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Assay Detail

CHEMBL5054551

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

Binding
Displacement of fluorescent labeled-ligand from ERalpha (unknown origin) by competitive binding assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Searching for an ideal SERM: Mining tamoxifen structure-activity relationships.
Price S, Bender SG, Yahn R, Till NA, Varady S, LaLonde RL.
Bioorg Med Chem Lett (2021) 52 : 128383 -128383
PubMed 34592434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.20 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489 AFIMOXIFENE 3.0 1 8.12
CHEMBL5078348 1 8.06
CHEMBL5081507 1 7.97
CHEMBL5088475 1 7.82
CHEMBL5083906 1 7.79
CHEMBL5078187 1 7.68
CHEMBL5084400 1 7.61
CHEMBL5077058 1 7.45
CHEMBL5094047 1 7.41
CHEMBL83 TAMOXIFEN 4.0 1 7.16
CHEMBL5081355 1 7.09
CHEMBL5083006 1 6.91
CHEMBL5085178 1 6.59
CHEMBL5075395 1 6.48
CHEMBL5077738 1 6.46
CHEMBL5089862 1 6.45
CHEMBL5087904 1 6.38
CHEMBL5094779 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489 AFIMOXIFENE IC50 = 7.5 nM 8.12
CHEMBL5078348 IC50 = 8.8 nM 8.06
CHEMBL5081507 IC50 = 10.7 nM 7.97
CHEMBL5088475 IC50 = 15.1 nM 7.82
CHEMBL5083906 IC50 = 16.3 nM 7.79
CHEMBL5078187 IC50 = 21.0 nM 7.68
CHEMBL5084400 IC50 = 24.3 nM 7.61
CHEMBL5077058 IC50 = 35.5 nM 7.45
CHEMBL5094047 IC50 = 39.1 nM 7.41
CHEMBL83 TAMOXIFEN IC50 = 69.0 nM 7.16
CHEMBL5081355 IC50 = 81.0 nM 7.09
CHEMBL5083006 IC50 = 124.0 nM 6.91
CHEMBL5085178 IC50 = 255.0 nM 6.59
CHEMBL5075395 IC50 = 333.0 nM 6.48
CHEMBL5077738 IC50 = 348.0 nM 6.46
CHEMBL5089862 IC50 = 359.0 nM 6.45
CHEMBL5087904 IC50 = 422.0 nM 6.38
CHEMBL5094779 IC50 = 571.0 nM 6.24