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Assay Detail

CHEMBL1764082

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

Binding
Inhibition of mouse 11beta-HSD2 expressed in CHO-K1 cells assessed as conversion of [3H]-cortisol to [3H]-cortisone by scintillation proximity assay
35
Total Activities
35
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 type 2 (CHEMBL3490)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome.
Maletic M, Leeman A, Szymonifka M, Mundt SS, Zokian HJ, Shah K, Dragovic J, Lyons K, Thieringer R, Vosatka AH, Balkovec J, Waddell ST.
Bioorg Med Chem Lett (2011) 21 : 2568 -2572
PubMed 21421311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.20 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1761135 1 6.72
CHEMBL200513 1 5.68
CHEMBL1761309 1 -
CHEMBL1761144 1 -
CHEMBL1761315 1 -
CHEMBL1761142 1 -
CHEMBL1761141 1 -
CHEMBL1761140 1 -
CHEMBL1761139 1 -
CHEMBL1761138 1 -
CHEMBL1761137 1 -
CHEMBL1761136 1 -
CHEMBL383352 1 -
CHEMBL1761143 1 -
CHEMBL1761329 1 -
CHEMBL1761328 1 -
CHEMBL1761327 1 -
CHEMBL1761326 1 -
CHEMBL1761325 1 -
CHEMBL1761324 1 -
CHEMBL1761323 1 -
CHEMBL1761322 MK-0736 2.0 1 -
CHEMBL1761321 1 -
CHEMBL1761320 1 -
CHEMBL1761319 1 -
CHEMBL1760014 1 -
CHEMBL1761318 1 -
CHEMBL1761317 1 -
CHEMBL1761330 1 -
CHEMBL1761316 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1761135 IC50 = 190.0 nM 6.72
CHEMBL200513 IC50 = 2100.0 nM 5.68
CHEMBL383352 IC50 > 4000.0 nM -
CHEMBL1761314 IC50 > 4000.0 nM -
CHEMBL1761136 IC50 > 4000.0 nM -
CHEMBL1761137 IC50 > 4000.0 nM -
CHEMBL1761138 IC50 > 4000.0 nM -
CHEMBL1761139 IC50 > 4000.0 nM -
CHEMBL1761140 IC50 > 4000.0 nM -
CHEMBL1761141 IC50 > 4000.0 nM -
CHEMBL1761142 IC50 > 4000.0 nM -
CHEMBL1761315 IC50 > 4000.0 nM -
CHEMBL1761144 IC50 > 4000.0 nM -
CHEMBL1761309 IC50 > 4000.0 nM -
CHEMBL1761310 IC50 > 4000.0 nM -
CHEMBL1761311 IC50 > 4000.0 nM -
CHEMBL1761312 IC50 > 4000.0 nM -
CHEMBL1761313 IC50 > 4000.0 nM -
CHEMBL1761322 MK-0736 IC50 > 4000.0 nM -
CHEMBL1761316 IC50 > 4000.0 nM -
CHEMBL1761330 IC50 > 4000.0 nM -
CHEMBL1761317 IC50 > 4000.0 nM -
CHEMBL1761318 IC50 > 4000.0 nM -
CHEMBL1760014 IC50 > 4000.0 nM -
CHEMBL1761319 IC50 > 4000.0 nM -
CHEMBL1761320 IC50 > 4000.0 nM -
CHEMBL1761321 IC50 > 4000.0 nM -
CHEMBL1761143 IC50 > 4000.0 nM -
CHEMBL1761323 IC50 > 4000.0 nM -
CHEMBL1761324 IC50 > 4000.0 nM -
CHEMBL1761325 IC50 > 4000.0 nM -
CHEMBL1761326 IC50 > 4000.0 nM -
CHEMBL1761327 IC50 > 4000.0 nM -
CHEMBL1761328 IC50 > 4000.0 nM -
CHEMBL1761329 IC50 > 4000.0 nM -