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Assay Detail

CHEMBL2025082

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

Binding
Inhibition of recombinant COX2
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. Therapeutic leads for castrate resistant prostate cancer.
Chen M, Adeniji AO, Twenter BM, Winkler JD, Christianson DW, Penning TM.
Bioorg Med Chem Lett (2012) 22 : 3492 -3497
PubMed 22507964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.92 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23588 FLUFENAMIC ACID 2.0 1 7.70
CHEMBL1682200 1 6.13
CHEMBL1682202 1 -
CHEMBL2023820 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23588 FLUFENAMIC ACID IC50 = 20.0 nM 7.70
CHEMBL1682200 IC50 = 740.0 nM 6.13
CHEMBL1682202 IC50 > 100000.0 nM -
CHEMBL2023820 IC50 > 100000.0 nM -