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Assay Detail

CHEMBL873017

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Functional
Antiproliferative activity against MCF-7 cell line
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 1 — Organism
Curated By Expert

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Lead identification of a potent benzopyranone selective estrogen receptor modulator.
McKie JA, Bhagwat SS, Brady H, Doubleday M, Gayo L, Hickman M, Jalluri RK, Khammungkhune S, Kois A, Mortensen D, Richard N, Sapienza J, Shevlin G, Stein B, Sutherland M.
Bioorg Med Chem Lett (2004) 14 : 3407 -3410
PubMed 15177442 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.35 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81 RALOXIFENE 4.0 1 8.31
CHEMBL439967 1 8.11
CHEMBL113712 1 8.02
CHEMBL115000 1 7.92
CHEMBL115303 1 7.89
CHEMBL115489 1 7.82
CHEMBL326146 1 7.75
CHEMBL2137046 1 7.62
CHEMBL262042 1 7.07
CHEMBL115060 1 6.87
CHEMBL115194 1 6.47
CHEMBL325889 1 6.47
CHEMBL117263 1 6.37
CHEMBL421892 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81 RALOXIFENE IC50 = 4.9 nM 8.31
CHEMBL439967 IC50 = 7.7 nM 8.11
CHEMBL113712 IC50 = 9.5 nM 8.02
CHEMBL115000 IC50 = 12.0 nM 7.92
CHEMBL115303 IC50 = 13.0 nM 7.89
CHEMBL115489 IC50 = 15.0 nM 7.82
CHEMBL326146 IC50 = 18.0 nM 7.75
CHEMBL2137046 IC50 = 24.0 nM 7.62
CHEMBL262042 IC50 = 85.0 nM 7.07
CHEMBL115060 IC50 = 134.0 nM 6.87
CHEMBL115194 IC50 = 335.0 nM 6.47
CHEMBL325889 IC50 = 335.0 nM 6.47
CHEMBL117263 IC50 = 425.0 nM 6.37
CHEMBL421892 IC50 = 720.0 nM 6.14