Compound name
UNC1215
Protein family
MBT
Target name
L3MBTL3@MBT1
Affinity biochemical (nM)
40
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000214b
SMILES
O=C(c1ccc(C(=O)N2CCC(N3CCCC3)CC2)c(Nc2ccccc2)c1)N1CCC(N2CCCC2)CC1
InChIKey
PQOOIERVZAXHBP-UHFFFAOYSA-N
NCBI gene ID
84456
UniProt ID
Q96JM7
Synonyms
KIAA1798
Mode of action
Antagonist
Negative control
UNC1079
Affinity biochemical definition
IC50
Affinity biochemical assay type
AlphaScreen assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1038/nchembio.1157
https://www.thesgc.org/chemical-probes/UNC1215
Affinity biochemical relation
=
Selectivity platform
Kme reader domain panel, literature
Selectivity platform number of targets
200
Selectivity remarks
Selective; <50% inhibition at 250 mM against 10 HMT targets; >50-fold selective against other members of human MBT family: IC50(L3MBTL1) = 2 µM, IC50(L3MBTL4) = 11 µM, IC50(SFMBT) >30 µM, IC50(MBTD1) = 6 µM (Alphascreen assay); Histone demethylases: < 50% inhibition at 10 mM versus 35 targets; Bromodomains: Tm shift < 0.5 °C at 10 mM versus 12 targets (DSF assay); Kinases: < 15% inhibition at 10 mM versus 49 kinases, closest target as % of contr.: FLT3 (64%); NIMH Psychoactive Drug Screening Program Selectivity Panel (Radioligand binding assay): Ki(M1) = 97 nM, Ki(M2) = 72 nM, Ki(M3) = 890 nM, Ki(M4) = 400 nM, Ki(M5) = 4.3 µM, Ki(Alpha 2C) = 860 nM
Selectivity Source Knowledge
https://doi.org/10.1038/nchembio.1157
https://www.thesgc.org/chemical-probes/UNC1215
Selectivity Number of Off-targets
0