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Assay Detail

CHEMBL682298

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Binding
Binding affinity for estrogen receptor alpha
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).
Wallace OB, Lauwers KS, Jones SA, Dodge JA.
Bioorg Med Chem Lett (2003) 13 : 1907 -1910
PubMed 12749895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.29 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81 RALOXIFENE 4.0 1 9.40
CHEMBL2137046 1 9.30
CHEMBL58688 1 9.22
CHEMBL56198 1 9.22
CHEMBL56390 1 9.05
CHEMBL56306 1 8.96
CHEMBL60538 1 8.77
CHEMBL293297 1 8.60
CHEMBL59146 1 7.54
CHEMBL59311 1 7.43
CHEMBL56166 1 7.06
CHEMBL293599 1 6.77
CHEMBL59438 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81 RALOXIFENE Ki = 0.4 nM 9.40
CHEMBL2137046 Ki = 0.5 nM 9.30
CHEMBL58688 Ki = 0.6 nM 9.22
CHEMBL56198 Ki = 0.6 nM 9.22
CHEMBL56390 Ki = 0.9 nM 9.05
CHEMBL56306 Ki = 1.1 nM 8.96
CHEMBL60538 Ki = 1.7 nM 8.77
CHEMBL293297 Ki = 2.5 nM 8.60
CHEMBL59146 Ki = 29.0 nM 7.54
CHEMBL59311 Ki = 37.0 nM 7.43
CHEMBL56166 Ki = 88.0 nM 7.06
CHEMBL293599 Ki = 170.0 nM 6.77
CHEMBL59438 Ki = 310.0 nM 6.51