Target
Ribosomal protein S6 kinase alpha-3
Ligand
BDBM13533
Substrate
n/a
Meas. Tech.
ChEMBL_774440 (CHEMBL1908657)
Kd
>10000±n/a nM
Citation
 Davis, MIHunt, JPHerrgard, SCiceri, PWodicka, LMPallares, GHocker, MTreiber, DKZarrinkar, PP Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol 29:1046-51 (2011) [PubMed]  Article 
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:
BDBM13533
Synonyms:
1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | 1-[5-tert-butyl-2-(4-methylphenyl)-3-pyrazolyl]-3-[4-[2-(4-morpholinyl)ethoxy]-1-naphthalenyl]urea | 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | 1-[5-tert-butyl-2-(p-tolyl)pyrazol-3-yl]-3-[4-(2-morpholinoethoxy)-1-naphthyl]urea | 3-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-1-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | 3-[3-tert-butyl-1-(4-methylphenyl)-1H-pyrazol-5-yl]-1-{4-[2-(morpholin-4-yl)ethoxy]naphthalen-1-yl}urea | BIRB 796 | BIRB-796 | BIRB-796, 3 | CHEMBL103667 | D3RKN_73 | Doramapimod | US11407771, Compound 43 | US8933228, BIRB 796 | US9187470, 43 (BIRB-796) | US9242960, BIRB 796 | US9260410, BIRB796 | cid_156422 | diaryl urea compound 10
Type:
Small organic molecule
Emp. Form.:
C31H37N5O3
Mol. Mass.:
527.6572
SMILES:
Cc1ccc(cc1)-n1nc(cc1NC(=O)Nc1ccc(OCCN2CCOCC2)c2ccccc12)C(C)(C)C
Structure:
Search PDB for entries with ligand similarity: