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Assay Detail

CHEMBL4370320

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

Binding
Induction of ERalpha degradation in human MCF7 cells after 18 to 24 hrs by in multiplexed cell assay
18
Total Activities
18
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

Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.
Scott JS, Bailey A, Buttar D, Carbajo RJ, Curwen J, Davey PRJ, Davies RDM, Degorce SL, Donald C, Gangl E, Greenwood R, Groombridge SD, Johnson T, Lamont S, Lawson M, Lister A, Morrow CJ, Moss TA, Pink JH, Polanski R.
J Med Chem (2019) 62 : 1593 -1608
PubMed 30640465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.94 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4583286 1 9.70
CHEMBL4448852 1 9.60
CHEMBL4515724 1 9.50
CHEMBL4586022 1 9.50
CHEMBL4436187 1 9.40
CHEMBL4584370 1 9.20
CHEMBL4541930 1 9.20
CHEMBL4536148 1 9.20
CHEMBL4462367 1 9.10
CHEMBL4436390 1 9.10
CHEMBL4517931 1 9.00
CHEMBL4586630 1 8.80
CHEMBL4536329 1 8.60
CHEMBL3775824 1 8.40
CHEMBL4518390 1 8.20
CHEMBL4515274 1 8.20
CHEMBL4451617 1 7.20
CHEMBL4554684 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4583286 IC50 = 0.1995 nM 9.70
CHEMBL4448852 IC50 = 0.2512 nM 9.60
CHEMBL4515724 IC50 = 0.3162 nM 9.50
CHEMBL4586022 IC50 = 0.3162 nM 9.50
CHEMBL4436187 IC50 = 0.3981 nM 9.40
CHEMBL4584370 IC50 = 0.631 nM 9.20
CHEMBL4541930 IC50 = 0.631 nM 9.20
CHEMBL4536148 IC50 = 0.631 nM 9.20
CHEMBL4462367 IC50 = 0.7943 nM 9.10
CHEMBL4436390 IC50 = 0.7943 nM 9.10
CHEMBL4517931 IC50 = 1.0 nM 9.00
CHEMBL4586630 IC50 = 1.585 nM 8.80
CHEMBL4536329 IC50 = 2.512 nM 8.60
CHEMBL3775824 IC50 = 3.981 nM 8.40
CHEMBL4518390 IC50 = 6.31 nM 8.20
CHEMBL4515274 IC50 = 6.31 nM 8.20
CHEMBL4451617 IC50 = 63.1 nM 7.20
CHEMBL4554684 IC50 > 10000.0 nM -