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Assay Detail

CHEMBL968790

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

Binding
Inhibition of human recombinant 20-alpha HSD expressed in BAEC assessed as inhibition of progesterone metabolism treated 2 hrs before progesterone challenge measured after 6 hrs by LC-MS analysis
2
Total Activities
2
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

Aldo-keto reductase family 1 member C1 (CHEMBL5905)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1).
El-Kabbani O, Scammells PJ, Gosling J, Dhagat U, Endo S, Matsunaga T, Soda M, Hara A.
J Med Chem (2009) 52 : 3259 -3264
PubMed 19397269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.99 6.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387536 1 6.34
CHEMBL447448 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387536 IC50 = 460.0 nM 6.34
CHEMBL447448 IC50 = 2300.0 nM 5.64