotope assay
IC50
>10000±n/a nM
Citation
 Dunn, SE; Jayanthan, A; Nagireddy, JR; Annedi, S; Van Drie, JH; Daynard, TS; Huynh, M Substituted tetrahydropyrido[3′,2′:4,5]pyrrolo[1,2-α]pyrazine-2-carboxamides as RSK inhibitors US Patent  US10081632 Publication Date 9/25/2018 
Target
Name:
Ribosomal protein S6 kinase alpha-3
Synonyms:
90 kDa ribosomal protein S6 kinase 3 | ISPK-1 | ISPK1 | KS6A3_HUMAN | MAP kinase-activated protein kinase 1b | MAPKAPK1B | RPS6KA3 | RPS6KA3(Kin.Dom.1 - N-terminal) | RSK2 | Ribosomal S6 kinase 2 (RSK2) | Ribosomal protein S6 kinase | Ribosomal protein S6 kinase alpha-1/alpha-3 | Ribosomal protein S6 kinase alpha-3 (RSK2) | Ribosomal protein S6 kinase alpha-3 (RSK3) | S6K-alpha 3 | insulin-stimulated protein kinase 1 | p90 ribosomal s6 kinase (RSK2) | p90-RSK 3 | p90RSK | pp90RSK2
Type:
Serine/threonine-protein kinase
Mol. Mass.:
83740.03
Organism:
Homo sapiens (Human)
Description:
The human RSK2 sequence differed from the Genbank entry NM_004586 at one residue, V45G. The protein was cloned and purified from baculovirus expression system.
Residue:
740
Sequence:
MPLAQLADPWQKMAVESPSDSAENGQQIMDEPMGEEEINPQTEEVSIKEIAITHHVKEGHEKADPSQFELLKVLGQGSFGKVFLVKKISGSDARQLYAMKVLKKATLKVRDRVRTKMERDILVEVNHPFIVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALALDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKESIDHEKKAYSFCGTVEYMAPEVVNRRGHTQSADWWSFGVLMFEMLTGTLPFQGKDRKETMTMILKAKLGMPQFLSPEAQSLLRMLFKRNPANRLGAGPDGVEEIKRHSFFSTIDWNKLYRREIHPPFKPATGRPEDTFYFDPEFTAKTPKDSPGIPPSANAHQLFRGFSFVAITSDDESQAMQTVGVHSIVQQLHRNSIQFTDGYEVKEDIGVGSYSVCKRCIHKATNMEFAVKIIDKSKRDPTEEIEILLRYGQHPNIITLKDVYDDGKYVYVVTELMKGGELLDKILRQKFFSEREASAVLFTITKTVEYLHAQGVVHRDLKPSNILYVDESGNPESIRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDAACDIWSLGVLLYTMLTGYTPFANGPDDTPEEILARIGSGKFSLSGGYWNSVSDTAKDLVSKMLHVDPHQRLTAALVLRHPWIVHWDQLPQYQLNRQDAPHLVKGAMAATYSALNRNQSPVLEPVGRSTLAQRRGIKKITSTAL
  
Inhibitor
Name:
BDBM286078
Synonyms:
1-Benzyl-N-(3-(morpholinomethyl)benzo[b]thiophen-5-yl)-1H-pyrazole-4-carboxamide | US10081632, Compound 5 | US10758530, Compound 5 | US9771366, Compound 5
Type:
Small organic molecule
Emp. Form.:
C24H24N4O2S
Mol. Mass.:
432.538
SMILES:
O=C(Nc1ccc2scc(CN3CCOCC3)c2c1)c1cnn(Cc2ccccc2)c1
Structure:
Search PDB for entries with ligand similarity: