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Assay Detail

CHEMBL831077

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

Binding
Inhibition of estrogen receptor alpha
22
Total Activities
22
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 10: Chromanes: old scaffolds for new SERAMs.
Tan Q, Blizzard TA, Morgan JD, Birzin ET, Chan W, Yang YT, Pai LY, Hayes EC, DaSilva CA, Warrier S, Yudkovitz J, Wilkinson HA, Sharma N, Fitzgerald PM, Li S, Colwell L, Fisher JE, Adamski S, Reszka AA, Kimmel D, DiNinno F, Rohrer SP, Freedman LP, Schaeffer JM, Hammond ML.
Bioorg Med Chem Lett (2005) 15 : 1675 -1681
PubMed 15745820 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 8.80 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181368 1 9.52
CHEMBL359633 1 9.30
CHEMBL362428 1 9.18
CHEMBL181248 1 9.15
CHEMBL304552 1 9.10
CHEMBL181404 1 9.10
CHEMBL180146 1 9.10
CHEMBL361005 1 9.10
CHEMBL181369 1 9.05
CHEMBL180995 1 9.05
CHEMBL433581 1 8.89
CHEMBL368449 1 8.89
CHEMBL135 ESTRADIOL 4.0 1 8.89
CHEMBL360315 1 8.85
CHEMBL178470 1 8.85
CHEMBL181936 1 8.82
CHEMBL2113002 1 8.82
CHEMBL369724 1 8.62
CHEMBL359671 1 8.60
CHEMBL178559 1 7.85
CHEMBL180253 1 7.42
CHEMBL180538 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181368 IC50 = 0.3 nM 9.52
CHEMBL359633 IC50 = 0.5 nM 9.30
CHEMBL362428 IC50 = 0.66 nM 9.18
CHEMBL181248 IC50 = 0.7 nM 9.15
CHEMBL304552 IC50 = 0.8 nM 9.10
CHEMBL181404 IC50 = 0.8 nM 9.10
CHEMBL180146 IC50 = 0.8 nM 9.10
CHEMBL361005 IC50 = 0.8 nM 9.10
CHEMBL181369 IC50 = 0.9 nM 9.05
CHEMBL180995 IC50 = 0.9 nM 9.05
CHEMBL433581 IC50 = 1.3 nM 8.89
CHEMBL368449 IC50 = 1.3 nM 8.89
CHEMBL135 ESTRADIOL IC50 = 1.3 nM 8.89
CHEMBL360315 IC50 = 1.4 nM 8.85
CHEMBL178470 IC50 = 1.4 nM 8.85
CHEMBL181936 IC50 = 1.5 nM 8.82
CHEMBL2113002 IC50 = 1.5 nM 8.82
CHEMBL369724 IC50 = 2.4 nM 8.62
CHEMBL359671 IC50 = 2.5 nM 8.60
CHEMBL178559 IC50 = 14.0 nM 7.85
CHEMBL180253 IC50 = 38.0 nM 7.42
CHEMBL180538 IC50 = 45.0 nM 7.35