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Assay Detail

CHEMBL766185

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

Binding
Binding affinity against human progesterone receptor-A (hPR-A)
42
Total Activities
42
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

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
Ki 42 7.35 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 8.96
CHEMBL433403 1 8.82
CHEMBL330527 1 8.72
CHEMBL93690 1 8.64
CHEMBL327847 1 8.51
CHEMBL92750 1 8.46
CHEMBL328506 1 8.44
CHEMBL313418 1 7.95
CHEMBL92089 1 7.91
CHEMBL92730 1 7.89
CHEMBL329198 1 7.85
CHEMBL91927 1 7.81
CHEMBL431280 1 7.68
CHEMBL446418 1 7.62
CHEMBL316348 1 7.59
CHEMBL328523 1 7.54
CHEMBL90766 1 7.54
CHEMBL330702 1 7.28
CHEMBL330235 1 7.24
CHEMBL327934 1 7.20
CHEMBL330726 1 7.11
CHEMBL327551 1 7.11
CHEMBL93894 1 7.06
CHEMBL328804 1 7.01
CHEMBL93451 1 7.00
CHEMBL329339 1 6.95
CHEMBL93463 1 6.88
CHEMBL91858 1 6.77
CHEMBL93345 1 6.75
CHEMBL328058 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE Ki = 1.1 nM 8.96
CHEMBL433403 Ki = 1.5 nM 8.82
CHEMBL330527 Ki = 1.9 nM 8.72
CHEMBL93690 Ki = 2.3 nM 8.64
CHEMBL327847 Ki = 3.1 nM 8.51
CHEMBL92750 Ki = 3.5 nM 8.46
CHEMBL328506 Ki = 3.6 nM 8.44
CHEMBL313418 Ki = 11.2 nM 7.95
CHEMBL92089 Ki = 12.4 nM 7.91
CHEMBL92730 Ki = 13.0 nM 7.89
CHEMBL329198 Ki = 14.0 nM 7.85
CHEMBL91927 Ki = 15.5 nM 7.81
CHEMBL431280 Ki = 20.9 nM 7.68
CHEMBL446418 Ki = 24.0 nM 7.62
CHEMBL316348 Ki = 25.5 nM 7.59
CHEMBL328523 Ki = 29.0 nM 7.54
CHEMBL90766 Ki = 29.1 nM 7.54
CHEMBL330702 Ki = 53.1 nM 7.28
CHEMBL330235 Ki = 57.0 nM 7.24
CHEMBL327934 Ki = 62.5 nM 7.20
CHEMBL327551 Ki = 77.0 nM 7.11
CHEMBL330726 Ki = 77.0 nM 7.11
CHEMBL93894 Ki = 87.0 nM 7.06
CHEMBL328804 Ki = 97.0 nM 7.01
CHEMBL93451 Ki = 101.0 nM 7.00
CHEMBL329339 Ki = 113.0 nM 6.95
CHEMBL93463 Ki = 133.0 nM 6.88
CHEMBL91858 Ki = 169.0 nM 6.77
CHEMBL93345 Ki = 176.0 nM 6.75
CHEMBL328058 Ki = 184.0 nM 6.74
CHEMBL328787 Ki = 202.0 nM 6.70
CHEMBL446160 Ki = 200.0 nM 6.70
CHEMBL328261 Ki = 449.0 nM 6.35
CHEMBL93407 Ki = 483.0 nM 6.32
CHEMBL91708 Ki = 1858.0 nM 5.73
CHEMBL92777 Ki = 2580.0 nM 5.59
CHEMBL94286 Ki = 3553.0 nM 5.45
CHEMBL93474 Ki > 10000.0 nM -
CHEMBL94183 Ki > 1000.0 nM -
CHEMBL91227 Ki > 10000.0 nM -
CHEMBL327918 Ki > 10000.0 nM -
CHEMBL328669 Ki > 10000.0 nM -