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Assay Detail

CHEMBL1919187

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

Binding
Transactivation activity at glucocorticoid receptor in rat H4II-E cells assessed as induction of tyrosine amino transferase
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type H4II-E
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucocorticoid receptor (CHEMBL3368)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.
Biju P, McCormick K, Aslanian R, Berlin M, Solomon D, Chapman R, McLeod R, Prelusky D, Eckel S, Kelly G, Natiello M, House A, Fernandez X, Bitar R, Phillips J, Anthes J.
Bioorg Med Chem Lett (2011) 21 : 6343 -6347
PubMed 21944381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.14 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1473 FLUTICASONE PROPIONATE 4.0 1 9.12
CHEMBL1917414 1 7.73
CHEMBL1917246 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1473 FLUTICASONE PROPIONATE EC50 = 0.76 nM 9.12
CHEMBL1917414 EC50 = 18.7 nM 7.73
CHEMBL1917246 EC50 = 27.0 nM 7.57