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Assay Detail

CHEMBL769653

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

Binding
Tested for inhibition against Prostaglandin G/H synthase 2
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors.
Reitz DB, Li JJ, Norton MB, Reinhard EJ, Collins JT, Anderson GD, Gregory SA, Koboldt CM, Perkins WE, Seibert K.
J Med Chem (1994) 37 : 3878 -3881
PubMed 7966148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.80 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127674 1 8.52
CHEMBL340573 1 8.52
CHEMBL108201 1 8.30
CHEMBL320784 1 8.15
CHEMBL7162 NS-398 1 8.00
CHEMBL89578 1 7.82
CHEMBL274893 SC-57666 1 7.58
CHEMBL322045 1 7.29
CHEMBL108975 1 7.28
CHEMBL111045 1 7.17
CHEMBL321182 1 7.12
CHEMBL274990 SC-58125 1 7.05
CHEMBL111039 1 6.66
CHEMBL109030 1 6.06
CHEMBL6 INDOMETHACIN 4.0 1 5.92
CHEMBL340458 1 5.65
CHEMBL109578 1 5.50
CHEMBL109486 1 5.18
CHEMBL129215 1 4.19
CHEMBL338105 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127674 IC50 = 3.0 nM 8.52
CHEMBL340573 IC50 = 3.0 nM 8.52
CHEMBL108201 IC50 = 5.0 nM 8.30
CHEMBL320784 IC50 = 7.0 nM 8.15
CHEMBL7162 NS-398 IC50 = 10.0 nM 8.00
CHEMBL89578 IC50 = 15.0 nM 7.82
CHEMBL274893 SC-57666 IC50 = 26.0 nM 7.58
CHEMBL322045 IC50 = 51.0 nM 7.29
CHEMBL108975 IC50 = 53.0 nM 7.28
CHEMBL111045 IC50 = 67.0 nM 7.17
CHEMBL321182 IC50 = 75.0 nM 7.12
CHEMBL274990 SC-58125 IC50 = 90.0 nM 7.05
CHEMBL111039 IC50 = 221.0 nM 6.66
CHEMBL109030 IC50 = 865.0 nM 6.06
CHEMBL6 INDOMETHACIN IC50 = 1200.0 nM 5.92
CHEMBL340458 IC50 = 2250.0 nM 5.65
CHEMBL109578 IC50 = 3200.0 nM 5.50
CHEMBL109486 IC50 = 6600.0 nM 5.18
CHEMBL129215 IC50 = 65000.0 nM 4.19
CHEMBL338105 IC50 = 77900.0 nM 4.11