Compound name
OICR-9429
Protein family
E3
Target name
WDR5
Affinity biochemical (nM)
24
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000211b
SMILES
CN1CCN(c2ccc(-c3cccc(CN4CCOCC4)c3)cc2NC(=O)c2c[nH]c(=O)cc2C(F)(F)F)CC1
InChIKey
DJOVLOYCGXNVPI-UHFFFAOYSA-N
NCBI gene ID
11091
UniProt ID
P61964
Synonyms
SWD3, CFAP89
Mode of action
Antagonist
Negative control
OICR-0547
Affinity biochemical definition
Kd
Affinity biochemical assay type
Biacore
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/OICR-9429
Affinity biochemical relation
=
Selectivity platform
Protein methyltransferase panel, literature
Selectivity platform number of targets
22
Selectivity remarks
Screened at 50 µM, >1000-fold selective (IC50 >50 µM); Screened against 8 Methyl-Lysine/Arginine binder (DSF assay), dTm(WDR5) = 18.1 K, closest target: dTm(TDRD3) = 1.8 K; Screened in CEREP panel against 215 targets (kinases, GPCRs, ion channels, transporters) at 1 µM: no kinase with >50% inhibition (IC50 >1 µM)
Selectivity Source Knowledge
https://doi.org/10.1038/nchembio.1859
https://www.thesgc.org/chemical-probes/OICR-9429
Selectivity Number of Off-targets
0