Compound name
PLX5622
Protein family
Protein Kinase
Target name
CSF1R
Affinity biochemical (nM)
16
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000697a
SMILES
CC1=CN=C(NC=C2CC3=C(F)N=C(NCC4=C(OC)N=CC(F)=C4)C=C3)C2=C1
InChIKey
NSMOZFXKTHCPTQ-UHFFFAOYSA-N
NCBI gene ID
1436
UniProt ID
P07333
Synonyms
C-FMS, CSFR, CD115
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic inhibition assay (100 µM ATP)
Affinity Biochemical Source Knowledge
https://doi.org/10.1038/s41467-019-11674-z
Affinity biochemical relation
=
Selectivity platform
SelectScreen (Invitrogen)
Selectivity platform number of targets
200
Selectivity remarks
Screened at 1 µM, closest targets: IC50(FLT3) = 390 nM, IC50(KIT) = 860 nM, IC50(AURKC) = 1000 nM, IC50(KDR) = 1100 nM (enzymatic assay with 100 µM ATP), other targets > 1 µM; Cellular selectivity: IC50(FLT3) > 10 µM (FLT3-ITD dependent proliferation of Ba/F3 cells); IC50(KIT) = 2.7 µM (BCR-KIT fusion dependent proliferation of Ba/F3 cells)
Selectivity Source Knowledge
https://doi.org/10.1038/s41467-019-11674-z
Selectivity Number of Off-targets
4