Target
Ribosomal protein S6 kinase alpha-3
Ligand
BDBM6866
Substrate
n/a
Meas. Tech.
ChEMBL_586724 (CHEMBL1062870)
Kd
>10000±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-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:
BDBM6866
Synonyms:
1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b | 4-({5-amino-1-[(2,6-difluorophenyl)carbonyl]-1H-1,2,4-triazol-3-yl}amino)benzene-1-sulfonamide | 4-[[5-Amino-1-(2,6-difluorobenzoyl)-1H-1,2,4-triazol-3-yl]amino]-benzenesulfonamide | CHEMBL191003 | JNJ-7706621 | cid_5330790
Type:
Small organic molecule
Emp. Form.:
C15H12F2N6O3S
Mol. Mass.:
394.356
SMILES:
Nc1nc(Nc2ccc(cc2)S(N)(=O)=O)nn1C(=O)c1c(F)cccc1F
Structure:
Search PDB for entries with ligand similarity: