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BI-99179 | BI 99179 : Inhibitor of FASN
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FASN
  • IC50:79 nM
  • IC50:570 nM
  • IC50:180 nM
Inhibitor
1-10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity within target family: No closely related mammalian proteins as potential off-targets. Se ...

Potency
Cellular
In Vitro

FASN

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.bmcl.2011.07.083

In Vivo Validations

Rat
Dose: 4 mg/kg
Systemic clearance: 8.2 ml/min/kg
Cmax: 1300 nM brain 2h
Fb : 46 %
Volume of Distribution at Steady-State: 1.6 l/kg

DOI Reference: 10.1016/j.bmcl.2011.07.083

Negative Control Compounds

BI 99990
Notes: Inhibition of FASN: >3 µM for inactive analog BI 99990; Shows weak off-target activity in the GPCR scan for TMEM97 (Sigma2) (Ki = 396.0 nM) and HRH4 (Ki = 1635.0 nM).

Orthogonal Probes def

GSK2194069

Chemical Information

Molecular Formula C23H25N3O3
SMILEs CCC(=O)N[C@H]1CC[C@@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1
InChI InChI=1S/C23H25N3O3/c1-3-21(27)24-17-11-8-16(14-17)23(28)26(2)18-12-9-15(10-13-18)22-25-19-6-4-5-7-20(19)29-22/h4-7,9-10,12-13,16-17H,3,8,11,14H2,1-2H3,(H,24,27)/t16-,17+/m1/s1
Molecular weight 391.19 Da
AlogP 4.152500000000003
HBond acceptors 6
HBond donors 1
Atoms 54

Vendors

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Expert Reviews

by SERP
(on 9 Feb 2022 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 18 Feb 2022 )
Cellular Use Rating
In Model Organisms
The compound was independently tested in an NADPH consumption assay (Singha et. al. Eur. Journal Pharm. Sciences 2020, 149, 105321) alongside GSK2194069, another FAS inhibitor reported in 2014 and was...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria