Compound name
Pexidartinib
Protein family
Protein Kinase
Target name
CSF1R
Affinity biochemical (nM)
20
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001865a
SMILES
FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1
InChIKey
JGWRKYUXBBNENE-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 assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22039576/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Invitrogen SelectScreen™ profiling service)
Selectivity platform number of targets
226
Selectivity remarks
Screened at 1 µM, in-vitro potency of the closest target in the screen: IC50(FLT3) = 160 nM, IC50(KDR) = 350 nM, IC50(LCK) = 860 nM, IC50(FLT1) = 880 nM, IC50(NTRK3) = 890 nM; In-vitro potency (Kinobeads assay): Kd(PRKCQ) = 6 nM, Kd(FLT3) = 55 nM, https://www.science.org/doi/10.1126/science.aan4368;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22039576/
Selectivity Number of Off-targets
5