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Assay Detail

CHEMBL5381568

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

Binding
Binding affinity to ERalpha (unknown origin) by LanthaScreen TR-FRET competitive binding assay
ChEMBL ↗
40
Total Activities
40
Compounds Tested
1
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

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 8.45 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5421791 — — 1 9.20
CHEMBL4862431 — — 1 9.10
CHEMBL5400637 — — 1 9.10
CHEMBL5408358 — — 1 9.00
CHEMBL4528514 — — 1 9.00
CHEMBL5423660 — — 1 9.00
CHEMBL5425697 — — 1 8.90
CHEMBL4868243 — — 1 8.90
CHEMBL5413311 — — 1 8.90
CHEMBL5426160 — — 1 8.90
CHEMBL5432698 — — 1 8.90
CHEMBL5427353 — — 1 8.80
CHEMBL5430945 — — 1 8.80
CHEMBL5439583 — — 1 8.80
CHEMBL5420450 — — 1 8.80
CHEMBL5404753 — — 1 8.80
CHEMBL5426983 — — 1 8.80
CHEMBL5424726 — — 1 8.80
CHEMBL5427839 — — 1 8.80
CHEMBL5440088 — — 1 8.70
CHEMBL5399407 — — 1 8.70
CHEMBL5428933 — — 1 8.70
CHEMBL5398790 — — 1 8.70
CHEMBL5424786 — — 1 8.60
CHEMBL5404810 — — 1 8.50
CHEMBL5424734 — — 1 8.40
CHEMBL5407684 — — 1 8.30
CHEMBL5425859 — — 1 8.30
CHEMBL5400175 — — 1 8.20
CHEMBL5430566 — — 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5421791 — IC50 = 0.631 nM 9.20
CHEMBL4862431 — IC50 = 0.7943 nM 9.10
CHEMBL5400637 — IC50 = 0.7943 nM 9.10
CHEMBL5408358 — IC50 = 1.0 nM 9.00
CHEMBL4528514 — IC50 = 1.0 nM 9.00
CHEMBL5423660 — IC50 = 1.0 nM 9.00
CHEMBL5425697 — IC50 = 1.259 nM 8.90
CHEMBL4868243 — IC50 = 1.259 nM 8.90
CHEMBL5413311 — IC50 = 1.259 nM 8.90
CHEMBL5426160 — IC50 = 1.259 nM 8.90
CHEMBL5432698 — IC50 = 1.259 nM 8.90
CHEMBL5427839 — IC50 = 1.585 nM 8.80
CHEMBL5430945 — IC50 = 1.585 nM 8.80
CHEMBL5439583 — IC50 = 1.585 nM 8.80
CHEMBL5420450 — IC50 = 1.585 nM 8.80
CHEMBL5427353 — IC50 = 1.585 nM 8.80
CHEMBL5404753 — IC50 = 1.585 nM 8.80
CHEMBL5426983 — IC50 = 1.585 nM 8.80
CHEMBL5424726 — IC50 = 1.585 nM 8.80
CHEMBL5398790 — IC50 = 1.995 nM 8.70
CHEMBL5399407 — IC50 = 1.995 nM 8.70
CHEMBL5440088 — IC50 = 1.995 nM 8.70
CHEMBL5428933 — IC50 = 1.995 nM 8.70
CHEMBL5424786 — IC50 = 2.512 nM 8.60
CHEMBL5404810 — IC50 = 3.162 nM 8.50
CHEMBL5424734 — IC50 = 3.981 nM 8.40
CHEMBL5407684 — IC50 = 5.012 nM 8.30
CHEMBL5425859 — IC50 = 5.012 nM 8.30
CHEMBL5400175 — IC50 = 6.31 nM 8.20
CHEMBL5430566 — IC50 = 6.31 nM 8.20
CHEMBL5424508 — IC50 = 7.943 nM 8.10
CHEMBL5432663 — IC50 = 10.0 nM 8.00
CHEMBL5406802 — IC50 = 12.59 nM 7.90
CHEMBL5436976 — IC50 = 15.85 nM 7.80
CHEMBL5396127 — IC50 = 19.95 nM 7.70
CHEMBL5394023 — IC50 = 25.12 nM 7.60
CHEMBL5414394 — IC50 = 25.12 nM 7.60
CHEMBL5403840 — IC50 = 31.62 nM 7.50
CHEMBL5433664 — IC50 = 199.53 nM 6.70
CHEMBL5421737 — IC50 = 251.19 nM 6.60