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Assay Detail

CHEMBL766187

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

Binding
Binding affinity towards human progesterone receptor A isoform using progesterone as radioligand
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.
Zhi L, Tegley CM, Pio B, Edwards JP, Motamedi M, Jones TK, Marschke KB, Mais DE, Risek B, Schrader WT.
J Med Chem (2003) 46 : 4104 -4112
PubMed 12954062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 8.67 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 9.47
CHEMBL132363 1 9.38
CHEMBL336736 1 9.26
CHEMBL422444 1 9.23
CHEMBL134602 1 9.21
CHEMBL413309 1 9.21
CHEMBL335249 1 9.21
CHEMBL302362 1 9.18
CHEMBL133117 1 9.15
CHEMBL336353 1 8.92
CHEMBL134277 1 8.89
CHEMBL130141 1 8.85
CHEMBL336751 1 8.82
CHEMBL337856 1 8.82
CHEMBL133483 1 8.80
CHEMBL132672 1 8.72
CHEMBL415524 1 8.64
CHEMBL422268 1 8.59
CHEMBL103 PROGESTERONE 4.0 1 8.46
CHEMBL335996 1 8.42
CHEMBL336169 1 8.33
CHEMBL130257 1 8.26
CHEMBL132578 1 8.19
CHEMBL335879 1 8.04
CHEMBL334747 1 7.94
CHEMBL334586 1 7.79
CHEMBL132256 1 7.65
CHEMBL133124 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE Ki = 0.34 nM 9.47
CHEMBL132363 Ki = 0.42 nM 9.38
CHEMBL336736 Ki = 0.55 nM 9.26
CHEMBL422444 Ki = 0.59 nM 9.23
CHEMBL134602 Ki = 0.62 nM 9.21
CHEMBL413309 Ki = 0.61 nM 9.21
CHEMBL335249 Ki = 0.62 nM 9.21
CHEMBL302362 Ki = 0.66 nM 9.18
CHEMBL133117 Ki = 0.71 nM 9.15
CHEMBL336353 Ki = 1.2 nM 8.92
CHEMBL134277 Ki = 1.3 nM 8.89
CHEMBL130141 Ki = 1.4 nM 8.85
CHEMBL336751 Ki = 1.5 nM 8.82
CHEMBL337856 Ki = 1.5 nM 8.82
CHEMBL133483 Ki = 1.6 nM 8.80
CHEMBL132672 Ki = 1.9 nM 8.72
CHEMBL415524 Ki = 2.3 nM 8.64
CHEMBL422268 Ki = 2.6 nM 8.59
CHEMBL103 PROGESTERONE Ki = 3.5 nM 8.46
CHEMBL335996 Ki = 3.8 nM 8.42
CHEMBL336169 Ki = 4.7 nM 8.33
CHEMBL130257 Ki = 5.5 nM 8.26
CHEMBL132578 Ki = 6.4 nM 8.19
CHEMBL335879 Ki = 9.2 nM 8.04
CHEMBL334747 Ki = 11.4 nM 7.94
CHEMBL334586 Ki = 16.4 nM 7.79
CHEMBL132256 Ki = 22.4 nM 7.65
CHEMBL133124 Ki = 45.5 nM 7.34