Compound name
L-Moses
Protein family
Bromodomain
Target name
KAT2A@BRD
Affinity biochemical (nM)
220
Affinity on-target cellular (nM)
220
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000218c
SMILES
Cc1nnc2c3ccccc3c(N[C@@H](C)[C@H](c3ccccc3)N(C)C)nn12
InChIKey
MSFPLTWUFWOKBX-IFXJQAMLSA-N
NCBI gene ID
2648
UniProt ID
Q92830
Synonyms
GCN5, PCAF-b
Mode of action
Inhibitor
Negative control
D-Moses
Affinity biochemical definition
IC50
Affinity biochemical assay type
BROMOscan assay (DiscoverX)
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/L-Moses
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Competing pull-down assay (full-length GCN5 from cell lysates using immobilized L-Moses)
Affinity on-target cellular relation
=
Selectivity platform
Bromodomain panel, literature
Selectivity platform number of targets
48
Selectivity remarks
Screened in DSF assay at 10 µM: highly selective, other targets <2 K; Screened against 130 enzymes (GPCR panel and Eurofins panel) at 10 µM, closest targets: opioid receptors, Ki(MU) = 100 nM, Ki(OPRL1) = 840 nM, Ki(kappa) = 1100 nM, and 5-HAT transporter, Ki = 220 nM
Selectivity Source Knowledge
https://doi.org/10.1002/anie.201610816
https://www.thesgc.org/chemical-probes/L-Moses
Selectivity Number of Off-targets
0