Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL902629

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

Binding
Binding affinity to human glucocorticoid receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
Bell MG, Gernert DL, Grese TA, Belvo MD, Borromeo PS, Kelley SA, Kennedy JH, Kolis SP, Lander PA, Richey R, Sharp VS, Stephenson GA, Williams JD, Yu H, Zimmerman KM, Steinberg MI, Jadhav PK.
J Med Chem (2007) 50 : 6443 -6445
PubMed 18038968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.90 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235206 1 8.05
CHEMBL1393 SPIRONOLACTONE 4.0 1 7.49
CHEMBL235209 1 6.78
CHEMBL391439 1 6.41
CHEMBL237122 EPIERENONE 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235206 Ki = 8.9 nM 8.05
CHEMBL1393 SPIRONOLACTONE Ki = 32.6 nM 7.49
CHEMBL235209 Ki = 167.0 nM 6.78
CHEMBL391439 Ki = 387.0 nM 6.41
CHEMBL237122 EPIERENONE Ki = 1758.0 nM 5.75