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Assay Detail

CHEMBL673864

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Functional
Ability to activate estrogen receptor 2-mediated transcription.
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.
Yang W, Wang Y, Ma Z, Golla R, Stouch T, Seethala R, Johnson S, Zhou R, Güngör T, Feyen JH, Dickson JK.
Bioorg Med Chem Lett (2004) 14 : 2327 -2330
PubMed 15081034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 7.32 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 9.17
CHEMBL74758 1 8.15
CHEMBL77609 1 8.10
CHEMBL77620 1 7.80
CHEMBL306636 1 7.75
CHEMBL77930 1 7.58
CHEMBL74757 1 7.52
CHEMBL264862 3 7.33
CHEMBL73989 1 7.11
CHEMBL74027 1 6.92
CHEMBL1405 ESTRONE 4.0 1 6.92
CHEMBL307205 1 6.85
CHEMBL77794 1 6.80
CHEMBL77466 1 6.75
CHEMBL44 GENISTEIN 2.0 1 6.70
CHEMBL77851 1 6.62
CHEMBL74022 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.67 nM 9.17
CHEMBL74758 EC50 = 7.0 nM 8.15
CHEMBL77609 EC50 = 8.0 nM 8.10
CHEMBL77620 EC50 = 16.0 nM 7.80
CHEMBL306636 EC50 = 18.0 nM 7.75
CHEMBL77930 EC50 = 26.0 nM 7.58
CHEMBL74757 EC50 = 30.0 nM 7.52
CHEMBL264862 EC50 = 47.0 nM 7.33
CHEMBL264862 EC50 = 50.0 nM 7.30
CHEMBL264862 EC50 = 74.0 nM 7.13
CHEMBL73989 EC50 = 77.0 nM 7.11
CHEMBL74027 EC50 = 120.0 nM 6.92
CHEMBL1405 ESTRONE EC50 = 120.0 nM 6.92
CHEMBL307205 EC50 = 140.0 nM 6.85
CHEMBL77794 EC50 = 160.0 nM 6.80
CHEMBL77466 EC50 = 180.0 nM 6.75
CHEMBL44 GENISTEIN EC50 = 200.0 nM 6.70
CHEMBL77851 EC50 = 240.0 nM 6.62
CHEMBL74022 EC50 = 270.0 nM 6.57