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Assay Detail

CHEMBL899210

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

Functional
Antiinflammatory activity assessed as upregulation of aromatase in HFF cells by transactivation assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HFF
Confidence 1 — Organism
Curated By Autocuration

Target

HFF (CHEMBL614071)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of dissociated non-steroidal glucocorticoid receptor agonists.
Kuzmich D, Kirrane T, Proudfoot J, Bekkali Y, Zindell R, Beck L, Nelson R, Shih CK, Kukulka AJ, Paw Z, Reilly P, Deleon R, Cardozo M, Nabozny G, Thomson D.
Bioorg Med Chem Lett (2007) 17 : 5025 -5031
PubMed 17692519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.91 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384467 DEXAMETHASONE 4.0 1 8.70
CHEMBL236755 1 8.10
CHEMBL235063 1 7.52
CHEMBL392499 1 6.61
CHEMBL392501 1 6.60
CHEMBL392500 1 6.58
CHEMBL393392 1 6.54
CHEMBL400609 1 6.18
CHEMBL235689 1 5.32
CHEMBL235280 1 -
CHEMBL263091 1 -
CHEMBL429987 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384467 DEXAMETHASONE EC50 = 2.0 nM 8.70
CHEMBL236755 EC50 = 8.0 nM 8.10
CHEMBL235063 EC50 = 30.0 nM 7.52
CHEMBL392499 EC50 = 245.0 nM 6.61
CHEMBL392501 EC50 = 250.0 nM 6.60
CHEMBL392500 EC50 = 260.0 nM 6.58
CHEMBL393392 EC50 = 285.0 nM 6.54
CHEMBL400609 EC50 = 660.0 nM 6.18
CHEMBL235689 EC50 = 4750.0 nM 5.32
CHEMBL235280 EC50 - -
CHEMBL263091 EC50 > 2000.0 nM -
CHEMBL429987 EC50 > 2000.0 nM -