Synonyms: ABT-101 | ABT101 | compound 78 [PMID: 31560541] | DBPR-112
Compound class:
Synthetic organic
Comment: DBPR112 (a.k.a. ABT-101) is an orally bioavailable, advanced inhibitor of the tyrosine kinase activity of epidermal growth factor receptors, EGFR and EGFR2 (HER2, ERBB2) [1]. It inhibits wild type and L858R/T790M double mutant EGFRs, and has demonstrated improved potency against EGFR and EGFR2 exon 20 insertion mutations compared to osimertinib. DBPR112 was designed for potential to treat advanced non-small cell lung cancer.
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
References |
1. Lin SY, Chang Hsu Y, Peng YH, Ke YY, Lin WH, Sun HY, Shiao HY, Kuo FM, Chen PY, Lien TW et al.. (2019)
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. J Med Chem, 62 (22): 10108-10123. [PMID:31560541] |