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Assay Detail

CHEMBL5381569

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 downregulation of ERaplha by multiplexed assay
ChEMBL ↗
40
Total Activities
40
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 a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.
Scott JS, Stead D, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Cureton N, Davey PRJ, Fisher DI, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Hughes SJ, Hunt TA, Johnson T, Kavanagh SL, Klinowska TCM, Larner CJB, Lawson M, Lister AS, Longmire D, Marden S, McGuire TM, McMillan C, McMurray L, Morrow CJ, Nissink JWM, Moss TA, O'Donovan DH, Polanski R, Stokes S, Thakur K, Trueman D, Truman C, Tucker MJ, Wang H, Whalley N, Wu D, Wu Y, Yang B, Yang W.
J Med Chem (2023) 66 : 2918 -2945
PubMed 36727211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 8.98 10.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5400637 — — 1 10.50
CHEMBL4528514 — — 1 10.10
CHEMBL5413311 — — 1 10.10
CHEMBL5427353 — — 1 10.10
CHEMBL5421791 — — 1 10.00
CHEMBL4868243 — — 1 9.90
CHEMBL5430945 — — 1 9.80
CHEMBL5439583 — — 1 9.80
CHEMBL5399407 — — 1 9.70
CHEMBL5432698 — — 1 9.70
CHEMBL4862431 — — 1 9.60
CHEMBL5398790 — — 1 9.60
CHEMBL5428933 — — 1 9.60
CHEMBL5423660 — — 1 9.50
CHEMBL5420450 — — 1 9.50
CHEMBL5408358 — — 1 9.50
CHEMBL5440088 — — 1 9.40
CHEMBL5426160 — — 1 9.40
CHEMBL5426983 — — 1 9.40
CHEMBL5425697 — — 1 9.30
CHEMBL5404810 — — 1 9.20
CHEMBL5427839 — — 1 9.10
CHEMBL5425859 — — 1 9.10
CHEMBL5432663 — — 1 9.10
CHEMBL5424786 — — 1 9.00
CHEMBL5424726 — — 1 8.90
CHEMBL5436976 — — 1 8.90
CHEMBL5424734 — — 1 8.80
CHEMBL5430566 — — 1 8.70
CHEMBL5404753 — — 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5400637 — IC50 = 0.03162 nM 10.50
CHEMBL4528514 — IC50 = 0.07943 nM 10.10
CHEMBL5427353 — IC50 = 0.07943 nM 10.10
CHEMBL5413311 — IC50 = 0.07943 nM 10.10
CHEMBL5421791 — IC50 = 0.1 nM 10.00
CHEMBL4868243 — IC50 = 0.1259 nM 9.90
CHEMBL5430945 — IC50 = 0.1585 nM 9.80
CHEMBL5439583 — IC50 = 0.1585 nM 9.80
CHEMBL5399407 — IC50 = 0.1995 nM 9.70
CHEMBL5432698 — IC50 = 0.1995 nM 9.70
CHEMBL5428933 — IC50 = 0.2512 nM 9.60
CHEMBL5398790 — IC50 = 0.2512 nM 9.60
CHEMBL4862431 — IC50 = 0.2512 nM 9.60
CHEMBL5408358 — IC50 = 0.3162 nM 9.50
CHEMBL5420450 — IC50 = 0.3162 nM 9.50
CHEMBL5423660 — IC50 = 0.3162 nM 9.50
CHEMBL5440088 — IC50 = 0.3981 nM 9.40
CHEMBL5426160 — IC50 = 0.3981 nM 9.40
CHEMBL5426983 — IC50 = 0.3981 nM 9.40
CHEMBL5425697 — IC50 = 0.5012 nM 9.30
CHEMBL5404810 — IC50 = 0.631 nM 9.20
CHEMBL5425859 — IC50 = 0.7943 nM 9.10
CHEMBL5432663 — IC50 = 0.7943 nM 9.10
CHEMBL5427839 — IC50 = 0.7943 nM 9.10
CHEMBL5424786 — IC50 = 1.0 nM 9.00
CHEMBL5424726 — IC50 = 1.259 nM 8.90
CHEMBL5436976 — IC50 = 1.259 nM 8.90
CHEMBL5424734 — IC50 = 1.585 nM 8.80
CHEMBL5430566 — IC50 = 1.995 nM 8.70
CHEMBL5400175 — IC50 = 3.981 nM 8.40
CHEMBL5404753 — IC50 = 3.981 nM 8.40
CHEMBL5407684 — IC50 = 6.31 nM 8.20
CHEMBL5406802 — IC50 = 15.85 nM 7.80
CHEMBL5424508 — IC50 = 15.85 nM 7.80
CHEMBL5414394 — IC50 = 25.12 nM 7.60
CHEMBL5403840 — IC50 = 39.81 nM 7.40
CHEMBL5396127 — IC50 = 50.12 nM 7.30
CHEMBL5394023 — IC50 = 63.1 nM 7.20
CHEMBL5433664 — IC50 = 100.0 nM 7.00
CHEMBL5421737 — IC50 = 125.89 nM 6.90