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Assay Detail

CHEMBL877124

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

Binding
Binding potency for human ER beta
17
Total Activities
17
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 beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.
Blizzard TA, DiNinno F, Morgan JD, Wu JY, Chen HY, Kim S, Chan W, Birzin ET, Yang YT, Pai LY, Zhang Z, Hayes EC, DaSilva CA, Tang W, Rohrer SP, Schaeffer JM, Hammond ML.
Bioorg Med Chem Lett (2004) 14 : 3865 -3868
PubMed 15225686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.99 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 8.96
CHEMBL81 RALOXIFENE 4.0 1 7.92
CHEMBL304552 1 7.35
CHEMBL184679 1 7.23
CHEMBL362623 1 7.19
CHEMBL362718 1 7.14
CHEMBL359774 1 7.09
CHEMBL185114 1 7.09
CHEMBL183084 1 6.94
CHEMBL360802 1 6.87
CHEMBL185383 1 6.61
CHEMBL185480 1 6.57
CHEMBL435696 1 6.56
CHEMBL184372 1 6.48
CHEMBL184491 1 6.44
CHEMBL184431 1 6.36
CHEMBL365484 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 1.1 nM 8.96
CHEMBL81 RALOXIFENE IC50 = 12.0 nM 7.92
CHEMBL304552 IC50 = 45.0 nM 7.35
CHEMBL184679 IC50 = 59.0 nM 7.23
CHEMBL362623 IC50 = 64.0 nM 7.19
CHEMBL362718 IC50 = 72.0 nM 7.14
CHEMBL359774 IC50 = 81.0 nM 7.09
CHEMBL185114 IC50 = 81.0 nM 7.09
CHEMBL183084 IC50 = 116.0 nM 6.94
CHEMBL360802 IC50 = 134.0 nM 6.87
CHEMBL185383 IC50 = 247.0 nM 6.61
CHEMBL185480 IC50 = 267.0 nM 6.57
CHEMBL435696 IC50 = 275.0 nM 6.56
CHEMBL184372 IC50 = 331.0 nM 6.48
CHEMBL184491 IC50 = 366.0 nM 6.44
CHEMBL184431 IC50 = 436.0 nM 6.36
CHEMBL365484 IC50 = 1113.0 nM 5.95