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Assay Detail

CHEMBL860995

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Functional
Inhibition of ER beta-mediated transactivation of ERE in HeLa cell luciferase assay at 10 uM
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Expert

Target

Estrogen receptor beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators.
Güngör T, Chen Y, Golla R, Ma Z, Corte JR, Northrop JP, Bin B, Dickson JK, Stouch T, Zhou R, Johnson SE, Seethala R, Feyen JH.
J Med Chem (2006) 49 : 2440 -2455
PubMed 16610787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 5.69 9.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 9.23
CHEMBL1405 ESTRONE 4.0 1 6.78
CHEMBL207101 1 6.11
CHEMBL44 GENISTEIN 2.0 1 6.02
CHEMBL206349 1 6.01
CHEMBL202996 THIOGENISTEIN 1 5.95
CHEMBL377083 1 5.94
CHEMBL206131 1 5.85
CHEMBL205920 1 5.83
CHEMBL379889 1 5.78
CHEMBL206137 1 5.62
CHEMBL206336 1 5.62
CHEMBL208324 1 5.55
CHEMBL205398 1 5.54
CHEMBL206764 1 5.51
CHEMBL206648 1 5.50
CHEMBL382698 1 5.37
CHEMBL379252 1 5.34
CHEMBL203351 1 5.34
CHEMBL205249 1 5.33
CHEMBL203724 1 5.31
CHEMBL203330 1 5.29
CHEMBL203283 1 5.28
CHEMBL205395 1 5.08
CHEMBL206773 1 5.03
CHEMBL202894 1 5.03
CHEMBL381720 1 5.03
CHEMBL202738 1 5.00
CHEMBL382786 1 -
CHEMBL377293 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.59 nM 9.23
CHEMBL1405 ESTRONE EC50 = 166.0 nM 6.78
CHEMBL207101 EC50 = 776.0 nM 6.11
CHEMBL44 GENISTEIN EC50 = 956.0 nM 6.02
CHEMBL206349 EC50 = 983.0 nM 6.01
CHEMBL202996 THIOGENISTEIN EC50 = 1125.0 nM 5.95
CHEMBL377083 EC50 = 1143.0 nM 5.94
CHEMBL206131 EC50 = 1427.0 nM 5.85
CHEMBL205920 EC50 = 1462.0 nM 5.83
CHEMBL379889 EC50 = 1669.0 nM 5.78
CHEMBL206137 EC50 = 2406.0 nM 5.62
CHEMBL206336 EC50 = 2392.0 nM 5.62
CHEMBL208324 EC50 = 2793.0 nM 5.55
CHEMBL205398 EC50 = 2918.0 nM 5.54
CHEMBL206764 EC50 = 3112.0 nM 5.51
CHEMBL206648 EC50 = 3143.0 nM 5.50
CHEMBL382698 EC50 = 4261.0 nM 5.37
CHEMBL379252 EC50 = 4576.0 nM 5.34
CHEMBL203351 EC50 = 4521.0 nM 5.34
CHEMBL205249 EC50 = 4624.0 nM 5.33
CHEMBL203724 EC50 = 4859.0 nM 5.31
CHEMBL203330 EC50 = 5137.0 nM 5.29
CHEMBL203283 EC50 = 5305.0 nM 5.28
CHEMBL205395 EC50 = 8317.0 nM 5.08
CHEMBL206773 EC50 = 9268.0 nM 5.03
CHEMBL202894 EC50 = 9317.0 nM 5.03
CHEMBL381720 EC50 = 9344.0 nM 5.03
CHEMBL202738 EC50 = 10082.0 nM 5.00
CHEMBL382786 EC50 - -
CHEMBL377293 EC50 - -