Assay Detail

CHEMBL3761680

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding

Inhibition of mPGES1 in LPS-induced dog whole blood assessed as suppression of PGE2 response pre-incubated for 30 mins followed by LPS addition and measured after 5 hrs by LC-MS/MS analysis

ChEMBL ↗

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Target

Prostaglandin E synthase (CHEMBL3341581) ↗

Open DB target context

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Prostaglandin E synthase (CHEMBL3341581) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Prostaglandin E synthase

CHEMBL3341581

Anchored from Assay target.

Protein identity Prostaglandin E synthase

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Canis lupus familiaris
Tissue	Blood
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Prostaglandin E synthase (CHEMBL3341581) ↗

Type	SINGLE PROTEIN
Organism	Canis familiaris

Publication

Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.

Schiffler MA, Antonysamy S, Bhattachar SN, Campanale KM, Chandrasekhar S, Condon B, Desai PV, Fisher MJ, Groshong C, Harvey A, Hickey MJ, Hughes NE, Jones SA, Kim EJ, Kuklish SL, Luz JG, Norman BH, Rathmell RE, Rizzo JR, Seng TW, Thibodeaux SJ, Woods TA, York JS, Yu XP.
J Med Chem (2016) 59 : 194 -205
PubMed 26653180 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	6.56	6.86
IC80	2	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3342693	—	—	2	6.86
CHEMBL2152712	LY-3031207	1.0	2	6.26

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3342693	—	IC50	=	139.0	nM	6.86
CHEMBL2152712	LY-3031207	IC50	=	555.0	nM	6.26
CHEMBL3342693	—	IC80	=	703.0	nM	-
CHEMBL2152712	LY-3031207	IC80	=	1.84	uM	-