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Assay Detail

CHEMBL3579896

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Binding
Inhibition of purified mPGES-1 (1 to 152) (unknown origin) extracted from detergent-solubilized baculovirus-infected insect Sf9 cell membranes using PGH2 as substrate assessed as PGE2 production after 2.5 mins by LC/MS analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E synthase (CHEMBL5658)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics.
Luz JG, Antonysamy S, Kuklish SL, Condon B, Lee MR, Allison D, Yu XP, Chandrasekhar S, Backer R, Zhang A, Russell M, Chang SS, Harvey A, Sloan AV, Fisher MJ.
J Med Chem (2015) 58 : 4727 -4737
PubMed 25961169 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.71 6.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL180650 1 6.02
CHEMBL412099 1 5.80
CHEMBL1076694 1 5.59
CHEMBL483894 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL180650 IC50 = 960.0 nM 6.02
CHEMBL412099 IC50 = 1590.0 nM 5.80
CHEMBL1076694 IC50 = 2580.0 nM 5.59
CHEMBL483894 IC50 = 3940.0 nM 5.41