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Assay Detail

CHEMBL4189815

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

Binding
Induction of nuclear translocation of human recombinant ProLabel-tagged glucocorticoid receptor expressed in CHO-K1 cells after 3 hrs by luminescence method
31
Total Activities
31
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

Glucocorticoid receptor (CHEMBL2034)
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 31 8.05 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1676 FLUTICASONE FUROATE 4.0 1 9.40
CHEMBL4205561 1 8.89
CHEMBL4204358 1 8.89
CHEMBL4204087 1 8.77
CHEMBL4204230 1 8.74
CHEMBL4217175 1 8.68
CHEMBL4214152 1 8.49
CHEMBL4202463 1 8.47
CHEMBL4202533 1 8.47
CHEMBL1370 BUDESONIDE 4.0 1 8.46
CHEMBL4208840 1 8.34
CHEMBL4211724 1 8.28
CHEMBL4215262 1 8.24
CHEMBL4216231 1 8.24
CHEMBL4203139 1 8.13
CHEMBL4203448 1 8.11
CHEMBL4208957 1 8.08
CHEMBL4211166 1 8.07
CHEMBL4206713 1 7.95
CHEMBL4211798 1 7.82
CHEMBL4217173 1 7.68
CHEMBL4213765 1 7.51
CHEMBL4217942 1 7.39
CHEMBL4202674 1 7.36
CHEMBL4213791 1 7.35
CHEMBL4218553 1 7.30
CHEMBL4212517 1 7.26
CHEMBL4214377 1 7.24
CHEMBL4217464 1 7.19
CHEMBL4216014 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1676 FLUTICASONE FUROATE EC50 = 0.4 nM 9.40
CHEMBL4205561 EC50 = 1.3 nM 8.89
CHEMBL4204358 EC50 = 1.3 nM 8.89
CHEMBL4204087 EC50 = 1.7 nM 8.77
CHEMBL4204230 EC50 = 1.8 nM 8.74
CHEMBL4217175 EC50 = 2.1 nM 8.68
CHEMBL4214152 EC50 = 3.2 nM 8.49
CHEMBL4202463 EC50 = 3.4 nM 8.47
CHEMBL4202533 EC50 = 3.4 nM 8.47
CHEMBL1370 BUDESONIDE EC50 = 3.5 nM 8.46
CHEMBL4208840 EC50 = 4.6 nM 8.34
CHEMBL4211724 EC50 = 5.3 nM 8.28
CHEMBL4215262 EC50 = 5.7 nM 8.24
CHEMBL4216231 EC50 = 5.8 nM 8.24
CHEMBL4203139 EC50 = 7.4 nM 8.13
CHEMBL4203448 EC50 = 7.7 nM 8.11
CHEMBL4208957 EC50 = 8.4 nM 8.08
CHEMBL4211166 EC50 = 8.5 nM 8.07
CHEMBL4206713 EC50 = 11.3 nM 7.95
CHEMBL4211798 EC50 = 15.2 nM 7.82
CHEMBL4217173 EC50 = 20.8 nM 7.68
CHEMBL4213765 EC50 = 31.2 nM 7.51
CHEMBL4217942 EC50 = 40.3 nM 7.39
CHEMBL4202674 EC50 = 44.1 nM 7.36
CHEMBL4213791 EC50 = 45.0 nM 7.35
CHEMBL4218553 EC50 = 50.0 nM 7.30
CHEMBL4212517 EC50 = 54.9 nM 7.26
CHEMBL4214377 EC50 = 57.0 nM 7.24
CHEMBL4217464 EC50 = 63.9 nM 7.19
CHEMBL4216014 EC50 = 248.0 nM 6.61
CHEMBL4210515 EC50 - -