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TP-020 | Inhibitor of MGAT2
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
MGAT2
  • IC50:7.8 nM (human) 2.4 nM (Mouse)
  • IC50:160 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - MGAT1 2.6 uM, DGAT1 >30 uM, DGAT2 >30 uM , ACAT1 19 uM

In Cell Selectivity Assessment
Selectivity Assessment Description:
KinomeSCAN and GPCR scan available from SGC

Potency
Cellular
In Vitro

MGAT2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

In Vivo Validations

Male C57BL/6J mice
Dose: 0.1-1-3-10-30 mg/Kg
Route of delivery: Oral
Systemic clearance: 205 mL/h/kg

Reference: --

Negative Control Compounds

TP-020n

Chemical Information

Molecular Formula C27H21ClF5N7O3S
SMILEs Cn1nc(C(F)(F)F)cc1-c1cnc(N2CCc3cc(S(=O)(=O)Nc4c(F)cc(Cl)cc4F)cc(N4CCCC4=O)c32)nc1
InChI InChI=1S/C27H21ClF5N7O3S/c1-38-20(11-22(36-38)27(31,32)33)15-12-34-26(35-13-15)40-6-4-14-7-17(10-21(25(14)40)39-5-2-3-23(39)41)44(42,43)37-24-18(29)8-16(28)9-19(24)30/h7-13,37H,2-6H2,1H3
Molecular weight 653.10 Da
AlogP 5.4493000000000045
HBond acceptors 10
HBond donors 1
Atoms 65

References

Publications

    Cross References

    canSARChEMBLBindingDBSGC additional compound analysis

    Vendors

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    Expert Reviews

    by SERP
    (on 24 Sept 2020 )
    Cellular Use Rating
    In Model Organisms
    Probe molecule was evaluated against MGAT2 in vitro, but not in cells. Evaluated against recombinant preparations of DGAT1, DGAT2 and ACAT1 shows selectivity for MGAT2. No data shown for other MGAT...
    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