Compound name
NVS-MLLT-1
Protein family
YEATS
Target name
MLLT1
Affinity biochemical (nM)
150
Affinity on-target cellular (nM)
500
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000283b
SMILES
C[C@H]1CCCN1Cc1nc2cc(NC(=O)c3ccc4cnccc4c3)ccc2[nH]1
InChIKey
ZRTFTZCKJUNZIU-HNNXBMFYSA-N
NCBI gene ID
4298
UniProt ID
Q03111
Synonyms
ENL, LTG19, YEATS1
Mode of action
Inhibitor
Negative control
NVS-iMLLT-C
Affinity biochemical definition
IC50
Affinity biochemical assay type
AlphaScreen assay
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/NVS-MLLT-1
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
Bromodomain panel, literature
Selectivity platform number of targets
42
Selectivity remarks
Selective across all bromodomains (IC50(CERC2) >40 µM, IC50(YESTS2/4) >20 µM (TR-FRET assay); Screened against 59 kinases (PSP kinase safety panel, Eurofins), closest targets: IC50(TRB2) = 3.5 µM, IC50(PIM1) = 8.6 µM, others >30 µM, Screened against 31 other targets (GPCRs, transporter and ion channels, PSP Principial panel 20118+, Eurofins), closest targets: IC50(ACES) = 250 nM, IC50(H3) = 290 nM, IC50(M2) = 1.8 µM, IC50(NET) = 8.7 µM, others >30 µM;
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/NVS-MLLT-1
Selectivity Number of Off-targets
0