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Assay Detail

CHEMBL677053

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

Binding
Ability to displace [3H]17-beta-estradiol from Estrogen receptor beta by scintillation proximity assay.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.
Henke BR, Drewry DH, Jones SA, Stewart EL, Weaver SL, Wiethe RW.
Bioorg Med Chem Lett (2001) 11 : 1939 -1942
PubMed 11459665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.42 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 8.46
CHEMBL81 RALOXIFENE 4.0 1 8.00
CHEMBL58714 1 6.96
CHEMBL58330 1 6.60
CHEMBL57093 1 6.48
CHEMBL58486 1 6.18
CHEMBL58563 1 6.17
CHEMBL292573 1 6.15
CHEMBL58504 1 6.10
CHEMBL61026 1 6.00
CHEMBL57875 1 5.98
CHEMBL294710 1 5.96
CHEMBL59184 1 5.95
CHEMBL60909 1 5.93
CHEMBL59552 1 5.90
CHEMBL58449 1 5.85
CHEMBL59271 1 -
CHEMBL58741 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL Ki = 3.5 nM 8.46
CHEMBL81 RALOXIFENE Ki = 10.0 nM 8.00
CHEMBL58714 Ki = 110.0 nM 6.96
CHEMBL58330 Ki = 250.0 nM 6.60
CHEMBL57093 Ki = 330.0 nM 6.48
CHEMBL58486 Ki = 660.0 nM 6.18
CHEMBL58563 Ki = 680.0 nM 6.17
CHEMBL292573 Ki = 710.0 nM 6.15
CHEMBL58504 Ki = 790.0 nM 6.10
CHEMBL61026 Ki = 1000.0 nM 6.00
CHEMBL57875 Ki = 1050.0 nM 5.98
CHEMBL294710 Ki = 1100.0 nM 5.96
CHEMBL59184 Ki = 1120.0 nM 5.95
CHEMBL60909 Ki = 1170.0 nM 5.93
CHEMBL59552 Ki = 1260.0 nM 5.90
CHEMBL58449 Ki = 1410.0 nM 5.85
CHEMBL59271 Ki > 3000.0 nM -
CHEMBL58741 Ki > 3000.0 nM -