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Assay Detail

CHEMBL1068436

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

Binding
Inhibition of human 17beta-HSD3 expressed in HeLa cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

17-beta-hydroxysteroid dehydrogenase type 3 (CHEMBL4234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.
Harada K, Kubo H, Tomigahara Y, Nishioka K, Takahashi J, Momose M, Inoue S, Kojima A.
Bioorg Med Chem Lett (2010) 20 : 272 -275
PubMed 19954971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.64 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL589158 1 8.82
CHEMBL590129 1 8.52
CHEMBL589396 1 8.10
CHEMBL589156 1 8.00
CHEMBL592758 1 7.70
CHEMBL590378 1 7.57
CHEMBL592043 1 7.52
CHEMBL590379 1 7.33
CHEMBL605407 1 7.23
CHEMBL590376 1 7.06
CHEMBL601700 1 7.04
CHEMBL605082 1 7.03
CHEMBL590131 1 7.02
CHEMBL600114 1 7.00
CHEMBL589883 1 7.00
CHEMBL104679 1 6.72
CHEMBL592042 1 6.70
CHEMBL589155 1 6.70
CHEMBL19240 1 6.68
CHEMBL590377 1 6.64
CHEMBL591811 1 6.62
CHEMBL590613 1 6.50
CHEMBL592761 1 6.38
CHEMBL590130 1 6.00
CHEMBL593427 1 6.00
CHEMBL609568 1 6.00
CHEMBL593424 1 6.00
CHEMBL593904 1 6.00
CHEMBL325841 1 6.00
CHEMBL12208 HYMECROMONE 2.0 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL589158 IC50 = 1.5 nM 8.82
CHEMBL590129 IC50 = 3.0 nM 8.52
CHEMBL589396 IC50 = 8.0 nM 8.10
CHEMBL589156 IC50 = 10.0 nM 8.00
CHEMBL592758 IC50 = 20.0 nM 7.70
CHEMBL590378 IC50 = 27.0 nM 7.57
CHEMBL592043 IC50 = 30.0 nM 7.52
CHEMBL590379 IC50 = 47.0 nM 7.33
CHEMBL605407 IC50 = 59.0 nM 7.23
CHEMBL590376 IC50 = 88.0 nM 7.06
CHEMBL601700 IC50 = 91.0 nM 7.04
CHEMBL605082 IC50 = 93.0 nM 7.03
CHEMBL590131 IC50 = 96.0 nM 7.02
CHEMBL600114 IC50 = 100.0 nM 7.00
CHEMBL589883 IC50 = 100.0 nM 7.00
CHEMBL104679 IC50 = 190.0 nM 6.72
CHEMBL592042 IC50 = 200.0 nM 6.70
CHEMBL589155 IC50 = 200.0 nM 6.70
CHEMBL19240 IC50 = 210.0 nM 6.68
CHEMBL590377 IC50 = 230.0 nM 6.64
CHEMBL591811 IC50 = 240.0 nM 6.62
CHEMBL590613 IC50 = 320.0 nM 6.50
CHEMBL592761 IC50 = 420.0 nM 6.38
CHEMBL593904 IC50 = 1000.0 nM 6.00
CHEMBL12208 HYMECROMONE IC50 = 1000.0 nM 6.00
CHEMBL325841 IC50 = 1000.0 nM 6.00
CHEMBL593424 IC50 = 1000.0 nM 6.00
CHEMBL609568 IC50 = 1000.0 nM 6.00
CHEMBL593427 IC50 = 1000.0 nM 6.00
CHEMBL590130 IC50 = 1000.0 nM 6.00
CHEMBL592760 IC50 = 4000.0 nM 5.40
CHEMBL607808 IC50 = 5000.0 nM 5.30
CHEMBL592524 IC50 = 5000.0 nM 5.30
CHEMBL601481 IC50 = 6000.0 nM 5.22
CHEMBL592759 IC50 = 10000.0 nM 5.00
CHEMBL592757 IC50 = 10000.0 nM 5.00