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Assay Detail

CHEMBL863237

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

Binding
Inhibition of binding to recombinant human ERbeta by scintillation proximity assay
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 beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
Blizzard TA, Morgan JD, Chan W, Birzin ET, Pai LY, Hayes EC, DaSilva CA, Mosley RT, Yang YT, Rohrer SP, Dininno F, Hammond ML.
Bioorg Med Chem Lett (2005) 15 : 5124 -5128
PubMed 16203138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.18 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437695 1 9.22
CHEMBL197495 1 9.05
CHEMBL328190 LASOFOXIFENE 4.0 1 8.74
CHEMBL372808 1 8.64
CHEMBL198914 1 8.62
CHEMBL198803 1 8.59
CHEMBL372337 1 8.51
CHEMBL46740 BAZEDOXIFENE 4.0 1 8.42
CHEMBL81 RALOXIFENE 4.0 1 7.92
CHEMBL180300 1 7.35
CHEMBL182402 1 7.28
CHEMBL362623 1 7.19
CHEMBL183584 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437695 IC50 = 0.6 nM 9.22
CHEMBL197495 IC50 = 0.9 nM 9.05
CHEMBL328190 LASOFOXIFENE IC50 = 1.8 nM 8.74
CHEMBL372808 IC50 = 2.3 nM 8.64
CHEMBL198914 IC50 = 2.4 nM 8.62
CHEMBL198803 IC50 = 2.6 nM 8.59
CHEMBL372337 IC50 = 3.1 nM 8.51
CHEMBL46740 BAZEDOXIFENE IC50 = 3.8 nM 8.42
CHEMBL81 RALOXIFENE IC50 = 12.0 nM 7.92
CHEMBL180300 IC50 = 45.0 nM 7.35
CHEMBL182402 IC50 = 52.0 nM 7.28
CHEMBL362623 IC50 = 64.0 nM 7.19
CHEMBL183584 IC50 = 161.0 nM 6.79