Compound name
BIX 02565
Protein family
Protein Kinase
Target name
RPS6KA3@kinase 1
Affinity biochemical (nM)
1.1
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000679a
SMILES
C[C@@H]1CCNC(=O)C2=CC3=C(N12)C=C(C=C3)C(=O)NC4=NC5=CC=CC=C5N4CCCN(C)C
InChIKey
ZHMXXVNQAFCXKK-QGZVFWFLSA-N
NCBI gene ID
6197
UniProt ID
P51812
Synonyms
RSK2, HU-3
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Kinase Glo Plus assay (Promega; 0.75 µM ATP)
Affinity Biochemical Source Knowledge
https://doi.org/10.1016/j.bmcl.2011.10.029
https://patents.google.com/patent/WO2011071716A1/en
Affinity biochemical relation
=
Selectivity platform
SelectScreen (Invitrogen)
Selectivity platform number of targets
200
Selectivity remarks
Screened at 1 µM, closest targets: IC50(PRKD2) = 139 nM, IC50(PRKD3) = 219 nM, IC50(RET) = 161 nM, IC50(FLT3) = 714 nM, IC50(LRRK2) =16 nM, IC50(PRKD1) = 35 nM, IC50(CLK1/2) = 512/ 112 nM, IC50(FGFR2) = 320 nM, IC50(PDGFRA) = 956 nM; Screened against panel of 68 receptors, ion channels and protein targets, at 10 µM, closest targets: IC50(A1A) = 914 nM, IC50(A1B) = 52 nM, IC50(A1D) = NA, IC50(A2A) = 1420 nM, IC50(AB2) = 1820 nM, IC50(imidazoline I2) = 97 nM (PMID: 22128344)
Selectivity Source Knowledge
https://doi.org/10.1016/j.bmcl.2011.10.029
Selectivity Number of Off-targets
10