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Assay Detail

CHEMBL907397

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

Binding
Inhibition of mouse truncated 11beta-HSD1 assessed as inhibition of radiolabeled cortisone to cortisol conversion by SPA
19
Total Activities
19
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

Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction.
Sorensen B, Rohde J, Wang J, Fung S, Monzon K, Chiou W, Pan L, Deng X, Stolarik D, Frevert EU, Jacobson P, Link JT.
Bioorg Med Chem Lett (2006) 16 : 5958 -5962
PubMed 16996734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.21 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220102 1 8.70
CHEMBL222319 1 8.52
CHEMBL222511 1 8.52
CHEMBL220282 1 8.40
CHEMBL222618 1 8.30
CHEMBL222670 1 8.30
CHEMBL374110 1 7.82
CHEMBL223804 1 7.82
CHEMBL373792 1 7.58
CHEMBL221159 1 7.24
CHEMBL376695 1 6.75
CHEMBL223138 1 6.57
CHEMBL220883 1 6.30
CHEMBL222365 1 6.24
CHEMBL219712 1 6.24
CHEMBL220153 1 6.16
CHEMBL223083 1 5.92
CHEMBL376293 1 5.82
CHEMBL222669 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220102 Ki = 2.0 nM 8.70
CHEMBL222319 Ki = 3.0 nM 8.52
CHEMBL222511 Ki = 3.0 nM 8.52
CHEMBL220282 Ki = 4.0 nM 8.40
CHEMBL222618 Ki = 5.0 nM 8.30
CHEMBL222670 Ki = 5.0 nM 8.30
CHEMBL374110 Ki = 15.0 nM 7.82
CHEMBL223804 Ki = 15.0 nM 7.82
CHEMBL373792 Ki = 26.0 nM 7.58
CHEMBL221159 Ki = 58.0 nM 7.24
CHEMBL376695 Ki = 180.0 nM 6.75
CHEMBL223138 Ki = 270.0 nM 6.57
CHEMBL220883 Ki = 500.0 nM 6.30
CHEMBL222365 Ki = 580.0 nM 6.24
CHEMBL219712 Ki = 580.0 nM 6.24
CHEMBL220153 Ki = 700.0 nM 6.16
CHEMBL223083 Ki = 1200.0 nM 5.92
CHEMBL376293 Ki = 1500.0 nM 5.82
CHEMBL222669 Ki = 1700.0 nM 5.77