Compound name
LP99
Protein family
Bromodomain
Target name
BRD7
Affinity biochemical (nM)
909
Affinity on-target cellular (nM)
3700
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000227c
SMILES
Cc1cc(=O)n(C)c2cc(N3C(=O)CC[C@H](NS(=O)(=O)CC(C)C)[C@H]3c3ccc(Cl)cc3)ccc12
InChIKey
LVDRREOUMKACNJ-BKMJKUGQSA-N
Mode of action
Inhibitor
Negative control
(2S,3R)-LP99, enantiomer of LP99
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://onlinelibrary.wiley.com/doi/10.1002/anie.201501394
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (BRD7-H3.3 interactions in HEK293 cells)
Affinity on-target cellular source knowledge
https://onlinelibrary.wiley.com/doi/10.1002/anie.201501394
Affinity on-target cellular relation
=
Selectivity platform
CEREP screen (receptors and ion channels, Eurofins)
Selectivity platform number of targets
55
Selectivity remarks
Screened at 10 µM, closest target as % of control: NK3 (66%); Screened at 10 µM against 48 BRDs in DSF assays: clean selectivity profile with dTm <1 K for all BRDs, including other members of sub-family IV, except BRD7/9;
In-vitro potency (TR-FRET binding assay): IC50(BRD9) = 325 nM;
Disruption of BRD9 interactions with chromatin at a concentration of 0.8 µM (FRAP assay);
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(BRD7) = 3.3 µM, IC50(BRD9) = 6.2 µM;
In-vitro potency (TR-FRET binding assay): IC50(BRD9) = 325 nM;
Disruption of BRD9 interactions with chromatin at a concentration of 0.8 µM (FRAP assay);
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(BRD7) = 3.3 µM, IC50(BRD9) = 6.2 µM;
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/LP99
Selectivity Number of Off-targets
0