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Assay Detail

CHEMBL762913

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Binding
In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (66 nM) using [14C]AA (50 uM) was determined
ChEMBL ↗
74
Total Activities
74
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

Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors.
Kalgutkar AS, Marnett AB, Crews BC, Remmel RP, Marnett LJ.
J Med Chem (2000) 43 : 2860 -2870
PubMed 10956194 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 74 6.72 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95402 — — 1 7.40
CHEMBL100331 — — 1 7.40
CHEMBL330194 — — 1 7.40
CHEMBL95643 — — 1 7.40
CHEMBL316866 — — 1 7.40
CHEMBL433160 — — 1 7.35
CHEMBL98514 — — 1 7.33
CHEMBL97179 — — 1 7.30
CHEMBL319148 — — 1 7.30
CHEMBL96954 — — 1 7.30
CHEMBL95989 — — 1 7.30
CHEMBL99199 — — 1 7.30
CHEMBL319764 — — 1 7.30
CHEMBL97562 — — 1 7.30
CHEMBL421385 — — 1 7.30
CHEMBL329480 — — 1 7.28
CHEMBL265078 — — 1 7.26
CHEMBL97846 — — 1 7.25
CHEMBL95558 — — 1 7.24
CHEMBL317332 — — 1 7.22
CHEMBL318206 — — 1 7.22
CHEMBL95625 — — 1 7.22
CHEMBL95311 — — 1 7.22
CHEMBL421570 — — 1 7.22
CHEMBL319359 — — 1 7.22
CHEMBL100092 — — 1 7.22
CHEMBL100091 — — 1 7.22
CHEMBL318881 — — 1 7.12
CHEMBL330162 — — 1 7.10
CHEMBL97411 — — 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95402 — IC50 = 40.0 nM 7.40
CHEMBL100331 — IC50 = 40.0 nM 7.40
CHEMBL330194 — IC50 = 40.0 nM 7.40
CHEMBL95643 — IC50 = 40.0 nM 7.40
CHEMBL316866 — IC50 = 40.0 nM 7.40
CHEMBL433160 — IC50 = 45.0 nM 7.35
CHEMBL98514 — IC50 = 47.0 nM 7.33
CHEMBL99199 — IC50 = 50.0 nM 7.30
CHEMBL421385 — IC50 = 50.0 nM 7.30
CHEMBL97562 — IC50 = 50.0 nM 7.30
CHEMBL319764 — IC50 = 50.0 nM 7.30
CHEMBL95989 — IC50 = 50.0 nM 7.30
CHEMBL96954 — IC50 = 50.0 nM 7.30
CHEMBL319148 — IC50 = 50.0 nM 7.30
CHEMBL97179 — IC50 = 50.0 nM 7.30
CHEMBL329480 — IC50 = 52.0 nM 7.28
CHEMBL265078 — IC50 = 55.0 nM 7.26
CHEMBL97846 — IC50 = 56.0 nM 7.25
CHEMBL95558 — IC50 = 58.0 nM 7.24
CHEMBL100092 — IC50 = 60.0 nM 7.22
CHEMBL100091 — IC50 = 60.0 nM 7.22
CHEMBL319359 — IC50 = 60.0 nM 7.22
CHEMBL421570 — IC50 = 60.0 nM 7.22
CHEMBL95625 — IC50 = 60.0 nM 7.22
CHEMBL318206 — IC50 = 60.0 nM 7.22
CHEMBL317332 — IC50 = 60.0 nM 7.22
CHEMBL95311 — IC50 = 60.0 nM 7.22
CHEMBL318881 — IC50 = 75.0 nM 7.12
CHEMBL330162 — IC50 = 80.0 nM 7.10
CHEMBL97411 — IC50 = 90.0 nM 7.05
CHEMBL99933 — IC50 = 100.0 nM 7.00
CHEMBL328864 — IC50 = 100.0 nM 7.00
CHEMBL318053 — IC50 = 120.0 nM 6.92
CHEMBL96011 — IC50 = 120.0 nM 6.92
CHEMBL318410 — IC50 = 120.0 nM 6.92
CHEMBL95469 — IC50 = 120.0 nM 6.92
CHEMBL327751 — IC50 = 140.0 nM 6.85
CHEMBL95572 — IC50 = 150.0 nM 6.82
CHEMBL95380 — IC50 = 190.0 nM 6.72
CHEMBL2112399 — IC50 = 190.0 nM 6.72
CHEMBL319578 — IC50 = 200.0 nM 6.70
CHEMBL330381 — IC50 = 220.0 nM 6.66
CHEMBL95988 — IC50 = 250.0 nM 6.60
CHEMBL73572 — IC50 = 250.0 nM 6.60
CHEMBL329052 — IC50 = 250.0 nM 6.60
CHEMBL24415 — IC50 = 250.0 nM 6.60
CHEMBL96057 — IC50 = 300.0 nM 6.52
CHEMBL2111594 — IC50 = 400.0 nM 6.40
CHEMBL319825 — IC50 = 400.0 nM 6.40
CHEMBL329292 — IC50 = 500.0 nM 6.30