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Assay Detail

CHEMBL999128

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

Functional
Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type MC9
Confidence 1 — Organism
Curated By Autocuration

Target

MC9 (CHEMBL614867)
Type CELL-LINE
Organism Mus musculus

Publication

Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD.
J Med Chem (2008) 51 : 3388 -3413
PubMed 18498150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.35 6.52
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118 CELECOXIB 4.0 1 6.52
CHEMBL154 NAPROXEN 4.0 1 6.48
CHEMBL272342 EFIPLADIB 2.0 1 6.05
CHEMBL26915 SC-560 1 -
CHEMBL93 ZILEUTON 4.0 1 -
CHEMBL404529 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118 CELECOXIB IC50 = 300.0 nM 6.52
CHEMBL154 NAPROXEN IC50 = 330.0 nM 6.48
CHEMBL272342 EFIPLADIB IC50 = 900.0 nM 6.05
CHEMBL26915 SC-560 IC50 < 5.0 nM -
CHEMBL93 ZILEUTON Activity - -
CHEMBL404529 IC50 > 1000.0 nM -