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Assay Detail

CHEMBL831071

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

Binding
Binding potency for human ER alpha
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 (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.
Blizzard TA, DiNinno F, Morgan JD, Chen HY, Wu JY, Gude C, Kim S, Chan W, Birzin ET, Tien Yang Y, Pai LY, Zhang Z, Hayes EC, DaSilva CA, Tang W, Rohrer SP, Schaeffer JM, Hammond ML.
Bioorg Med Chem Lett (2004) 14 : 3861 -3864
PubMed 15225685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 9.12 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL433769 1 9.52
CHEMBL185083 1 9.40
CHEMBL181862 1 9.30
CHEMBL184367 1 9.22
CHEMBL184421 1 9.22
CHEMBL184371 1 9.22
CHEMBL184360 1 9.22
CHEMBL184202 1 9.15
CHEMBL434525 1 9.15
CHEMBL184598 1 9.10
CHEMBL304552 1 9.10
CHEMBL368688 1 9.05
CHEMBL185231 1 9.00
CHEMBL184974 1 8.92
CHEMBL361056 1 8.89
CHEMBL135 ESTRADIOL 4.0 1 8.89
CHEMBL81 RALOXIFENE 4.0 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL433769 IC50 = 0.3 nM 9.52
CHEMBL185083 IC50 = 0.4 nM 9.40
CHEMBL181862 IC50 = 0.5 nM 9.30
CHEMBL184367 IC50 = 0.6 nM 9.22
CHEMBL184421 IC50 = 0.6 nM 9.22
CHEMBL184371 IC50 = 0.6 nM 9.22
CHEMBL184360 IC50 = 0.6 nM 9.22
CHEMBL184202 IC50 = 0.7 nM 9.15
CHEMBL434525 IC50 = 0.7 nM 9.15
CHEMBL184598 IC50 = 0.8 nM 9.10
CHEMBL304552 IC50 = 0.8 nM 9.10
CHEMBL368688 IC50 = 0.9 nM 9.05
CHEMBL185231 IC50 = 1.0 nM 9.00
CHEMBL184974 IC50 = 1.2 nM 8.92
CHEMBL361056 IC50 = 1.3 nM 8.89
CHEMBL135 ESTRADIOL IC50 = 1.3 nM 8.89
CHEMBL81 RALOXIFENE IC50 = 1.8 nM 8.74