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Assay Detail

CHEMBL948317

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

Binding
Inhibition of steroid sulfatase-mediated conversion of [3H]E1S to E1
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

Steryl-sulfatase (CHEMBL3559)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents.
Leese MP, Jourdan FL, Gaukroger K, Mahon MF, Newman SP, Foster PA, Stengel C, Regis-Lydi S, Ferrandis E, Di Fiore A, De Simone G, Supuran CT, Purohit A, Reed MJ, Potter BV.
J Med Chem (2008) 51 : 1295 -1308
PubMed 18260615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.99 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190628 1 7.80
CHEMBL218382 1 7.41
CHEMBL408967 1 6.89
CHEMBL407952 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190628 IC50 = 16.0 nM 7.80
CHEMBL218382 IC50 = 39.0 nM 7.41
CHEMBL408967 IC50 = 130.0 nM 6.89
CHEMBL407952 IC50 = 1400.0 nM 5.85