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Assay Detail

CHEMBL1105682

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

Binding
Inhibition of mouse 11-beta-HSD1
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.
Cheng H, Hoffman J, Le P, Nair SK, Cripps S, Matthews J, Smith C, Yang M, Kupchinsky S, Dress K, Edwards M, Cole B, Walters E, Loh C, Ermolieff J, Fanjul A, Bhat GB, Herrera J, Pauly T, Hosea N, Paderes G, Rejto P.
Bioorg Med Chem Lett (2010) 20 : 2897 -2902
PubMed 20363126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.99 9.00
Ki(app) 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1096870 1 9.00
CHEMBL1088117 1 9.00
CHEMBL1097177 1 8.46
CHEMBL1097827 1 8.44
CHEMBL1088116 1 8.27
CHEMBL1097828 1 8.20
CHEMBL1095033 1 8.03
CHEMBL1095786 1 7.80
CHEMBL1095787 1 7.77
CHEMBL1097178 1 7.45
CHEMBL1095785 1 7.40
CHEMBL1096451 1 7.32
CHEMBL1098159 1 6.77
CHEMBL1098130 1 -
CHEMBL1098131 1 -
CHEMBL1098145 1 -
CHEMBL1098160 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1096870 Ki = 1.0 nM 9.00
CHEMBL1088117 Ki = 1.0 nM 9.00
CHEMBL1097177 Ki = 3.5 nM 8.46
CHEMBL1097827 Ki = 3.6 nM 8.44
CHEMBL1088116 Ki = 5.4 nM 8.27
CHEMBL1097828 Ki = 6.3 nM 8.20
CHEMBL1095033 Ki = 9.4 nM 8.03
CHEMBL1095786 Ki = 16.0 nM 7.80
CHEMBL1095787 Ki = 17.0 nM 7.77
CHEMBL1097178 Ki = 35.2 nM 7.45
CHEMBL1095785 Ki = 40.0 nM 7.40
CHEMBL1096451 Ki = 48.0 nM 7.32
CHEMBL1098159 Ki = 170.0 nM 6.77
CHEMBL1098130 Ki(app) - -
CHEMBL1098131 Ki(app) - -
CHEMBL1098145 Ki(app) - -
CHEMBL1098160 Ki(app) - -