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Assay Detail

CHEMBL2329809

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

Binding
Inhibition of COX1 (unknown origin)-mediated oxidation of N,N,N,Ntetramethyl-1,4-phenylenediamine using arachidonic acid as substrate by colorimetric assay
6
Total Activities
6
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 1 (CHEMBL221)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.
Liedtke AJ, Adeniji AO, Chen M, Byrns MC, Jin Y, Christianson DW, Marnett LJ, Penning TM.
J Med Chem (2013) 56 : 2429 -2446
PubMed 23432095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.56 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6 INDOMETHACIN 4.0 1 7.70
CHEMBL2323522 1 6.12
CHEMBL2323490 1 5.66
CHEMBL178687 1 4.31
CHEMBL2323507 1 4.00
CHEMBL2323511 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6 INDOMETHACIN IC50 = 20.0 nM 7.70
CHEMBL2323522 IC50 = 750.0 nM 6.12
CHEMBL2323490 IC50 = 2190.0 nM 5.66
CHEMBL178687 IC50 = 48800.0 nM 4.31
CHEMBL2323507 IC50 = 100000.0 nM 4.00
CHEMBL2323511 IC50 > 100000.0 nM -