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Assay Detail

CHEMBL3107541

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

Binding
Inhibition of LPS-induced COX-2 in mouse J774 cells using arachidonic acid as substrate assessed as inhibition of prostaglandin E2 production preincubated for 15 mins followed by substrate addition measured after 30 mins by RIA
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type J774
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 2 (CHEMBL4321)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
Biava M, Battilocchio C, Poce G, Alfonso S, Consalvi S, Di Capua A, Calderone V, Martelli A, Testai L, Sautebin L, Rossi A, Ghelardini C, Di Cesare Mannelli L, Giordani A, Persiani S, Colovic M, Dovizio M, Patrignani P, Anzini M.
Bioorg Med Chem (2014) 22 : 772 -786
PubMed 24373735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.79 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3104559 1 7.35
CHEMBL3104552 1 7.33
CHEMBL3104549 1 7.27
CHEMBL3104545 1 7.17
CHEMBL3104540 1 7.17
CHEMBL3104548 1 7.07
CHEMBL3104550 1 6.85
CHEMBL3104541 1 6.85
CHEMBL3104547 1 6.80
CHEMBL3104555 1 6.60
CHEMBL3104556 1 6.60
CHEMBL3104558 1 6.54
CHEMBL3104554 1 6.52
CHEMBL3104539 1 6.52
CHEMBL3104543 1 6.51
CHEMBL3104557 1 6.51
CHEMBL3104544 1 5.80
CHEMBL3104542 1 -
CHEMBL3104546 1 -
CHEMBL3104551 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3104559 IC50 = 45.0 nM 7.35
CHEMBL3104552 IC50 = 47.0 nM 7.33
CHEMBL3104549 IC50 = 54.0 nM 7.27
CHEMBL3104545 IC50 = 68.0 nM 7.17
CHEMBL3104540 IC50 = 68.0 nM 7.17
CHEMBL3104548 IC50 = 86.0 nM 7.07
CHEMBL3104550 IC50 = 140.0 nM 6.85
CHEMBL3104541 IC50 = 140.0 nM 6.85
CHEMBL3104547 IC50 = 160.0 nM 6.80
CHEMBL3104555 IC50 = 250.0 nM 6.60
CHEMBL3104556 IC50 = 249.0 nM 6.60
CHEMBL3104558 IC50 = 290.0 nM 6.54
CHEMBL3104554 IC50 = 300.0 nM 6.52
CHEMBL3104539 IC50 = 300.0 nM 6.52
CHEMBL3104543 IC50 = 310.0 nM 6.51
CHEMBL3104557 IC50 = 310.0 nM 6.51
CHEMBL3104544 IC50 = 1600.0 nM 5.80
CHEMBL3104542 IC50 - -
CHEMBL3104546 IC50 - -
CHEMBL3104551 IC50 > 10000.0 nM -