Compound name
PF-06650833
Protein family
Protein Kinase
Target name
IRAK4
Affinity biochemical (nM)
0.2
Affinity on-target cellular (nM)
0.29
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000639a
SMILES
COC(C(C(N)=O)=C1)=CC2=C1C=CN=C2OC[C@H]3NC([C@@H](F)[C@H]3CC)=O
InChIKey
JKDGKIBAOAFRPJ-ZBINZKHDSA-N
NCBI gene ID
51135
UniProt ID
Q9NWZ3
Synonyms
NY-REN-64
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Dissociation-Enhanced Lanthanide Fluorescent Immunoassay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/28498658/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (in HEK293T cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/28498658/
Affinity on-target cellular relation
=
Selectivity platform
Invitrogen panel (inhibition)
Selectivity platform number of targets
278
Selectivity remarks
Screened at 200 nM, closest targets with >90% inhibition: IRAK1, targets with >70% inhibition: MNK2, LRRK2, CLK4, CK1g; Screened in KiNativ kinome screen (ActivX) in THP1 cell lysates at 10, 50, 200, 1000, and 5000 nM against 270 kinases; closest targets >50% inhibition at 200 nM: CSNK1G2, IRAK3, PIPK2C, CKSNK1D/E, https://pubmed.ncbi.nlm.nih.gov/28498658/; Cellular potency (NanoBRET assay in HEK293T cells): IC50(CSNK1G2) = 7.1 µM (SGC-Frankfurt, in-house data)
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/28498658/