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Assay Detail

CHEMBL1764757

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

Binding
Inhibition of mouse 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation counting
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL3910)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Substituted phenyl triazoles as selective inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1.
Sun W, Maletic M, Mundt SS, Shah K, Zokian H, Lyons K, Waddell ST, Balkovec J.
Bioorg Med Chem Lett (2011) 21 : 2141 -2145
PubMed 21334894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 8.19 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1760803 1 9.12
CHEMBL1760804 1 9.00
CHEMBL1760806 1 9.00
CHEMBL1760685 1 9.00
CHEMBL1760681 1 9.00
CHEMBL1760797 1 8.96
CHEMBL522701 1 8.89
CHEMBL1760796 1 8.82
CHEMBL1760802 1 8.80
CHEMBL1760805 1 8.77
CHEMBL1760690 1 8.72
CHEMBL1760793 1 8.70
CHEMBL1760791 1 8.66
CHEMBL1760809 1 8.64
CHEMBL1760691 1 8.59
CHEMBL1760795 1 8.55
CHEMBL1760687 1 8.55
CHEMBL1760792 1 8.54
CHEMBL1760674 1 8.52
CHEMBL1760799 1 8.47
CHEMBL525361 1 8.40
CHEMBL1760798 1 8.39
CHEMBL1760800 1 8.22
CHEMBL1760676 1 8.18
CHEMBL1760673 1 8.11
CHEMBL1760683 1 8.04
CHEMBL1760684 1 7.96
CHEMBL1760675 1 7.96
CHEMBL257149 1 7.85
CHEMBL1760682 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1760803 IC50 = 0.75 nM 9.12
CHEMBL1760804 IC50 = 1.0 nM 9.00
CHEMBL1760681 IC50 = 1.0 nM 9.00
CHEMBL1760806 IC50 = 1.0 nM 9.00
CHEMBL1760685 IC50 = 1.0 nM 9.00
CHEMBL1760797 IC50 = 1.1 nM 8.96
CHEMBL522701 IC50 = 1.3 nM 8.89
CHEMBL1760796 IC50 = 1.5 nM 8.82
CHEMBL1760802 IC50 = 1.6 nM 8.80
CHEMBL1760805 IC50 = 1.7 nM 8.77
CHEMBL1760690 IC50 = 1.9 nM 8.72
CHEMBL1760793 IC50 = 2.0 nM 8.70
CHEMBL1760791 IC50 = 2.2 nM 8.66
CHEMBL1760809 IC50 = 2.3 nM 8.64
CHEMBL1760691 IC50 = 2.6 nM 8.59
CHEMBL1760795 IC50 = 2.8 nM 8.55
CHEMBL1760687 IC50 = 2.8 nM 8.55
CHEMBL1760792 IC50 = 2.9 nM 8.54
CHEMBL1760674 IC50 = 3.0 nM 8.52
CHEMBL1760799 IC50 = 3.4 nM 8.47
CHEMBL525361 IC50 = 4.0 nM 8.40
CHEMBL1760798 IC50 = 4.1 nM 8.39
CHEMBL1760800 IC50 = 6.0 nM 8.22
CHEMBL1760676 IC50 = 6.6 nM 8.18
CHEMBL1760673 IC50 = 7.8 nM 8.11
CHEMBL1760683 IC50 = 9.1 nM 8.04
CHEMBL1760684 IC50 = 11.0 nM 7.96
CHEMBL1760675 IC50 = 11.0 nM 7.96
CHEMBL257149 IC50 = 14.0 nM 7.85
CHEMBL1760682 IC50 = 15.0 nM 7.82
CHEMBL1760680 IC50 = 19.0 nM 7.72
CHEMBL1760672 IC50 = 26.0 nM 7.58
CHEMBL523177 IC50 = 52.0 nM 7.28
CHEMBL1760677 IC50 = 62.0 nM 7.21
CHEMBL1760807 IC50 = 68.0 nM 7.17
CHEMBL1760671 IC50 = 87.0 nM 7.06
CHEMBL256778 IC50 = 98.0 nM 7.01
CHEMBL1760678 IC50 = 130.0 nM 6.89
CHEMBL1760808 IC50 = 150.0 nM 6.82
CHEMBL1760679 IC50 = 200.0 nM 6.70
CHEMBL1760801 IC50 < 1.0 nM -
CHEMBL1760794 IC50 < 1.0 nM -
CHEMBL1760689 IC50 < 1.0 nM -
CHEMBL1760688 IC50 < 1.0 nM -
CHEMBL1760686 IC50 < 1.0 nM -