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Assay Detail

CHEMBL680188

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

Binding
Binding affinity against human glucocorticoid receptor expressed in SF-12 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SF-12
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.
Tegley CM, Zhi L, Marschke KB, Gottardis MM, Yang Q, Jones TK.
J Med Chem (1998) 41 : 4354 -4359
PubMed 9784110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.90 7.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 7.88
CHEMBL103 PROGESTERONE 4.0 1 7.52
CHEMBL137103 1 6.76
CHEMBL32812 1 6.75
CHEMBL342426 1 6.62
CHEMBL134421 1 6.52
CHEMBL302362 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE Ki = 13.2 nM 7.88
CHEMBL103 PROGESTERONE Ki = 30.5 nM 7.52
CHEMBL137103 Ki = 173.0 nM 6.76
CHEMBL32812 Ki = 180.0 nM 6.75
CHEMBL342426 Ki = 237.0 nM 6.62
CHEMBL134421 Ki = 299.0 nM 6.52
CHEMBL302362 Ki = 564.0 nM 6.25