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Assay Detail

CHEMBL765241

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

Binding
Effective concentration for half-maximal activation of human progesterone receptor expressed in CV-1 cells
9
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.
Edwards JP, Zhi L, Pooley CL, Tegley CM, West SJ, Wang MW, Gottardis MM, Pathirana C, Schrader WT, Jones TK.
J Med Chem (1998) 41 : 2779 -2785
PubMed 9667968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 8.18 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416411 3 8.89
CHEMBL103 PROGESTERONE 4.0 1 8.82
CHEMBL1160663 2 8.62
CHEMBL94749 1 8.57
CHEMBL104183 1 8.44
CHEMBL94753 1 8.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416411 EC50 = 1.3 nM 8.89
CHEMBL103 PROGESTERONE EC50 = 1.5 nM 8.82
CHEMBL1160663 EC50 = 2.4 nM 8.62
CHEMBL94749 EC50 = 2.7 nM 8.57
CHEMBL416411 EC50 = 2.8 nM 8.55
CHEMBL104183 EC50 = 3.6 nM 8.44
CHEMBL94753 EC50 = 9.4 nM 8.03
CHEMBL416411 EC50 = 135.0 nM 6.87
CHEMBL1160663 EC50 = 147.0 nM 6.83