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Assay Detail

CHEMBL4178552

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

Binding
Inhibition of human 17beta-HSD2 expressed in HEK293 cell lysates incubated for 10 mins using [2,4,6,7-3H]-estradiol and NAD+ by scintillation counting method
21
Total Activities
21
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 2 (CHEMBL2789)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potential Antiosteoporotic Natural Product Lead Compounds That Inhibit 17β-Hydroxysteroid Dehydrogenase Type 2.
Vuorinen A, Engeli RT, Leugger S, Bachmann F, Akram M, Atanasov AG, Waltenberger B, Temml V, Stuppner H, Krenn L, Ateba SB, Njamen D, Davis RA, Odermatt A, Schuster D.
J Nat Prod (2017) 80 : 965 -974
PubMed 28319389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.68 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL150 KAEMPFEROL 1.0 1 6.44
CHEMBL129795 ISOLIQUIRITIGENIN 1 6.44
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 6.42
CHEMBL4210403 1 6.11
CHEMBL375927 (-)-DIHYDROGUAIARETICACID 1 6.03
CHEMBL4205522 1 6.01
CHEMBL4206971 1 5.89
CHEMBL312186 1 5.82
CHEMBL50 QUERCETIN 3.0 1 5.81
CHEMBL601464 1 5.80
CHEMBL140 CURCUMIN 3.0 1 5.76
CHEMBL6665 1 5.69
CHEMBL589354 1 5.47
CHEMBL324842 ROSMARINIC ACID 1 5.43
CHEMBL128000 BUTEIN 1 5.14
CHEMBL487601 JACEOSIDINE 1 5.03
CHEMBL131921 BIOCHANIN 1 5.00
CHEMBL9352 NARINGENIN 1 4.84
CHEMBL44 GENISTEIN 2.0 1 4.78
CHEMBL276915 7-HYDROXYFLAVONE 1 -
CHEMBL28 APIGENIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL150 KAEMPFEROL IC50 = 360.0 nM 6.44
CHEMBL129795 ISOLIQUIRITIGENIN IC50 = 360.0 nM 6.44
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 380.0 nM 6.42
CHEMBL4210403 IC50 = 780.0 nM 6.11
CHEMBL375927 (-)-DIHYDROGUAIARETICACID IC50 = 940.0 nM 6.03
CHEMBL4205522 IC50 = 980.0 nM 6.01
CHEMBL4206971 IC50 = 1280.0 nM 5.89
CHEMBL312186 IC50 = 1520.0 nM 5.82
CHEMBL50 QUERCETIN IC50 = 1540.0 nM 5.81
CHEMBL601464 IC50 = 1570.0 nM 5.80
CHEMBL140 CURCUMIN IC50 = 1730.0 nM 5.76
CHEMBL6665 IC50 = 2030.0 nM 5.69
CHEMBL589354 IC50 = 3420.0 nM 5.47
CHEMBL324842 ROSMARINIC ACID IC50 = 3720.0 nM 5.43
CHEMBL128000 BUTEIN IC50 = 7300.0 nM 5.14
CHEMBL487601 JACEOSIDINE IC50 = 9300.0 nM 5.03
CHEMBL131921 BIOCHANIN IC50 = 9900.0 nM 5.00
CHEMBL9352 NARINGENIN IC50 = 14400.0 nM 4.84
CHEMBL44 GENISTEIN IC50 = 16500.0 nM 4.78
CHEMBL276915 7-HYDROXYFLAVONE IC50 > 20000.0 nM -
CHEMBL28 APIGENIN IC50 > 20000.0 nM -