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Assay Detail

CHEMBL909896

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

Binding
Inhibition of mouse 11beta-HSD1 expressed in Escherichia coli by SPA
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

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 23 7.32 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL375341 1 8.70
CHEMBL425104 2 8.30
CHEMBL374728 1 8.30
CHEMBL217917 1 8.15
CHEMBL424937 1 8.10
CHEMBL415429 1 8.05
CHEMBL375156 1 7.82
CHEMBL218144 1 7.75
CHEMBL218093 1 7.68
CHEMBL218758 1 7.62
CHEMBL218197 1 7.48
CHEMBL219142 1 7.47
CHEMBL218142 1 7.29
CHEMBL384364 1 7.28
CHEMBL218143 1 6.96
CHEMBL218358 1 6.96
CHEMBL386029 1 6.92
CHEMBL219443 1 6.75
CHEMBL373889 1 6.52
CHEMBL374922 1 6.33
CHEMBL219494 1 6.04
CHEMBL218096 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL375341 Ki = 2.0 nM 8.70
CHEMBL425104 Ki = 5.0 nM 8.30
CHEMBL374728 Ki = 5.0 nM 8.30
CHEMBL217917 Ki = 7.0 nM 8.15
CHEMBL424937 Ki = 8.0 nM 8.10
CHEMBL415429 Ki = 9.0 nM 8.05
CHEMBL375156 Ki = 15.0 nM 7.82
CHEMBL218144 Ki = 18.0 nM 7.75
CHEMBL218093 Ki = 21.0 nM 7.68
CHEMBL218758 Ki = 24.0 nM 7.62
CHEMBL218197 Ki = 33.0 nM 7.48
CHEMBL219142 Ki = 34.0 nM 7.47
CHEMBL218142 Ki = 51.0 nM 7.29
CHEMBL384364 Ki = 53.0 nM 7.28
CHEMBL218358 Ki = 110.0 nM 6.96
CHEMBL218143 Ki = 110.0 nM 6.96
CHEMBL386029 Ki = 120.0 nM 6.92
CHEMBL219443 Ki = 180.0 nM 6.75
CHEMBL425104 Ki = 260.0 nM 6.58
CHEMBL373889 Ki = 300.0 nM 6.52
CHEMBL374922 Ki = 470.0 nM 6.33
CHEMBL219494 Ki = 910.0 nM 6.04
CHEMBL218096 Ki = 4100.0 nM 5.39