Compound name
TP-020
Protein family
Transferase
Target name
MGAT2
Affinity biochemical (nM)
7.8
Affinity on-target cellular (nM)
160
CG-Set
Other targets
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000315b
SMILES
Cn1nc(C(F)(F)F)cc1-c1cnc(N2CCc3cc(S(=O)(=O)Nc4c(F)cc(Cl)cc4F)cc(N4CCCC4=O)c32)nc1
InChIKey
VSZRYLHBOKTNBO-UHFFFAOYSA-N
NCBI gene ID
4247
UniProt ID
Q10469
Synonyms
MGAT2
Mode of action
Inhibitor
Negative control
TP-020n
Affinity biochemical definition
IC50
Affinity biochemical assay type
RapidFire/MS assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1016/j.bmc.2015.06.003
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-020
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Cell-based assay
Affinity on-target cellular relation
=
Selectivity remarks
High selectivity over other acyltransferases, >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); Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: MARK3 (12%), FLT3(ITD,F691L) (32%), SRPK2 (34%); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest target: Ki(HTR1D) = 4.65 µM
Selectivity Source Knowledge
https://doi.org/10.1016/j.bmc.2015.06.003
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-020