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Assay Detail

CHEMBL1803828

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

Binding
Inhibition of human 15-PGDH expressed in Escherichia coli using PGE2 as substrate and NAD+ as coenzyme assessed as formation of NADH by spectrophotometric analysis
9
Total Activities
9
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

15-hydroxyprostaglandin dehydrogenase [NAD(+)] (CHEMBL1293255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase inhibitors.
Wu Y, Karna S, Choi CH, Tong M, Tai HH, Na DH, Jang CH, Cho H.
J Med Chem (2011) 54 : 5260 -5264
PubMed 21650226 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.65 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800139 1 8.10
CHEMBL1800143 1 8.00
CHEMBL1800140 1 7.72
CHEMBL1800144 1 7.62
CHEMBL1800138 1 7.60
CHEMBL1800142 1 7.55
CHEMBL1800141 1 7.33
CHEMBL599406 1 7.29
CHEMBL1800076 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800139 IC50 = 8.0 nM 8.10
CHEMBL1800143 IC50 = 10.0 nM 8.00
CHEMBL1800140 IC50 = 19.0 nM 7.72
CHEMBL1800144 IC50 = 24.0 nM 7.62
CHEMBL1800138 IC50 = 25.0 nM 7.60
CHEMBL1800142 IC50 = 28.0 nM 7.55
CHEMBL1800141 IC50 = 47.0 nM 7.33
CHEMBL599406 IC50 = 51.0 nM 7.29
CHEMBL1800076 IC50 > 50000.0 nM -