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Assay Detail

CHEMBL909906

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

Binding
Inhibitory activity against human 11beta-HSD2 by SPA
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

11-beta-hydroxysteroid dehydrogenase type 2 (CHEMBL3746)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
Rohde JJ, Pliushchev MA, Sorensen BK, Wodka D, Shuai Q, Wang J, Fung S, Monzon KM, Chiou WJ, Pan L, Deng X, Chovan LE, Ramaiya A, Mullally M, Henry RF, Stolarik DF, Imade HM, Marsh KC, Beno DW, Fey TA, Droz BA, Brune ME, Camp HS, Sham HL, Frevert EU, Jacobson PB, Link JT.
J Med Chem (2007) 50 : 149 -164
PubMed 17201418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.23 4.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217917 1 4.25
CHEMBL374728 1 4.21
CHEMBL218143 1 -
CHEMBL384364 1 -
CHEMBL218358 1 -
CHEMBL386029 1 -
CHEMBL373889 1 -
CHEMBL219142 1 -
CHEMBL424937 1 -
CHEMBL375156 1 -
CHEMBL218758 1 -
CHEMBL415429 1 -
CHEMBL375341 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217917 IC50 = 56000.0 nM 4.25
CHEMBL374728 IC50 = 62000.0 nM 4.21
CHEMBL218143 IC50 > 100000.0 nM -
CHEMBL384364 IC50 > 100000.0 nM -
CHEMBL218358 IC50 > 100000.0 nM -
CHEMBL386029 IC50 > 20000.0 nM -
CHEMBL373889 IC50 > 10000.0 nM -
CHEMBL219142 IC50 > 100000.0 nM -
CHEMBL424937 IC50 > 100000.0 nM -
CHEMBL375156 IC50 > 100000.0 nM -
CHEMBL218758 IC50 > 100000.0 nM -
CHEMBL415429 IC50 > 100000.0 nM -
CHEMBL375341 IC50 > 100000.0 nM -