Compound name
FHT-5908
Protein family
Bromodomain
Target name
SMARCA2@BRD
Affinity biochemical (nM)
1880
Affinity on-target cellular (nM)
4350
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002235a
SMILES
C[C@H](NC(=O)c1cn(C2(C#N)CC2)cn1)C(=O)Nc1nc(-c2cccc(-c3ccn(C)n3)c2)cs1
InChIKey
DMEDHHKXKVEBDF-HNNXBMFYSA-N
NCBI gene ID
6595
UniProt ID
P51531
Synonyms
BAF190, hSNF2a, hBRM, Sth1p, SNF2LA, BRM, SNF2, SWI2
Mode of action
Negative control for FHT-2344
Affinity biochemical definition
IC50
Affinity biochemical assay type
ADP-Glo assay
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/FHT-2344
Affinity biochemical relation
0
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Luciferase transporter assay (SMARCA-mutant cell line)
Affinity on-target cellular source knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/FHT-2344
Affinity on-target cellular relation
0
Selectivity platform
GPCR panel (PDSP screen)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, closest targets as % of inhibition: SLC6A3 (-151.28%), SIGMAR1 (83.25%), HTR2B (86.81%), GABA/PBR (64.56%), SLC6A2 (69.81%); In-vitro potency (enzymatic assay): Ki(SLC6A3) >10000 nM, Ki(SIGMAR1) = 416.9 nM, Ki(HTR2B) = 507.65 nM, Ki(GABA/PBR) = 1583.39 nM, Ki(SLC6A2) = 8271.8 nM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!usageview/FHT-2344
Selectivity Number of Off-targets
3