Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.

doi:10.1021/acs.jmedchem.8b01040

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Article

Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.

Journal of medicinal chemistry - 27 Sept 2018

Schoepfer Joseph, Jahnke Wolfgang, Berellini Giuliano, Buonamici Silvia, Cotesta Simona, Cowan-Jacob Sandra W, Dodd Stephanie, Drueckes Peter, Fabbro Doriano, Gabriel Tobias, Groell Jean-Marc, Grotzfeld Robert M, Hassan A Quamrul, Henry Chrystèle, Iyer Varsha, Jones Darryl, Lombardo Franco, Loo Alice, Manley Paul W, Pellé Xavier, Rummel Gabriele, Salem Bahaa, Warmuth Markus, Wylie Andrew A, Zoller Thomas, Marzinzik Andreas L, Furet Pascal

Abstract excerpt

Chronic myelogenous leukemia (CML) arises from the constitutive activity of the BCR-ABL1 oncoprotein. Tyrosine kinase inhibitors (TKIs) that target the ATP-binding site have transformed CML into a chronic manageable disease. However, some patients develop drug resistance due to ATP-site mutations impeding drug binding. We describe the discovery of asciminib (ABL001), the first allosteric BCR-ABL1 inhibitor to...

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Identifiers

PMID: 30137981
DOI: 10.1021/acs.jmedchem.8b01040

Genes

ABL1
BCR

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.PMID 30137981Read ↗

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