Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL848481

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

Functional
In vitro inhibitory effect on production of prostaglandin E2 (PGE2) in rat synovial cells.
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclooxygenase (CHEMBL2095157)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.
Inagaki M, Tsuri T, Jyoyama H, Ono T, Yamada K, Kobayashi M, Hori Y, Arimura A, Yasui K, Ohno K, Kakudo S, Koizumi K, Suzuki R, Kawai S, Kato M, Matsumoto S.
J Med Chem (2000) 43 : 2040 -2048
PubMed 10821716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.22 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305076 1 8.68
CHEMBL64507 1 8.60
CHEMBL60496 1 8.60
CHEMBL6 INDOMETHACIN 4.0 1 8.54
CHEMBL64813 1 8.21
CHEMBL60725 1 8.04
CHEMBL291543 1 8.02
CHEMBL60738 1 8.00
CHEMBL62990 1 7.92
CHEMBL62920 1 7.89
CHEMBL65330 1 7.62
CHEMBL64585 1 7.52
CHEMBL1908355 TENIDAP 2.0 1 7.28
CHEMBL60793 1 7.00
CHEMBL302441 1 6.70
CHEMBL62632 1 6.62
CHEMBL64759 1 6.50
CHEMBL293689 1 6.50
CHEMBL64182 1 6.47
CHEMBL61731 1 6.39
CHEMBL62723 1 6.39
CHEMBL62874 1 6.16
CHEMBL302155 1 6.00
CHEMBL303365 1 5.47
CHEMBL64891 1 5.36
CHEMBL62439 1 -
CHEMBL303092 1 -
CHEMBL65140 1 -
CHEMBL65325 1 -
CHEMBL294100 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305076 IC50 = 2.1 nM 8.68
CHEMBL64507 IC50 = 2.5 nM 8.60
CHEMBL60496 IC50 = 2.5 nM 8.60
CHEMBL6 INDOMETHACIN IC50 = 2.9 nM 8.54
CHEMBL64813 IC50 = 6.2 nM 8.21
CHEMBL60725 IC50 = 9.1 nM 8.04
CHEMBL291543 IC50 = 9.5 nM 8.02
CHEMBL60738 IC50 = 10.0 nM 8.00
CHEMBL62990 IC50 = 12.0 nM 7.92
CHEMBL62920 IC50 = 13.0 nM 7.89
CHEMBL65330 IC50 = 24.0 nM 7.62
CHEMBL64585 IC50 = 30.0 nM 7.52
CHEMBL1908355 TENIDAP IC50 = 53.0 nM 7.28
CHEMBL60793 IC50 = 100.0 nM 7.00
CHEMBL302441 IC50 = 200.0 nM 6.70
CHEMBL62632 IC50 = 240.0 nM 6.62
CHEMBL64759 IC50 = 320.0 nM 6.50
CHEMBL293689 IC50 = 320.0 nM 6.50
CHEMBL64182 IC50 = 340.0 nM 6.47
CHEMBL61731 IC50 = 410.0 nM 6.39
CHEMBL62723 IC50 = 410.0 nM 6.39
CHEMBL62874 IC50 = 700.0 nM 6.16
CHEMBL302155 IC50 = 1000.0 nM 6.00
CHEMBL303365 IC50 = 3400.0 nM 5.47
CHEMBL64891 IC50 = 4400.0 nM 5.36
CHEMBL62439 IC50 < 1.0 nM -
CHEMBL303092 IC50 < 1.0 nM -
CHEMBL65140 IC50 < 1.0 nM -
CHEMBL65325 IC50 < 1.0 nM -
CHEMBL294100 IC50 < 1.0 nM -
CHEMBL304489 IC50 < 1.0 nM -