Reaction Details Report a problem with these data
Target
Ribosomal protein S6 kinase alpha-3 [399-740]
Ligand
BDBM259865
Substrate
n/a
Meas. Tech.
RSK2 Inhibition Assay
pH
8±n/a
Temperature
295.15±n/a K
IC50
>500±n/a nM
Comments
extracted
Citation
 Taunton, Jr., JW; Maglathlin, R; Serafimova, I; Cohen, MS; Miller, R; Paavilainen, V; McFarland, J; Krishnan, S Kinase inhibitors US Patent  US9505766 Publication Date 11/29/2016 
Target
Name:
Ribosomal protein S6 kinase alpha-3 [399-740]
Synonyms:
ISPK1 | KS6A3_HUMAN | MAPKAPK1B | RPS6KA3 | RSK2 | Ribosomal S6 kinase 2 (RSK-2)
Type:
Enzyme
Mol. Mass.:
38435.14
Organism:
Homo sapiens (Human)
Description:
aa 399-740; RSK2 C-terminal kinase domain (CTD)
Residue:
342
Sequence:
MQTVGVHSIVQQLHRNSIQFTDGYEVKEDIGVGSYSVCKRCIHKATNMEFAVKIIDKSKRDPTEEIEILLRYGQHPNIITLKDVYDDGKYVYVVTELMKGGELLDKILRQKFFSEREASAVLFTITKTVEYLHAQGVVHRDLKPSNILYVDESGNPESIRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDAACDIWSLGVLLYTMLTGYTPFANGPDDTPEEILARIGSGKFSLSGGYWNSVSDTAKDLVSKMLHVDPHQRLTAALVLRHPWIVHWDQLPQYQLNRQDAPHLVKGAMAATYSALNRNQSPVLEPVGRSTLAQRRGIKKITSTAL
  
Inhibitor
Name:
BDBM259865
Synonyms:
US9505766, 70
Type:
Small organic molecule
Emp. Form.:
C30H34N6O2
Mol. Mass.:
510.63
SMILES:
Cc1ccc(cc1)-c1c(\C=C(/C#N)C(=O)NC23CC4CC(CC(C4)C2)C3)n(CCCO)c2ncnc(N)c12 |TLB:23:22:25:19.18.17,23:18:25:22.24.21,THB:15:16:19:22.23.21,24:22:19:25.16.17,24:16:19:22.23.21|
Structure:
Search PDB for entries with ligand similarity: