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Assay Detail

CHEMBL4132701

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

Binding
Inhibition of human full-length 11beta-HSD2 expressed in HEK293 cells using cortisol as substrate after 2 hrs by LC-MS analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

11-beta-hydroxysteroid dehydrogenase type 2 (CHEMBL3746)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction.
Leiva R, Griñan-Ferré C, Seira C, Valverde E, McBride A, Binnie M, Pérez B, Luque FJ, Pallàs M, Bidon-Chanal A, Webster SP, Vázquez S.
Eur J Med Chem (2017) 139 : 412 -428
PubMed 28818766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.67 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4160328 1 7.00
CHEMBL4170932 1 7.00
CHEMBL4170544 1 6.00
CHEMBL4163698 1 -
CHEMBL4174368 1 -
CHEMBL4162610 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4160328 IC50 = 100.0 nM 7.00
CHEMBL4170932 IC50 = 100.0 nM 7.00
CHEMBL4170544 IC50 = 1000.0 nM 6.00
CHEMBL4163698 IC50 < 100.0 nM -
CHEMBL4174368 IC50 < 100.0 nM -
CHEMBL4162610 IC50 < 100.0 nM -