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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 (human), 13 (rat) nM
  • IC50:75 nM
Inhibitor
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

In Vivo Validations

Mouse (C57BL/6J, male), Rat (Sprague-Dawley, male), Dog (Beagle, male)
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

Reference: --

Orthogonal Probes def

AZD3988

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 5.6082
HBond acceptors 8
HBond donors 3
Atoms 57

References

Publications

    Cross References

    canSARChEMBLBindingDB

    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 5 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)...
    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