EUB0000270b_NSD3@PWWP1

Chemical structure of compound EUB0000270b
Compound name
BI-9466
Protein family
HMT
Target name
NSD3@PWWP1
Affinity biochemical (nM)
120000
Affinity on-target cellular (nM)
10000
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000270b
SMILES
Cc1cc(CN)cc(C)c1-c1ncn(C)c1-c1cncn1C
InChIKey
SFZHMKDAVPIXRB-UHFFFAOYSA-N
NCBI gene ID
54904
UniProt ID
Q9BZ95
Synonyms
FLJ20353, WHISTLE, KMT3F
Mode of action
Negative control for BI-9321
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET binding assay (NSD3-PWWP1)
Affinity Biochemical Source Knowledge
https://www.nature.com/articles/s41589-019-0310-x
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (Nluc-NSD3-PWWP1 fusion protein in U2OS cells)
Affinity on-target cellular source knowledge
https://www.nature.com/articles/s41589-019-0310-x
Affinity on-target cellular relation
>
Selectivity platform
PWWP, WD40, and Tudor domain panel (DSLS measurements, literature)
Selectivity platform number of targets
20
Selectivity remarks
Screened at 500 µM against 10 PWWP, 4 WD40, 3 Tudor and 4 MBT domains of 20 proteins (DSLS measurements): dTagg(NSD3@PWWP1) = 0.7 K, dTagg(NSD2@PWWP1) = 0.1 K, dTagg(NSD3@PWWP2) = 0.5 K, dTagg(BRPF1@PWWP) = 0.0 K, dTagg(BRD1@PWWP) = -2.2 K, dTagg(BRPF3@PWWP) = 0.3 K, dTagg(ZCWPW1@PWWP) = 0.0 K, dTagg(DNMT3A@PWWP1) = -0.1 K, dTagg(DNMT3B@PWWP1) = 0.0 K, dTagg(MSH6@PWWP) = -0.2 K, dTagg(WDR20@PWWP) = 0.0 K, dTagg(WDR5@PWWP) = - 0.7 K, dTagg(WDR48@PWWP) = 0.1 K, dTagg(EED@PWWP) = 0.2 K, dTagg(53BP1@PWWP1) = 0.1 K, dTagg(SETDB1@PWWP) = 0.9 K, dTagg(TDRD3@PWWP) = 0.8 K, dTagg(L3MBTL3@PWWP) = 0.2 K, dTagg(L3MBTL1@PWWP1) = 0.2 K, dTagg(SCML2@PWWP1) = 0.1 K (https://www.nature.com/articles/s41589-019-0310-x); Screened at 1 µM and 10 µM against 34 protein, RNA and DNA methyltransferases and EP300 (acetyltransferase): highly selective with >80% remaining activity on all proteins tested (https://www.nature.com/articles/s41589-019-0310-x); Screened at 100 µM against 48 bromodomains (DSF assay): clean selectivity profile with all targets dTm <2K (https://www.nature.com/articles/s41589-019-0310-x)
Selectivity Source Knowledge
https://www.nature.com/articles/s41589-019-0310-x