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Assay Detail

CHEMBL5731782

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

Binding
MCF-7 ER Down-Regulation Assay: The ability of compounds to down-regulate Estrogen Receptor (ER) numbers was assessed in a cell based immuno-fluorescence assay using the MCF-7 human ductal carcinoma breast cell line.
ChEMBL ↗
234
Total Activities
72
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor (CHEMBL206) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chemical compounds
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 78 9.31 10.10
kon 78 - -
k_off 78 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5815414 — — 3 10.10
CHEMBL5993536 — — 3 10.10
CHEMBL5966618 — — 6 10.07
CHEMBL5427353 — — 3 10.06
CHEMBL5965839 — — 6 10.06
CHEMBL5918610 — — 3 10.03
CHEMBL4862453 — — 3 10.03
CHEMBL4868243 — — 3 9.92
CHEMBL6037451 — — 3 9.89
CHEMBL5888343 — — 3 9.85
CHEMBL6007343 — — 3 9.85
CHEMBL5894591 — — 3 9.85
CHEMBL6030138 — — 9 9.85
CHEMBL5799604 — — 3 9.85
CHEMBL5439583 — — 3 9.82
CHEMBL5430945 — — 3 9.80
CHEMBL5779249 — — 3 9.77
CHEMBL5951441 — — 3 9.77
CHEMBL5947266 — — 3 9.72
CHEMBL5793901 — — 3 9.70
CHEMBL5988881 — — 3 9.68
CHEMBL5743383 — — 3 9.68
CHEMBL5910449 — — 3 9.66
CHEMBL5827170 — — 3 9.62
CHEMBL6012876 — — 3 9.62
CHEMBL5819655 — — 3 9.60
CHEMBL5940600 — — 3 9.60
CHEMBL5874352 — — 3 9.59
CHEMBL5858886 — — 3 9.59
CHEMBL5755796 — — 3 9.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5815414 — IC50 = 0.079 nM 10.10
CHEMBL5993536 — IC50 = 0.08 nM 10.10
CHEMBL5966618 — IC50 = 0.086 nM 10.07
CHEMBL5965839 — IC50 = 0.087 nM 10.06
CHEMBL5427353 — IC50 = 0.087 nM 10.06
CHEMBL4862453 — IC50 = 0.093 nM 10.03
CHEMBL5918610 — IC50 = 0.094 nM 10.03
CHEMBL4868243 — IC50 = 0.12 nM 9.92
CHEMBL6037451 — IC50 = 0.13 nM 9.89
CHEMBL6007343 — IC50 = 0.14 nM 9.85
CHEMBL6030138 — IC50 = 0.14 nM 9.85
CHEMBL5894591 — IC50 = 0.14 nM 9.85
CHEMBL5888343 — IC50 = 0.14 nM 9.85
CHEMBL5799604 — IC50 = 0.14 nM 9.85
CHEMBL5439583 — IC50 = 0.15 nM 9.82
CHEMBL5430945 — IC50 = 0.16 nM 9.80
CHEMBL5779249 — IC50 = 0.17 nM 9.77
CHEMBL5951441 — IC50 = 0.17 nM 9.77
CHEMBL5947266 — IC50 = 0.19 nM 9.72
CHEMBL5793901 — IC50 = 0.2 nM 9.70
CHEMBL5988881 — IC50 = 0.21 nM 9.68
CHEMBL5743383 — IC50 = 0.21 nM 9.68
CHEMBL5910449 — IC50 = 0.22 nM 9.66
CHEMBL5827170 — IC50 = 0.24 nM 9.62
CHEMBL6012876 — IC50 = 0.24 nM 9.62
CHEMBL6030138 — IC50 = 0.24 nM 9.62
CHEMBL5940600 — IC50 = 0.25 nM 9.60
CHEMBL5819655 — IC50 = 0.25 nM 9.60
CHEMBL5858886 — IC50 = 0.26 nM 9.59
CHEMBL6030138 — IC50 = 0.26 nM 9.59
CHEMBL5874352 — IC50 = 0.26 nM 9.59
CHEMBL5755796 — IC50 = 0.27 nM 9.57
CHEMBL5948876 — IC50 = 0.28 nM 9.55
CHEMBL5938595 — IC50 = 0.31 nM 9.51
CHEMBL5917923 — IC50 = 0.32 nM 9.49
CHEMBL5956187 — IC50 = 0.33 nM 9.48
CHEMBL5904118 — IC50 = 0.36 nM 9.44
CHEMBL6065596 — IC50 = 0.37 nM 9.43
CHEMBL5904118 — IC50 = 0.38 nM 9.42
CHEMBL6000859 — IC50 = 0.4 nM 9.40
CHEMBL5996830 — IC50 = 0.41 nM 9.39
CHEMBL5873454 — IC50 = 0.42 nM 9.38
CHEMBL5782368 — IC50 = 0.43 nM 9.37
CHEMBL6021048 — IC50 = 0.43 nM 9.37
CHEMBL5987451 — IC50 = 0.46 nM 9.34
CHEMBL5821865 — IC50 = 0.47 nM 9.33
CHEMBL5955230 — IC50 = 0.48 nM 9.32
CHEMBL5425697 — IC50 = 0.49 nM 9.31
CHEMBL6065596 — IC50 = 0.5 nM 9.30
CHEMBL5847607 — IC50 = 0.51 nM 9.29