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GSK2973980A | Inhibitor of DGAT1
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
DGAT1
  • IC50:3.3 nM
  • IC50:75 nM
up to 100 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Radiometric Assay
Selectivity Assessment Description:
<strong>Within Target Family: </strong>exhibited &gt;2900-fold selectivity over human DGAT2, ACAT ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Thermal Shift Assay
Selectivity Assessment Description:
Out of the 7103 quantified proteins, in addition to DGAT1, the thermal stability of only two othe ...

Potency
Cellular
In Vitro

DGAT1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acsmedchemlett.7b00450

In Vivo Validations

Mouse, Rat, Dog
Dose: 1, 3, 10 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 2.6 h
Systemic clearance: 3.3 (R), 13.3 (M), 5.1 (D) mL/min/kg

DOI Reference: 10.1021/acsmedchemlett.7b00450

Orthogonal Probes def

AZD-3988
T863

Chemical Information

Molecular Formula C25H19F5N4O4
SMILEs O=C(O)C[C@]1(CC(F)(F)F)CCc2cc(-c3cnc(NC(=O)Nc4ccc(F)c(F)c4)cn3)ccc2C1=O
InChI InChI=1S/C25H19F5N4O4/c26-17-4-2-15(8-18(17)27)33-23(38)34-20-11-31-19(10-32-20)14-1-3-16-13(7-14)5-6-24(22(16)37,9-21(35)36)12-25(28,29)30/h1-4,7-8,10-11H,5-6,9,12H2,(H,35,36)(H2,32,33,34,38)/t24-/m0/s1
Molecular weight 534.13 Da
AlogP 5.608200000000004
HBond acceptors 8
HBond donors 3
Atoms 57

Vendors

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Expert Reviews

by SERP
(on 20 May 2021)
Cellular Use Rating
In Model Organisms
Regarding the doses used in vivo and mode of delivery, one needs to think about the goal of the experiment. The authors observed high inhibition of triglyceride synthesis in mice at a low dose of 0.088...
by SERP
(on 4 Aug 2021)
Cellular Use Rating
In Model Organisms
GSK2973980A has an acceptable in-vitro profile against its primary target and the off-targets that have been explored. There remains the possibility of in-vivo effects (desired efficacy and safety/toxicity)...
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