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Assay Detail

CHEMBL1768320

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

Binding
Inhibition of human recombinant COX-2 after 2 mins by fluorescence assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.
Hwang SH, Wagner KM, Morisseau C, Liu JY, Dong H, Wecksler AT, Hammock BD.
J Med Chem (2011) 54 : 3037 -3050
PubMed 21434686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.76 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118 CELECOXIB 4.0 1 8.00
CHEMBL1766299 1 6.16
CHEMBL1766288 1 6.05
CHEMBL1766298 1 6.00
CHEMBL1766295 1 6.00
CHEMBL1766287 1 5.89
CHEMBL1766297 1 5.70
CHEMBL1766285 1 5.70
CHEMBL122 ROFECOXIB 4.0 1 5.70
CHEMBL1766294 1 5.60
CHEMBL1766301 1 5.55
CHEMBL1766300 1 5.52
CHEMBL1766286 1 5.22
CHEMBL1766292 1 5.16
CHEMBL1766284 1 5.16
CHEMBL6 INDOMETHACIN 4.0 1 4.77
CHEMBL1766293 1 -
CHEMBL1766296 1 -
CHEMBL1766291 1 -
CHEMBL1766290 1 -
CHEMBL1766289 1 -
CHEMBL1766302 1 -
CHEMBL1766283 1 -
CHEMBL242459 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118 CELECOXIB IC50 = 10.0 nM 8.00
CHEMBL1766299 IC50 = 700.0 nM 6.16
CHEMBL1766288 IC50 = 900.0 nM 6.05
CHEMBL1766298 IC50 = 1000.0 nM 6.00
CHEMBL1766295 IC50 = 1000.0 nM 6.00
CHEMBL1766287 IC50 = 1300.0 nM 5.89
CHEMBL1766297 IC50 = 2000.0 nM 5.70
CHEMBL1766285 IC50 = 2000.0 nM 5.70
CHEMBL122 ROFECOXIB IC50 = 2000.0 nM 5.70
CHEMBL1766294 IC50 = 2500.0 nM 5.60
CHEMBL1766301 IC50 = 2800.0 nM 5.55
CHEMBL1766300 IC50 = 3000.0 nM 5.52
CHEMBL1766286 IC50 = 6000.0 nM 5.22
CHEMBL1766292 IC50 = 7000.0 nM 5.16
CHEMBL1766284 IC50 = 7000.0 nM 5.16
CHEMBL6 INDOMETHACIN IC50 = 17000.0 nM 4.77
CHEMBL1766293 IC50 > 10000.0 nM -
CHEMBL1766296 IC50 > 10000.0 nM -
CHEMBL1766291 IC50 > 10000.0 nM -
CHEMBL1766290 IC50 > 10000.0 nM -
CHEMBL1766289 IC50 > 10000.0 nM -
CHEMBL1766302 IC50 > 10000.0 nM -
CHEMBL1766283 IC50 > 10000.0 nM -
CHEMBL242459 IC50 > 100000.0 nM -