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Assay Detail

CHEMBL765831

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

Functional
Antagonist activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.
Hamann LG, Winn DT, Pooley CL, Tegley CM, West SJ, Farmer LJ, Zhi L, Edwards JP, Marschke KB, Mais DE, Goldman ME, Jones TK.
Bioorg Med Chem Lett (1998) 8 : 2731 -2736
PubMed 9873612 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.37 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.52
CHEMBL92750 1 8.00
CHEMBL327934 1 7.34
CHEMBL329339 1 7.23
CHEMBL328787 1 7.13
CHEMBL316348 1 7.10
CHEMBL328506 1 7.05
CHEMBL328261 1 7.00
CHEMBL330527 1 7.00
CHEMBL93451 1 6.91
CHEMBL327847 1 6.84
CHEMBL313418 1 6.84
CHEMBL90766 1 6.80
CHEMBL93345 1 6.79
CHEMBL330702 1 6.79
CHEMBL329198 1 6.66
CHEMBL328523 1 6.61
CHEMBL91858 1 6.55
CHEMBL94286 1 6.45
CHEMBL91227 1 6.44
CHEMBL330726 1 6.38
CHEMBL93894 1 6.37
CHEMBL446418 1 6.36
CHEMBL91927 1 6.30
CHEMBL92730 1 6.26
CHEMBL93407 1 6.21
CHEMBL94183 1 6.18
CHEMBL93463 1 6.11
CHEMBL327551 1 5.94
CHEMBL330235 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.3 nM 9.52
CHEMBL92750 IC50 = 10.0 nM 8.00
CHEMBL327934 IC50 = 46.0 nM 7.34
CHEMBL329339 IC50 = 59.0 nM 7.23
CHEMBL328787 IC50 = 74.0 nM 7.13
CHEMBL316348 IC50 = 80.0 nM 7.10
CHEMBL328506 IC50 = 90.0 nM 7.05
CHEMBL328261 IC50 = 99.0 nM 7.00
CHEMBL330527 IC50 = 100.0 nM 7.00
CHEMBL93451 IC50 = 122.0 nM 6.91
CHEMBL313418 IC50 = 146.0 nM 6.84
CHEMBL327847 IC50 = 146.0 nM 6.84
CHEMBL90766 IC50 = 158.0 nM 6.80
CHEMBL93345 IC50 = 164.0 nM 6.79
CHEMBL330702 IC50 = 163.0 nM 6.79
CHEMBL329198 IC50 = 220.0 nM 6.66
CHEMBL328523 IC50 = 248.0 nM 6.61
CHEMBL91858 IC50 = 284.0 nM 6.55
CHEMBL94286 IC50 = 353.0 nM 6.45
CHEMBL91227 IC50 = 365.0 nM 6.44
CHEMBL330726 IC50 = 416.0 nM 6.38
CHEMBL93894 IC50 = 424.0 nM 6.37
CHEMBL446418 IC50 = 434.0 nM 6.36
CHEMBL91927 IC50 = 496.0 nM 6.30
CHEMBL92730 IC50 = 549.0 nM 6.26
CHEMBL93407 IC50 = 609.0 nM 6.21
CHEMBL94183 IC50 = 662.0 nM 6.18
CHEMBL93463 IC50 = 783.0 nM 6.11
CHEMBL327551 IC50 = 1144.0 nM 5.94
CHEMBL330235 IC50 = 1674.0 nM 5.78
CHEMBL93690 IC50 = 1772.0 nM 5.75
CHEMBL328058 IC50 = 1847.0 nM 5.73
CHEMBL446160 IC50 = 2330.0 nM 5.63
CHEMBL328804 IC50 = 3331.0 nM 5.48
CHEMBL91708 IC50 = 3443.0 nM 5.46
CHEMBL431280 IC50 = 5685.0 nM 5.25
CHEMBL327918 IC50 = 10000.0 nM 5.00
CHEMBL92089 IC50 = 10000.0 nM 5.00
CHEMBL93474 IC50 = 10000.0 nM 5.00
CHEMBL92777 IC50 = 10000.0 nM 5.00
CHEMBL328669 IC50 = 10000.0 nM 5.00