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Assay Detail

CHEMBL1647079

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

Binding
Inhibition of human 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay
32
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group.
Kwon SW, Kang SK, Lee JH, Bok JH, Kim CH, Dal Rhee S, Jung WH, Kim HY, Bae MA, Song JS, Ha DC, Cheon HG, Kim KY, Ahn JH.
Bioorg Med Chem Lett (2011) 21 : 435 -439
PubMed 21093259 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.30 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1642841 2 8.70
CHEMBL1642622 4 8.52
CHEMBL1642618 1 8.30
CHEMBL1642620 1 8.10
CHEMBL1642843 1 8.00
CHEMBL1642608 1 8.00
CHEMBL1642613 1 8.00
CHEMBL1642614 1 8.00
CHEMBL1642615 1 8.00
CHEMBL1642624 1 7.96
CHEMBL1642623 1 7.96
CHEMBL1642840 2 7.92
CHEMBL1642621 1 7.80
CHEMBL1642844 1 7.70
CHEMBL1642609 1 7.70
CHEMBL1642612 1 7.70
CHEMBL1642842 1 7.43
CHEMBL1642610 1 7.26
CHEMBL1642606 1 7.20
CHEMBL1642619 1 7.17
CHEMBL1642611 1 6.83
CHEMBL1642617 1 6.77
CHEMBL499915 CARBENOXOLONE 2.0 1 6.30
CHEMBL1642605 1 6.26
CHEMBL1642616 1 6.17
CHEMBL1642607 1 6.03
CHEMBL1642604 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1642841 IC50 = 2.0 nM 8.70
CHEMBL1642622 IC50 = 3.0 nM 8.52
CHEMBL1642622 IC50 = 4.0 nM 8.40
CHEMBL1642622 IC50 = 4.0 nM 8.40
CHEMBL1642618 IC50 = 5.0 nM 8.30
CHEMBL1642620 IC50 = 8.0 nM 8.10
CHEMBL1642843 IC50 = 10.0 nM 8.00
CHEMBL1642608 IC50 = 10.0 nM 8.00
CHEMBL1642613 IC50 = 10.0 nM 8.00
CHEMBL1642614 IC50 = 10.0 nM 8.00
CHEMBL1642615 IC50 = 10.0 nM 8.00
CHEMBL1642624 IC50 = 11.0 nM 7.96
CHEMBL1642623 IC50 = 11.0 nM 7.96
CHEMBL1642840 IC50 = 12.0 nM 7.92
CHEMBL1642621 IC50 = 16.0 nM 7.80
CHEMBL1642844 IC50 = 20.0 nM 7.70
CHEMBL1642609 IC50 = 20.0 nM 7.70
CHEMBL1642612 IC50 = 20.0 nM 7.70
CHEMBL1642842 IC50 = 37.0 nM 7.43
CHEMBL1642610 IC50 = 55.0 nM 7.26
CHEMBL1642606 IC50 = 63.0 nM 7.20
CHEMBL1642619 IC50 = 67.0 nM 7.17
CHEMBL1642611 IC50 = 149.0 nM 6.83
CHEMBL1642617 IC50 = 170.0 nM 6.77
CHEMBL499915 CARBENOXOLONE IC50 = 500.0 nM 6.30
CHEMBL1642605 IC50 = 554.0 nM 6.26
CHEMBL1642616 IC50 = 683.0 nM 6.17
CHEMBL1642607 IC50 = 945.0 nM 6.03
CHEMBL1642841 IC50 = 1340.0 nM 5.87
CHEMBL1642604 IC50 = 2130.0 nM 5.67
CHEMBL1642622 IC50 = 7950.0 nM 5.10
CHEMBL1642840 IC50 = 38700.0 nM 4.41