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FHT-2344 | FHT-2344 : Inhibitor of SMARCA2, SMARCA4 ATPase domains
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SMARCA2
  • IC50:13.8 ± 3.3 nM
  • IC50:29.8 nM
SMARCA4
  • IC50:26.1 ± 7.3 nM
  • IC50:30.2 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Measurement of the ATPase catalytic activity using ADP-Glo™ detection reagent: CHD4 (IC50 > 200 μM, ...

Potency
Cellular
In Vitro

SMARCA2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

Other Reference: Peer reviewed at SGC

SMARCA4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

Other Reference: Peer reviewed at SGC

In Vivo Validations

Mouse
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 2.09 h
Systemic clearance: 0.985 mL/min/kg
Bioavailability: ~100%
Volume of Distribution at Steady-State: 0.207 L/Kg

Reference: --

Negative Control Compounds

FHT-5908
Notes: FHT-5908: Measurement of the ATPase catalytic activity using the ADP-Glo™ detection reagent: SMARCA2 (IC50 = 1.88 ± 0.32 μM, n= 5); SMARCA4 (IC50 = 3.99 ± 0.68 μM, n= 5) Luciferase reporter assay: SMARCA2 transcriptional activity in a SMARCA4-mutant cell line (IC50 = 4.35 ± 1.29 μM; n=3); SMARCA4 transcriptional activity in a SMARCA2-mutant cell line (IC50 = 2.37 ± 0.85 μM; n=3) Closest off-targets in the GPCR scan are: SIGMAR1 (Ki = 416.9 nM), HTR2B (Ki = 507.65 nM)
SMILES: C[C@@H](C(Nc1nc(cs1)c1cccc(c1)c1ccn(C)n1)=O)NC(c1cn(cn1)C1(CC1)C#N)=O

Orthogonal Probes def

SGC-SMARCA-BRDVIII

Chemical Information

Molecular Formula C23H24N6O5S2
SMILEs COC[C@H](NC(=O)c1ccn(S(C)(=O)=O)c1)C(=O)Nc1nc(-c2cccc(-c3ccn(C)n3)c2)cs1
InChI InChI=1S/C23H24N6O5S2/c1-28-9-8-18(27-28)15-5-4-6-16(11-15)20-14-35-23(25-20)26-22(31)19(13-34-2)24-21(30)17-7-10-29(12-17)36(3,32)33/h4-12,14,19H,13H2,1-3H3,(H,24,30)(H,25,26,31)/t19-/m0/s1
Molecular weight 528.12 Da
AlogP 0.0
HBond acceptors 11
HBond donors 2
Atoms 60

Expert Reviews

No SERP comments found for FHT-2344

Probe FHT-2344 is in the process of SERP review.

Please continue to check back for new reviews and commentary.