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Assay Detail

CHEMBL941997

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

Functional
Antagonist activity at human glucocorticoid receptor in SW1353 cells assessed as inhibition of dexamethasone-induced luciferase expression by MMTV5 reporter gene assay
19
Total Activities
19
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 Intermediate

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
Clark RD, Ray NC, Blaney P, Crackett PH, Hurley C, Williams K, Dyke HJ, Clark DE, Lockey PM, Devos R, Wong M, White A, Belanoff JK.
Bioorg Med Chem Lett (2007) 17 : 5704 -5708
PubMed 17822897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.08 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 8.92
CHEMBL78625 1 8.40
CHEMBL246834 1 6.75
CHEMBL250700 1 6.70
CHEMBL247632 1 6.70
CHEMBL247234 1 6.70
CHEMBL401013 1 6.64
CHEMBL248027 1 6.49
CHEMBL247006 1 6.40
CHEMBL246835 1 -
CHEMBL398668 1 -
CHEMBL247815 1 -
CHEMBL247638 1 -
CHEMBL400161 1 -
CHEMBL250288 1 -
CHEMBL247814 1 -
CHEMBL247812 1 -
CHEMBL247051 1 -
CHEMBL247634 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE Ki = 1.2 nM 8.92
CHEMBL78625 Ki = 4.0 nM 8.40
CHEMBL246834 Ki = 180.0 nM 6.75
CHEMBL250700 Ki = 200.0 nM 6.70
CHEMBL247632 Ki = 200.0 nM 6.70
CHEMBL247234 Ki = 200.0 nM 6.70
CHEMBL401013 Ki = 230.0 nM 6.64
CHEMBL248027 Ki = 323.0 nM 6.49
CHEMBL247006 Ki = 400.0 nM 6.40
CHEMBL246835 Ki > 1000.0 nM -
CHEMBL398668 Ki > 1000.0 nM -
CHEMBL247815 Ki > 1000.0 nM -
CHEMBL247638 Ki > 1000.0 nM -
CHEMBL400161 Ki > 1000.0 nM -
CHEMBL250288 Ki - -
CHEMBL247814 Ki - -
CHEMBL247812 Ki - -
CHEMBL247051 Ki > 1000.0 nM -
CHEMBL247634 Ki - -