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Assay Detail

CHEMBL765836

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Binding
Binding affinity was determined against hPR-A (human progesterone receptor) using progesterone radioligand in competitive binding assay
29
Total Activities
29
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-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
Ki 29 8.17 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 9.47
CHEMBL286446 1 9.36
CHEMBL112987 1 9.06
CHEMBL325221 1 9.02
CHEMBL116007 1 8.96
CHEMBL114941 1 8.92
CHEMBL116221 1 8.82
CHEMBL114607 1 8.77
CHEMBL326092 1 8.54
CHEMBL332264 1 8.49
CHEMBL115174 1 8.48
CHEMBL103 PROGESTERONE 4.0 1 8.46
CHEMBL322108 1 8.46
CHEMBL64123 1 8.44
CHEMBL8639 1 8.32
CHEMBL113098 1 8.22
CHEMBL65079 1 8.21
CHEMBL325213 1 8.18
CHEMBL114553 1 7.79
CHEMBL1908373 ONAPRISTONE 2.0 1 7.75
CHEMBL115173 1 7.64
CHEMBL114611 1 7.61
CHEMBL321243 1 7.58
CHEMBL114435 1 7.42
CHEMBL294116 1 7.30
CHEMBL113099 1 7.19
CHEMBL333167 1 7.09
CHEMBL67362 1 7.08
CHEMBL112058 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE Ki = 0.34 nM 9.47
CHEMBL286446 Ki = 0.44 nM 9.36
CHEMBL112987 Ki = 0.87 nM 9.06
CHEMBL325221 Ki = 0.95 nM 9.02
CHEMBL116007 Ki = 1.1 nM 8.96
CHEMBL114941 Ki = 1.2 nM 8.92
CHEMBL116221 Ki = 1.5 nM 8.82
CHEMBL114607 Ki = 1.7 nM 8.77
CHEMBL326092 Ki = 2.9 nM 8.54
CHEMBL332264 Ki = 3.2 nM 8.49
CHEMBL115174 Ki = 3.3 nM 8.48
CHEMBL103 PROGESTERONE Ki = 3.5 nM 8.46
CHEMBL322108 Ki = 3.5 nM 8.46
CHEMBL64123 Ki = 3.6 nM 8.44
CHEMBL8639 Ki = 4.8 nM 8.32
CHEMBL113098 Ki = 6.0 nM 8.22
CHEMBL65079 Ki = 6.1 nM 8.21
CHEMBL325213 Ki = 6.6 nM 8.18
CHEMBL114553 Ki = 16.4 nM 7.79
CHEMBL1908373 ONAPRISTONE Ki = 18.0 nM 7.75
CHEMBL115173 Ki = 23.0 nM 7.64
CHEMBL114611 Ki = 24.3 nM 7.61
CHEMBL321243 Ki = 26.5 nM 7.58
CHEMBL114435 Ki = 38.4 nM 7.42
CHEMBL294116 Ki = 50.2 nM 7.30
CHEMBL113099 Ki = 64.0 nM 7.19
CHEMBL333167 Ki = 80.5 nM 7.09
CHEMBL67362 Ki = 84.0 nM 7.08
CHEMBL112058 Ki = 400.0 nM 6.40