Compound name
A-196
Protein family
HMT
Target name
SUV420H1@Methyltransferase
Affinity biochemical (nM)
25
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000193b
SMILES
Clc1cc2c(NC3CCCC3)nnc(-c3ccncc3)c2cc1Cl
InChIKey
ABGOSOMRWSYAOB-UHFFFAOYSA-N
NCBI gene ID
51111
UniProt ID
Q4FZB7
Synonyms
CGI-85
Mode of action
Inhibitor
Negative control
A-197,SGC2043
Affinity biochemical definition
IC50
Affinity biochemical assay type
Scintillation proximity assay (SPA)
Affinity Biochemical Source Knowledge
https://doi.org/10.1038/nchembio.2282
https://www.thesgc.org/chemical-probes/A-196
Affinity biochemical relation
=
Selectivity platform
Epigenetic methyltransferases panel, literature
Selectivity platform number of targets
29
Selectivity remarks
Highly selective in methyltransferase screen at 1 µM and 10 µM; Inactive against protein arginine methyltransferases and DNA methyltransferases; Selective against a panel of 9 epigenetic readers and chromatin binders; Screened against 125 nonepigenetic targets (CEREP panel: GPCRS, ion channels, transporters) at 10 µM, closest targets >50% inhibition: Adenosin A1 receptor (98%, Ki = 21 nM), Adenosin A2A receptor (98%, Ki = 28 nM), Cl-chanel (GABA-gated, 90%, Ki = 1.8 µM), Adenosin A2 receptor (74%, 2 µM), kappa (KOP, 62%, Ki >10 µM), NK2 (61%, Ki = 4.1 µM), delta2 (DOP, 51%, Ki = 9 µM)
Selectivity Source Knowledge
https://doi.org/10.1038/nchembio.2282
https://www.thesgc.org/chemical-probes/A-196
Selectivity Number of Off-targets
0