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Assay Detail

CHEMBL2396178

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Binding
Inhibition of rat 11beta-HSD1
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension.
Bauman DR, Whitehead A, Contino LC, Cui J, Garcia-Calvo M, Gu X, Kevin N, Ma X, Pai LY, Shah K, Shen X, Stribling S, Zokian HJ, Metzger J, Shevell DE, Waddell ST.
Bioorg Med Chem Lett (2013) 23 : 3650 -3653
PubMed 23659858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.33 8.89
IC50 4 8.28 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373257 2 8.89
CHEMBL1761313 2 8.41
CHEMBL2391969 2 8.35
CHEMBL1761321 2 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373257 Ki = 1.3 nM 8.89
CHEMBL373257 IC50 = 3.0 nM 8.52
CHEMBL1761313 Ki = 3.9 nM 8.41
CHEMBL2391969 IC50 = 4.5 nM 8.35
CHEMBL1761313 IC50 = 6.0 nM 8.22
CHEMBL2391969 Ki = 7.0 nM 8.15
CHEMBL1761321 IC50 = 9.1 nM 8.04
CHEMBL1761321 Ki = 13.1 nM 7.88