Compound name
BI 1002494
Protein family
Protein Kinase
Target name
SYK
Affinity biochemical (nM)
0.8
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001692aCl
SMILES
COc1cc(-c2cc3ncccc3c(O[C@H](C)[C@H]3CNC(=O)C3)n2)cc(OC)c1OC.Cl
NCBI gene ID
6850
UniProt ID
P43405
Mode of action
Inhibitor
Negative control
BI-2492
Affinity biochemical definition
IC50
Affinity biochemical assay type
Kinase-Glo ATP (15 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/27048659/
Affinity biochemical relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
535
Selectivity remarks
Screened at 1 µM, closest targets as % of control: ZAP70 (0.875%), MAP2K5 (1.3%), LRRK3(G2019S) = 1.3%), SYK(2.4%), NEK10(3.45%), LRRK2(4%), JAK1(JH2, 5%), TTK (5.75%), STK33(9.8%), Screened also at 10 µM, full screening data available at OpenMe website, https://www.opnme.com/molecules/syk-bi1002494; Screened at 10 µM and 1 µM against 383 kinases (Kinase panel, Invitrogen), closest targets at 1 µM as % of control: FER (2%), FES (5%), LRRK2 (3%), MAP3K9 (-3%), RET (V804L, 2%), STK22D (1%), SYK (-7%), full screening data available at OpenMe website, https://www.opnme.com/molecules/syk-bi1002494; Screened at 10 µM against 64 other enzymes (GPCRs, ion channels, SafetyScreen44™), closest targets as % of control: D2 (agonist, 3%), full screening data available at OpenMe website, https://www.opnme.com/molecules/syk-bi1002494;
Selectivity Source Knowledge
https://www.opnme.com/molecules/syk-bi1002494
Selectivity Number of Off-targets
7