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Assay Detail

CHEMBL4189817

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

Binding
Induction of nuclear translocation of human recombinant ProLabel-tagged mineralocorticoid receptor expressed in CHO-K1 cells after 3 hrs by luminescence method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
Ghidini E, Marchini G, Capelli AM, Carnini C, Cenacchi V, Fioni A, Facchinetti F, Rancati F.
J Med Chem (2018) 61 : 4757 -4773
PubMed 29741897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.55 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217175 1 8.80
CHEMBL4204230 1 8.60
CHEMBL4211724 1 8.49
CHEMBL1370 BUDESONIDE 4.0 1 8.32
CHEMBL1676 FLUTICASONE FUROATE 4.0 1 -
CHEMBL4217942 1 -
CHEMBL4213791 1 -
CHEMBL4214377 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217175 EC50 = 1.6 nM 8.80
CHEMBL4204230 EC50 = 2.5 nM 8.60
CHEMBL4211724 EC50 = 3.2 nM 8.49
CHEMBL1370 BUDESONIDE EC50 = 4.8 nM 8.32
CHEMBL1676 FLUTICASONE FUROATE EC50 > 3000.0 nM -
CHEMBL4217942 EC50 > 3000.0 nM -
CHEMBL4213791 EC50 > 3000.0 nM -
CHEMBL4214377 EC50 > 3000.0 nM -