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Assay Detail

CHEMBL762598

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

Functional
Inhibition of PGE-2 production in 3T3 (murine fibroblast) cell culture.
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Prostaglandin G/H synthase (cyclooxygenase) (CHEMBL2111349)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Dibenzoxepinone hydroxylamines and hydroxamic acids: dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity.
Hamer RR, Tegeler JJ, Kurtz ES, Allen RC, Bailey SC, Elliott ME, Hellyer L, Helsley GC, Przekop P, Freed BS, White J, Martin LL.
J Med Chem (1996) 39 : 246 -252
PubMed 8568814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.74 7.70
Inhibition 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6 INDOMETHACIN 4.0 1 7.70
CHEMBL83990 1 7.10
CHEMBL85776 1 6.96
CHEMBL84785 1 6.92
CHEMBL313428 1 6.72
CHEMBL82325 1 6.68
CHEMBL521 IBUPROFEN 4.0 1 6.66
CHEMBL84670 1 6.62
CHEMBL84599 1 6.34
CHEMBL82292 1 6.28
CHEMBL85455 1 6.12
CHEMBL86214 1 -
CHEMBL310794 1 -
CHEMBL315801 1 -
CHEMBL83425 1 -
CHEMBL314856 1 -
CHEMBL82680 1 -
CHEMBL2114190 1 -
CHEMBL312837 1 -
CHEMBL83482 1 -
CHEMBL431007 1 -
CHEMBL315944 1 -
CHEMBL85113 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6 INDOMETHACIN IC50 = 20.0 nM 7.70
CHEMBL83990 IC50 = 80.0 nM 7.10
CHEMBL85776 IC50 = 110.0 nM 6.96
CHEMBL84785 IC50 = 120.0 nM 6.92
CHEMBL313428 IC50 = 190.0 nM 6.72
CHEMBL82325 IC50 = 210.0 nM 6.68
CHEMBL521 IBUPROFEN IC50 = 220.0 nM 6.66
CHEMBL84670 IC50 = 240.0 nM 6.62
CHEMBL84599 IC50 = 460.0 nM 6.34
CHEMBL82292 IC50 = 530.0 nM 6.28
CHEMBL85455 IC50 = 750.0 nM 6.12
CHEMBL86214 Inhibition = 47.0 % -
CHEMBL310794 Inhibition = 86.0 % -
CHEMBL315801 Inhibition = 62.0 % -
CHEMBL83425 Inhibition = 73.0 % -
CHEMBL314856 Inhibition = 53.0 % -
CHEMBL82680 Inhibition = 60.0 % -
CHEMBL2114190 IC50 > 1000.0 nM -
CHEMBL312837 IC50 > 1000.0 nM -
CHEMBL83482 Inhibition = 47.0 % -
CHEMBL431007 IC50 > 1000.0 nM -
CHEMBL315944 IC50 > 1000.0 nM -
CHEMBL85113 Inhibition = 45.0 % -