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Assay Detail

CHEMBL3429911

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

Binding
Suppression of ER alpha in human MCF7 cells after 24 hrs by immunostaining analysis
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.
Degorce SL, Bailey A, Callis R, De Savi C, Ducray R, Lamont G, MacFaul P, Maudet M, Martin S, Morgentin R, Norman RA, Peru A, Pink JH, Plé PA, Roberts B, Scott JS.
J Med Chem (2015) 58 : 3522 -3533
PubMed 25790336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.47 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3427402 1 8.57
CHEMBL195515 1 8.15
CHEMBL3427399 1 8.15
CHEMBL3427401 1 7.68
CHEMBL3427398 1 7.52
CHEMBL3427393 1 7.28
CHEMBL3427405 1 7.26
CHEMBL3427404 1 7.22
CHEMBL3427415 1 7.00
CHEMBL3427397 1 6.93
CHEMBL3427395 1 6.75
CHEMBL3427414 1 6.61
CHEMBL3427501 1 6.60
CHEMBL3427400 1 6.59
CHEMBL3425530 1 6.50
CHEMBL3427392 1 6.46
CHEMBL3427390 1 6.33
CHEMBL3427500 1 6.30
CHEMBL3427407 1 6.29
CHEMBL3427391 1 6.28
CHEMBL3427394 1 6.18
CHEMBL3427410 1 6.00
CHEMBL3427385 1 5.93
CHEMBL3427409 1 5.89
CHEMBL3427389 1 5.89
CHEMBL3427502 1 5.86
CHEMBL3427403 1 5.84
CHEMBL3427388 1 5.77
CHEMBL3427396 1 5.65
CHEMBL3427386 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3427402 IC50 = 2.7 nM 8.57
CHEMBL195515 IC50 = 7.0 nM 8.15
CHEMBL3427399 IC50 = 7.0 nM 8.15
CHEMBL3427401 IC50 = 21.0 nM 7.68
CHEMBL3427398 IC50 = 30.0 nM 7.52
CHEMBL3427393 IC50 = 52.0 nM 7.28
CHEMBL3427405 IC50 = 55.0 nM 7.26
CHEMBL3427404 IC50 = 60.0 nM 7.22
CHEMBL3427415 IC50 = 100.0 nM 7.00
CHEMBL3427397 IC50 = 117.0 nM 6.93
CHEMBL3427395 IC50 = 178.0 nM 6.75
CHEMBL3427414 IC50 = 248.0 nM 6.61
CHEMBL3427501 IC50 = 253.0 nM 6.60
CHEMBL3427400 IC50 = 256.0 nM 6.59
CHEMBL3425530 IC50 = 320.0 nM 6.50
CHEMBL3427392 IC50 = 350.0 nM 6.46
CHEMBL3427390 IC50 = 471.0 nM 6.33
CHEMBL3427500 IC50 = 506.0 nM 6.30
CHEMBL3427407 IC50 = 509.0 nM 6.29
CHEMBL3427391 IC50 = 531.0 nM 6.28
CHEMBL3427394 IC50 = 660.0 nM 6.18
CHEMBL3427410 IC50 = 1000.0 nM 6.00
CHEMBL3427385 IC50 = 1180.0 nM 5.93
CHEMBL3427409 IC50 = 1300.0 nM 5.89
CHEMBL3427389 IC50 = 1280.0 nM 5.89
CHEMBL3427502 IC50 = 1380.0 nM 5.86
CHEMBL3427403 IC50 = 1450.0 nM 5.84
CHEMBL3427388 IC50 = 1710.0 nM 5.77
CHEMBL3427396 IC50 = 2260.0 nM 5.65
CHEMBL3427386 IC50 = 3090.0 nM 5.51
CHEMBL3427412 IC50 = 3600.0 nM 5.44
CHEMBL3427387 IC50 = 5640.0 nM 5.25
CHEMBL3427408 IC50 = 5840.0 nM 5.23
CHEMBL3427413 IC50 = 10600.0 nM 4.97
CHEMBL3427406 IC50 > 3000.0 nM -
CHEMBL3427411 IC50 > 2150.0 nM -
CHEMBL33899 IC50 > 1270.0 nM -