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Assay Detail

CHEMBL760815

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

Functional
Antagonist activity against hPR (human progesterone receptor) compared to that of progesterone (100%)
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.
Zhi L, Tegley CM, Edwards JP, West SJ, Marschke KB, Gottardis MM, Mais DE, Jones TK.
Bioorg Med Chem Lett (1998) 8 : 3365 -3370
PubMed 9873735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 6.91 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1908373 ONAPRISTONE 2.0 1 8.80
CHEMBL65079 1 7.58
CHEMBL115174 1 7.37
CHEMBL64123 1 7.35
CHEMBL114435 1 7.34
CHEMBL333167 1 7.31
CHEMBL114553 1 7.24
CHEMBL113099 1 7.16
CHEMBL67362 1 7.15
CHEMBL294116 1 7.12
CHEMBL112058 1 7.12
CHEMBL114611 1 6.73
CHEMBL114607 1 6.51
CHEMBL325213 1 6.46
CHEMBL115173 1 6.43
CHEMBL321243 1 6.27
CHEMBL8639 1 6.25
CHEMBL325221 1 6.00
CHEMBL332264 1 5.17
CHEMBL286446 1 -
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 -
CHEMBL116221 1 -
CHEMBL116007 1 -
CHEMBL112987 1 -
CHEMBL103 PROGESTERONE 4.0 1 -
CHEMBL326092 1 -
CHEMBL322108 1 -
CHEMBL114941 1 -
CHEMBL113098 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1908373 ONAPRISTONE EC50 = 1.6 nM 8.80
CHEMBL65079 EC50 = 26.0 nM 7.58
CHEMBL115174 EC50 = 43.0 nM 7.37
CHEMBL64123 EC50 = 45.0 nM 7.35
CHEMBL114435 EC50 = 46.0 nM 7.34
CHEMBL333167 EC50 = 49.0 nM 7.31
CHEMBL114553 EC50 = 57.0 nM 7.24
CHEMBL113099 EC50 = 69.0 nM 7.16
CHEMBL67362 EC50 = 71.0 nM 7.15
CHEMBL294116 EC50 = 75.0 nM 7.12
CHEMBL112058 EC50 = 75.0 nM 7.12
CHEMBL114611 EC50 = 187.0 nM 6.73
CHEMBL114607 EC50 = 307.0 nM 6.51
CHEMBL325213 EC50 = 345.0 nM 6.46
CHEMBL115173 EC50 = 375.0 nM 6.43
CHEMBL321243 EC50 = 538.0 nM 6.27
CHEMBL8639 EC50 = 561.0 nM 6.25
CHEMBL325221 EC50 = 997.0 nM 6.00
CHEMBL332264 EC50 = 6700.0 nM 5.17
CHEMBL286446 EC50 > 10000.0 nM -
CHEMBL717 MEDROXYPROGESTERONE ACETATE EC50 > 10000.0 nM -
CHEMBL116221 EC50 > 10000.0 nM -
CHEMBL116007 EC50 > 10000.0 nM -
CHEMBL112987 EC50 > 10000.0 nM -
CHEMBL103 PROGESTERONE EC50 > 10000.0 nM -
CHEMBL326092 EC50 > 10000.0 nM -
CHEMBL322108 EC50 > 10000.0 nM -
CHEMBL114941 EC50 > 10000.0 nM -
CHEMBL113098 EC50 > 10000.0 nM -