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TP-020

2D structure
Target MGAT2 
Mode of action Inhibitor
Control TP-020n
Recommended cellular usage concentration 1 - 10 µM
In vivo use yes
Synonyms MGAT2-IN-1
Donated by Takeda


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: MGAT2 (human): IC50 = 7.8 nM; MGAT2 (mouse): IC50 = 2.4 nM (enzyme assay);
Selectivity within target family: > 30-fold Surpasses criterion: >100-fold over mouse MGAT1 (IC50 = 2.6 µM), >1000-fold over human DGAT1 (IC50 > 30 µM), human DGAT2 (IC50 > 30 µM), human ACAT1 (IC50 = 19 µM)
Selectivity outside target family Clean PDSP scan.
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 human MGAT1: IC50 = 160 nM (cell-based assay)
Control compound (100 times less potent than the probe) Surpasses criterion: IC50 = 3300 nM, more than 100-fold weaker than the probe candidate; Clean PDSP scan.