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Assay Detail

CHEMBL681739

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

Functional
Cross-reactivity as binding to human glucocorticoid receptor (hGR)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.
Zhi L, Tegley CM, Pio B, West SJ, Marschke KB, Mais DE, Jones TK.
Bioorg Med Chem Lett (2000) 10 : 415 -418
PubMed 10743938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.46 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1908373 ONAPRISTONE 2.0 1 7.57
CHEMBL132889 1 7.46
CHEMBL134260 1 6.95
CHEMBL131855 1 6.11
CHEMBL131681 1 6.05
CHEMBL335992 1 5.58
CHEMBL132193 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1908373 ONAPRISTONE IC50 = 27.0 nM 7.57
CHEMBL132889 IC50 = 35.0 nM 7.46
CHEMBL134260 IC50 = 113.0 nM 6.95
CHEMBL131855 IC50 = 780.0 nM 6.11
CHEMBL131681 IC50 = 900.0 nM 6.05
CHEMBL335992 IC50 = 2600.0 nM 5.58
CHEMBL132193 IC50 = 3200.0 nM 5.50