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Assay Detail

CHEMBL681750

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

Binding
Displacement of Dexamethasone from human glucocorticoid receptor
12
Total Activities
12
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

5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.
Zhi L, Tegley CM, Edwards JP, West SJ, Marschke KB, Gottardis MM, Mais DE, Jones TK.
Bioorg Med Chem Lett (1998) 8 : 3365 -3370
PubMed 9873735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.70 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
CHEMBL114941 1 7.29
CHEMBL322108 1 6.89
CHEMBL114607 1 6.80
CHEMBL116221 1 6.58
CHEMBL286446 1 6.43
CHEMBL112987 1 6.41
CHEMBL326092 1 6.27
CHEMBL116007 1 6.13
CHEMBL325221 1 6.09
CHEMBL8639 1 6.05

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
CHEMBL114941 Ki = 51.0 nM 7.29
CHEMBL322108 Ki = 130.0 nM 6.89
CHEMBL114607 Ki = 158.0 nM 6.80
CHEMBL116221 Ki = 260.0 nM 6.58
CHEMBL286446 Ki = 367.0 nM 6.43
CHEMBL112987 Ki = 394.0 nM 6.41
CHEMBL326092 Ki = 533.0 nM 6.27
CHEMBL116007 Ki = 749.0 nM 6.13
CHEMBL325221 Ki = 813.0 nM 6.09
CHEMBL8639 Ki = 889.0 nM 6.05