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Assay Detail

CHEMBL1838801

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Functional
Agonist activity at GR in human SW1353 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SW1353
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma.
Millan DS, Ballard SA, Chunn S, Dybowski JA, Fulton CK, Glossop PA, Guillabert E, Hewson CA, Jones RM, Lamb DJ, Napier CM, Payne-Cook TA, Renery ER, Selby MD, Tutt MF, Yeadon M.
Bioorg Med Chem Lett (2011) 21 : 5826 -5830
PubMed 21880489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 8.67 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1834538 1 9.42
CHEMBL1834534 1 9.37
CHEMBL1676 FLUTICASONE FUROATE 4.0 1 9.31
CHEMBL1834536 1 9.15
CHEMBL1834533 1 9.11
CHEMBL1473 FLUTICASONE PROPIONATE 4.0 1 8.96
CHEMBL1834541 1 8.76
CHEMBL1834542 1 8.73
CHEMBL1834543 1 8.55
CHEMBL1834544 1 8.53
CHEMBL1834537 1 8.41
CHEMBL1834540 1 8.13
CHEMBL1834535 1 8.06
CHEMBL1370 BUDESONIDE 4.0 1 7.91
CHEMBL3142314 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1834538 EC50 = 0.38 nM 9.42
CHEMBL1834534 EC50 = 0.43 nM 9.37
CHEMBL1676 FLUTICASONE FUROATE EC50 = 0.49 nM 9.31
CHEMBL1834536 EC50 = 0.71 nM 9.15
CHEMBL1834533 EC50 = 0.78 nM 9.11
CHEMBL1473 FLUTICASONE PROPIONATE EC50 = 1.09 nM 8.96
CHEMBL1834541 EC50 = 1.75 nM 8.76
CHEMBL1834542 EC50 = 1.87 nM 8.73
CHEMBL1834543 EC50 = 2.82 nM 8.55
CHEMBL1834544 EC50 = 2.97 nM 8.53
CHEMBL1834537 EC50 = 3.93 nM 8.41
CHEMBL1834540 EC50 = 7.35 nM 8.13
CHEMBL1834535 EC50 = 8.78 nM 8.06
CHEMBL1370 BUDESONIDE EC50 = 12.4 nM 7.91
CHEMBL3142314 EC50 = 21.1 nM 7.68