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Assay Detail

CHEMBL681747

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

Binding
Displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
Morgan BP, Swick AG, Hargrove DM, LaFlamme JA, Moynihan MS, Carroll RS, Martin KA, Lee E, Decosta D, Bordner J.
J Med Chem (2002) 45 : 2417 -2424
PubMed 12036351 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.11 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77779 1 10.00
CHEMBL78704 1 10.00
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.62
CHEMBL78646 1 6.80
CHEMBL82307 1 -
CHEMBL78807 1 -
CHEMBL310370 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77779 Ki = 0.1 nM 10.00
CHEMBL78704 Ki = 0.1 nM 10.00
CHEMBL1276308 MIFEPRISTONE Ki = 0.24 nM 9.62
CHEMBL78646 Ki = 157.0 nM 6.80
CHEMBL82307 Ki > 10000.0 nM -
CHEMBL78807 Ki > 10000.0 nM -
CHEMBL310370 Ki > 10000.0 nM -