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Assay Detail

CHEMBL4676154

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

Binding
Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ER-alpha level incubated for 18 to 24 hrs by Alexa fluor 488/Hoechst staining based immunofluorescence imaging analysis
ChEMBL ↗
36
Total Activities
36
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

Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Scott JS,Moss TA,Balazs A,Barlaam B,Breed J,Carbajo RJ,Chiarparin E,Davey PRJ,Delpuech O,Fawell S,Fisher DI,Gagrica S,Gangl ET,Grebe T,Greenwood RD,Hande S,Hatoum-Mokdad H,Herlihy K,Hughes S,Hunt TA,Huynh H,Janbon SLM,Johnson T,Kavanagh S,Klinowska T,Lawson M,Lister AS,Marden S,McGinnity DF,Morrow CJ,Nissink JWM,O'Donovan DH,Peng B,Polanski R,Stead DS,Stokes S,Thakur K,Throner SR,Tucker MJ,Varnes J,Wang H,Wilson DM,Wu D,Wu Y,Yang B,Yang W
J Med Chem (2020) 63 : 14530 -14559
PubMed 32910656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 9.52 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4743256 — — 1 10.40
CHEMBL4759597 — — 1 10.20
CHEMBL4758424 — — 1 10.00
CHEMBL4756497 — — 1 9.90
CHEMBL4752435 — — 1 9.90
CHEMBL4780809 — — 1 9.90
CHEMBL4650365 CAMIZESTRANT 3.0 1 9.80
CHEMBL4795387 — — 1 9.80
CHEMBL4756831 — — 1 9.80
CHEMBL4785486 — — 1 9.80
CHEMBL4759688 — — 1 9.70
CHEMBL4751770 — — 1 9.70
CHEMBL4751971 — — 1 9.70
CHEMBL4792482 — — 1 9.70
CHEMBL4777960 — — 1 9.60
CHEMBL4792890 — — 1 9.50
CHEMBL4754747 — — 1 9.50
CHEMBL4749269 — — 1 9.50
CHEMBL4753585 — — 1 9.50
CHEMBL4742862 — — 1 9.50
CHEMBL4779715 — — 1 9.40
CHEMBL4750007 — — 1 9.40
CHEMBL4782483 — — 1 9.40
CHEMBL4757886 — — 1 9.40
CHEMBL4762458 — — 1 9.40
CHEMBL4790076 — — 1 9.30
CHEMBL4763079 — — 1 9.30
CHEMBL4752903 — — 1 9.30
CHEMBL4780994 — — 1 9.30
CHEMBL4759607 — — 1 9.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4743256 — IC50 = 0.03981 nM 10.40
CHEMBL4759597 — IC50 = 0.0631 nM 10.20
CHEMBL4758424 — IC50 = 0.1 nM 10.00
CHEMBL4756497 — IC50 = 0.1259 nM 9.90
CHEMBL4752435 — IC50 = 0.1259 nM 9.90
CHEMBL4780809 — IC50 = 0.1259 nM 9.90
CHEMBL4785486 — IC50 = 0.1585 nM 9.80
CHEMBL4756831 — IC50 = 0.1585 nM 9.80
CHEMBL4795387 — IC50 = 0.1585 nM 9.80
CHEMBL4650365 CAMIZESTRANT IC50 = 0.1585 nM 9.80
CHEMBL4759688 — IC50 = 0.1995 nM 9.70
CHEMBL4751770 — IC50 = 0.1995 nM 9.70
CHEMBL4751971 — IC50 = 0.1995 nM 9.70
CHEMBL4792482 — IC50 = 0.1995 nM 9.70
CHEMBL4777960 — IC50 = 0.2512 nM 9.60
CHEMBL4754747 — IC50 = 0.3162 nM 9.50
CHEMBL4749269 — IC50 = 0.3162 nM 9.50
CHEMBL4742862 — IC50 = 0.3162 nM 9.50
CHEMBL4792890 — IC50 = 0.3162 nM 9.50
CHEMBL4753585 — IC50 = 0.3162 nM 9.50
CHEMBL4779715 — IC50 = 0.3981 nM 9.40
CHEMBL4750007 — IC50 = 0.3981 nM 9.40
CHEMBL4782483 — IC50 = 0.3981 nM 9.40
CHEMBL4757886 — IC50 = 0.3981 nM 9.40
CHEMBL4762458 — IC50 = 0.3981 nM 9.40
CHEMBL4763079 — IC50 = 0.5012 nM 9.30
CHEMBL4780994 — IC50 = 0.5012 nM 9.30
CHEMBL4752903 — IC50 = 0.5012 nM 9.30
CHEMBL4790076 — IC50 = 0.5012 nM 9.30
CHEMBL4759607 — IC50 = 0.631 nM 9.20
CHEMBL4744329 — IC50 = 0.631 nM 9.20
CHEMBL4797178 — IC50 = 0.7943 nM 9.10
CHEMBL4797729 — IC50 = 0.7943 nM 9.10
CHEMBL4787725 — IC50 = 1.0 nM 9.00
CHEMBL4779640 — IC50 = 1.0 nM 9.00
CHEMBL4756084 — IC50 = 3.162 nM 8.50