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Assay Detail

CHEMBL766949

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

Binding
Concentration required to inhibit 50% activity of prostaglandin synthetase was determined in vitro in mouse brain microsomes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Microsome
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Prostaglandin-H2 D-isomerase (CHEMBL4334)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Antinociceptive (aminoalkyl)indoles.
Bell MR, D'Ambra TE, Kumar V, Eissenstat MA, Herrmann JL, Wetzel JR, Rosi D, Philion RE, Daum SJ, Hlasta DJ.
J Med Chem (1991) 34 : 1099 -1110
PubMed 1900533 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.90 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13078 1 8.22
CHEMBL274833 1 7.82
CHEMBL13288 1 7.75
CHEMBL2092862 1 6.80
CHEMBL13376 CLOMETACIN 4.0 1 6.70
CHEMBL469 KETOROLAC 4.0 1 6.64
CHEMBL13215 1 6.52
CHEMBL273700 1 6.30
CHEMBL6 INDOMETHACIN 4.0 1 6.30
CHEMBL274572 1 6.16
CHEMBL1907833 1 6.16
CHEMBL275241 1 6.05
CHEMBL13319 1 5.85
CHEMBL12955 1 5.85
CHEMBL1907834 1 5.52
CHEMBL13178 PRAVADOLINE 2.0 1 5.46
CHEMBL416343 1 5.30
CHEMBL273372 1 5.30
CHEMBL337134 1 5.10
CHEMBL1907835 1 5.05
CHEMBL275312 1 5.00
CHEMBL13463 1 4.92
CHEMBL521 IBUPROFEN 4.0 1 4.89
CHEMBL154 NAPROXEN 4.0 1 4.89
CHEMBL427657 1 4.75
CHEMBL2092863 1 4.10
CHEMBL273606 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13078 IC50 = 6.0 nM 8.22
CHEMBL274833 IC50 = 15.0 nM 7.82
CHEMBL13288 IC50 = 18.0 nM 7.75
CHEMBL2092862 IC50 = 160.0 nM 6.80
CHEMBL13376 CLOMETACIN IC50 = 200.0 nM 6.70
CHEMBL469 KETOROLAC IC50 = 230.0 nM 6.64
CHEMBL13215 IC50 = 300.0 nM 6.52
CHEMBL273700 IC50 = 500.0 nM 6.30
CHEMBL6 INDOMETHACIN IC50 = 500.0 nM 6.30
CHEMBL274572 IC50 = 700.0 nM 6.16
CHEMBL1907833 IC50 = 700.0 nM 6.16
CHEMBL275241 IC50 = 900.0 nM 6.05
CHEMBL13319 IC50 = 1400.0 nM 5.85
CHEMBL12955 IC50 = 1400.0 nM 5.85
CHEMBL1907834 IC50 = 3000.0 nM 5.52
CHEMBL13178 PRAVADOLINE IC50 = 3500.0 nM 5.46
CHEMBL416343 IC50 = 5000.0 nM 5.30
CHEMBL273372 IC50 = 5000.0 nM 5.30
CHEMBL337134 IC50 = 8000.0 nM 5.10
CHEMBL1907835 IC50 = 9000.0 nM 5.05
CHEMBL275312 IC50 = 10000.0 nM 5.00
CHEMBL13463 IC50 = 12000.0 nM 4.92
CHEMBL521 IBUPROFEN IC50 = 13000.0 nM 4.89
CHEMBL154 NAPROXEN IC50 = 13000.0 nM 4.89
CHEMBL427657 IC50 = 18000.0 nM 4.75
CHEMBL2092863 IC50 = 79000.0 nM 4.10
CHEMBL273606 IC50 > 30000.0 nM -