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Assay Detail

CHEMBL3119935

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

Binding
Inhibition of COX-2 in human whole blood assessed as PGE2 level in plasma after 5 mins by enzyme immunoassay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostaglandin G/H synthase 2 (CHEMBL230)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism.
Renard JF, Lecomte F, Hubert P, de Leval X, Pirotte B.
Eur J Med Chem (2014) 74 : 12 -22
PubMed 24440378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.70 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3113234 1 7.05
CHEMBL3113239 1 6.62
CHEMBL3113224 1 6.58
CHEMBL3113235 1 6.52
CHEMBL3113240 1 6.52
CHEMBL118 CELECOXIB 4.0 1 6.46
CHEMBL3113231 1 6.26
CHEMBL56367 NIMESULIDE 4.0 1 6.16
CHEMBL3113229 1 5.98
CHEMBL3113236 1 5.80
CHEMBL3113233 1 5.71
CHEMBL3113237 1 5.64
CHEMBL3113241 1 5.00
CHEMBL3113242 1 4.68
CHEMBL3113232 1 4.51
CHEMBL3113228 1 4.46
CHEMBL3113226 1 4.44
CHEMBL3113227 1 4.25
CHEMBL3113225 1 -
CHEMBL3113230 1 -
CHEMBL3113238 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3113234 IC50 = 90.0 nM 7.05
CHEMBL3113239 IC50 = 240.0 nM 6.62
CHEMBL3113224 IC50 = 260.0 nM 6.58
CHEMBL3113235 IC50 = 300.0 nM 6.52
CHEMBL3113240 IC50 = 300.0 nM 6.52
CHEMBL118 CELECOXIB IC50 = 350.0 nM 6.46
CHEMBL3113231 IC50 = 550.0 nM 6.26
CHEMBL56367 NIMESULIDE IC50 = 700.0 nM 6.16
CHEMBL3113229 IC50 = 1040.0 nM 5.98
CHEMBL3113236 IC50 = 1570.0 nM 5.80
CHEMBL3113233 IC50 = 1960.0 nM 5.71
CHEMBL3113237 IC50 = 2270.0 nM 5.64
CHEMBL3113241 IC50 = 10050.0 nM 5.00
CHEMBL3113242 IC50 = 20680.0 nM 4.68
CHEMBL3113232 IC50 = 30740.0 nM 4.51
CHEMBL3113228 IC50 = 35090.0 nM 4.46
CHEMBL3113226 IC50 = 36230.0 nM 4.44
CHEMBL3113227 IC50 = 56760.0 nM 4.25
CHEMBL3113225 IC50 > 100000.0 nM -
CHEMBL3113230 IC50 > 100000.0 nM -
CHEMBL3113238 IC50 > 100000.0 nM -