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Assay Detail

CHEMBL5255157

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Toxicity
Binding affinity to human ERG
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.
Cui Y, Wang R, Wei Y, Hou F, Li H, Jiang Y, Sun Y, Fu S, Zuo L, Wang X, Li M, Li J, Liu N, Zhang K, Wei M, Yang G.
Bioorg Med Chem (2023) 81 : 117202 -117202
PubMed 36804726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.88 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545154 POZIOTINIB 3.0 1 6.04
CHEMBL5282641 1 5.95
CHEMBL1173655 AFATINIB 4.0 1 5.66
CHEMBL5288888 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545154 POZIOTINIB IC50 = 915.0 nM 6.04
CHEMBL5282641 IC50 = 1135.0 nM 5.95
CHEMBL1173655 AFATINIB IC50 = 2206.0 nM 5.66
CHEMBL5288888 IC50 > 15000.0 nM -