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Assay Detail

CHEMBL5037523

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

Functional
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by cell counter method
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 Autocuration

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer.
Caciolla J, Martini S, Spinello A, Pavlin M, Turrini E, Simonelli F, Belluti F, Rampa A, Bisi A, Fimognari C, Zaffaroni N, Gobbi S, Magistrato A.
Eur J Med Chem (2021) 224 : 113733 -113733
PubMed 34364162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.72 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093458 ENDOXIFEN 3.0 1 7.00
CHEMBL1444 LETROZOLE 4.0 1 5.39
CHEMBL5082245 1 5.00
CHEMBL5072101 1 4.61
CHEMBL5080066 1 4.56
CHEMBL5087363 1 4.43
CHEMBL5074047 1 4.43
CHEMBL5081446 1 4.40
CHEMBL5069811 1 4.38
CHEMBL5092560 1 4.38
CHEMBL5077976 1 4.28
CHEMBL5082681 1 4.24
CHEMBL5075144 1 4.22
CHEMBL5092843 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093458 ENDOXIFEN IC50 = 100.0 nM 7.00
CHEMBL1444 LETROZOLE IC50 = 4100.0 nM 5.39
CHEMBL5082245 IC50 = 10000.0 nM 5.00
CHEMBL5072101 IC50 = 24300.0 nM 4.61
CHEMBL5080066 IC50 = 27600.0 nM 4.56
CHEMBL5087363 IC50 = 37000.0 nM 4.43
CHEMBL5074047 IC50 = 37100.0 nM 4.43
CHEMBL5081446 IC50 = 39800.0 nM 4.40
CHEMBL5069811 IC50 = 41200.0 nM 4.38
CHEMBL5092560 IC50 = 42100.0 nM 4.38
CHEMBL5077976 IC50 = 53000.0 nM 4.28
CHEMBL5082681 IC50 = 58000.0 nM 4.24
CHEMBL5075144 IC50 = 60000.0 nM 4.22
CHEMBL5092843 IC50 > 100000.0 nM -