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Assay Detail

CHEMBL909359

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Binding
Inhibitory activity against rat 11beta-HSD1
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL2391)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 5 8.06 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL375341 1 8.52
CHEMBL375156 1 8.40
CHEMBL219142 1 8.22
CHEMBL374728 1 7.89
CHEMBL217917 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL375341 Ki = 3.0 nM 8.52
CHEMBL375156 Ki = 4.0 nM 8.40
CHEMBL219142 Ki = 6.0 nM 8.22
CHEMBL374728 Ki = 13.0 nM 7.89
CHEMBL217917 Ki = 52.0 nM 7.28