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Assay Detail

CHEMBL3100233

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

Binding
Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry
8
Total Activities
8
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

Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities.
Singh P, Shaveta, Sharma S, Bhatti R.
Bioorg Med Chem Lett (2014) 24 : 77 -82
PubMed 24332492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.92 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139 DICLOFENAC 4.0 1 7.70
CHEMBL118 CELECOXIB 4.0 1 7.40
CHEMBL3100129 1 6.16
CHEMBL6 INDOMETHACIN 4.0 1 6.02
CHEMBL3100124 1 5.21
CHEMBL3100127 1 5.14
CHEMBL3100125 1 5.10
CHEMBL117 CHRYSIN 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139 DICLOFENAC IC50 = 20.0 nM 7.70
CHEMBL118 CELECOXIB IC50 = 40.0 nM 7.40
CHEMBL3100129 IC50 = 700.0 nM 6.16
CHEMBL6 INDOMETHACIN IC50 = 960.0 nM 6.02
CHEMBL3100124 IC50 = 6200.0 nM 5.21
CHEMBL3100127 IC50 = 7300.0 nM 5.14
CHEMBL3100125 IC50 = 7900.0 nM 5.10
CHEMBL117 CHRYSIN IC50 = 25500.0 nM 4.59