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Assay Detail

CHEMBL680189

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

Binding
Binding affinity against baculovirus expressed human glucocorticoid receptor (hGR)
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification.
Zhi L, Tegley CM, Marschke KB, Mais DE, Jones TK.
J Med Chem (1999) 42 : 1466 -1472
PubMed 10212133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.50 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
CHEMBL36564 1 6.71
CHEMBL286158 1 6.60
CHEMBL284475 1 6.60
CHEMBL36065 1 6.59
CHEMBL35429 1 6.48
CHEMBL32603 1 6.17
CHEMBL35525 1 6.06
CHEMBL34015 1 6.04
CHEMBL285705 1 6.04
CHEMBL34824 1 5.33

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
CHEMBL36564 Ki = 193.0 nM 6.71
CHEMBL286158 Ki = 250.0 nM 6.60
CHEMBL284475 Ki = 249.0 nM 6.60
CHEMBL36065 Ki = 257.0 nM 6.59
CHEMBL35429 Ki = 331.0 nM 6.48
CHEMBL32603 Ki = 680.0 nM 6.17
CHEMBL35525 Ki = 864.0 nM 6.06
CHEMBL34015 Ki = 913.0 nM 6.04
CHEMBL285705 Ki = 909.0 nM 6.04
CHEMBL34824 Ki = 4728.0 nM 5.33