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Assay Detail

CHEMBL760108

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Functional
Agonistic activity by cotransfection assay against human Progesterone receptor in T47D cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type T47D
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
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
EC50 15 7.81 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 9.48
CHEMBL103 PROGESTERONE 4.0 1 8.74
CHEMBL286446 1 8.00
CHEMBL35429 1 7.96
CHEMBL36564 1 7.83
CHEMBL32603 1 7.74
CHEMBL34015 1 7.65
CHEMBL284475 1 7.63
CHEMBL34824 1 7.60
CHEMBL35525 1 7.58
CHEMBL416411 1 7.57
CHEMBL285705 1 7.46
CHEMBL36065 1 7.43
CHEMBL32812 1 7.29
CHEMBL286158 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE EC50 = 0.33 nM 9.48
CHEMBL103 PROGESTERONE EC50 = 1.8 nM 8.74
CHEMBL286446 EC50 = 10.0 nM 8.00
CHEMBL35429 EC50 = 10.9 nM 7.96
CHEMBL36564 EC50 = 14.8 nM 7.83
CHEMBL32603 EC50 = 18.3 nM 7.74
CHEMBL34015 EC50 = 22.6 nM 7.65
CHEMBL284475 EC50 = 23.5 nM 7.63
CHEMBL34824 EC50 = 25.0 nM 7.60
CHEMBL35525 EC50 = 26.0 nM 7.58
CHEMBL416411 EC50 = 27.0 nM 7.57
CHEMBL285705 EC50 = 35.0 nM 7.46
CHEMBL36065 EC50 = 37.0 nM 7.43
CHEMBL32812 EC50 = 51.0 nM 7.29
CHEMBL286158 EC50 = 63.0 nM 7.20