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Assay Detail

CHEMBL3705053

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

Binding
Radioactivity Assay: The determination of IC50 values was performed with enzyme isolated from human placenta (Luu-The, V. et al., J. Steroid Biochem. Mol. Biol., 55:581-587 (1995): Sam, K. M. et al., Drug Des Discov., 15:157-180 (1997)). The radioactivity is determined by means of scintillation measurement.
17
Total Activities
17
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

17-beta-hydroxysteroid dehydrogenase type 1 (CHEMBL3181)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.28 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3645224 1 8.15
CHEMBL3645221 1 8.00
CHEMBL3645217 1 7.70
CHEMBL1650657 1 7.70
CHEMBL1650658 1 7.64
CHEMBL3645225 1 7.52
CHEMBL1650647 1 7.41
CHEMBL1650655 1 7.40
CHEMBL3645219 1 7.30
CHEMBL3645223 1 7.30
CHEMBL3645226 1 7.22
CHEMBL3645215 1 7.16
CHEMBL3645218 1 7.05
CHEMBL3645222 1 6.94
CHEMBL3645220 1 6.85
CHEMBL3645216 1 6.30
CHEMBL1650646 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3645224 IC50 = 7.0 nM 8.15
CHEMBL3645221 IC50 = 10.0 nM 8.00
CHEMBL3645217 IC50 = 20.0 nM 7.70
CHEMBL1650657 IC50 = 20.0 nM 7.70
CHEMBL1650658 IC50 = 23.0 nM 7.64
CHEMBL3645225 IC50 = 30.0 nM 7.52
CHEMBL1650647 IC50 = 39.0 nM 7.41
CHEMBL1650655 IC50 = 40.0 nM 7.40
CHEMBL3645219 IC50 = 50.0 nM 7.30
CHEMBL3645223 IC50 = 50.0 nM 7.30
CHEMBL3645226 IC50 = 60.0 nM 7.22
CHEMBL3645215 IC50 = 70.0 nM 7.16
CHEMBL3645218 IC50 = 90.0 nM 7.05
CHEMBL3645222 IC50 = 114.0 nM 6.94
CHEMBL3645220 IC50 = 140.0 nM 6.85
CHEMBL3645216 IC50 = 500.0 nM 6.30
CHEMBL1650646 IC50 = 840.0 nM 6.08