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Assay Detail

CHEMBL3761674

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

Binding
Inhibition of mPGES1 in rhIL-1beta-stimulated human A549 cells assessed as PGE2 level treated for 18 hrs after 30 mins pre-incubation with rhIL-1beta by EIA method
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

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 19 6.26 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342693 1 7.92
CHEMBL3758953 1 7.72
CHEMBL3758924 1 7.43
CHEMBL3759288 1 7.41
CHEMBL412099 1 7.12
CHEMBL3758222 1 7.01
CHEMBL2152710 1 6.55
CHEMBL3758879 1 6.14
CHEMBL2152712 LY-3031207 1.0 1 6.06
CHEMBL3758663 1 5.91
CHEMBL3758186 1 5.91
CHEMBL2152711 1 5.56
CHEMBL3760103 1 5.50
CHEMBL3759737 1 5.49
CHEMBL3758743 1 5.49
CHEMBL3759709 1 5.33
CHEMBL3760032 1 5.05
CHEMBL3759119 1 5.05
CHEMBL3758980 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342693 IC50 = 12.0 nM 7.92
CHEMBL3758953 IC50 = 19.0 nM 7.72
CHEMBL3758924 IC50 = 37.0 nM 7.43
CHEMBL3759288 IC50 = 39.0 nM 7.41
CHEMBL412099 IC50 = 76.0 nM 7.12
CHEMBL3758222 IC50 = 98.0 nM 7.01
CHEMBL2152710 IC50 = 284.0 nM 6.55
CHEMBL3758879 IC50 = 720.0 nM 6.14
CHEMBL2152712 LY-3031207 IC50 = 870.0 nM 6.06
CHEMBL3758663 IC50 = 1230.0 nM 5.91
CHEMBL3758186 IC50 = 1230.0 nM 5.91
CHEMBL2152711 IC50 = 2770.0 nM 5.56
CHEMBL3760103 IC50 = 3150.0 nM 5.50
CHEMBL3759737 IC50 = 3230.0 nM 5.49
CHEMBL3758743 IC50 = 3250.0 nM 5.49
CHEMBL3759709 IC50 = 4620.0 nM 5.33
CHEMBL3760032 IC50 = 8860.0 nM 5.05
CHEMBL3759119 IC50 = 8850.0 nM 5.05
CHEMBL3758980 IC50 > 10000.0 nM -