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Synonyms: A250 [WO2012170976] | M-2951 | M2951 | MSC 2364447 | MSC-2364447C | MSC2364447C
Compound class: Synthetic organic
Comment: Evobrutinib is a Bruton's tyrosine kinase Inhibitor discovered by Merck, that has clinical potential across multiple autoimmune conditions (including rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis) . it is an orally active, ootent, and highly selective inhibitor with a covalent binding mode. The chemical structure is claimed as A250 in patent WO2012170976 .
Ligand Activity Visualisation Charts
These 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.✖
1. Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS et al.. (2019)
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
J Med Chem, 62 (17): 7643-7655. [PMID:31368705]
2. Haselmayer P, Camps M, Liu-Bujalski L, Nguyen N, Morandi F, Head J, O'Mahony A, Zimmerli SC, Bruns L, Bender AT et al.. (2019)
Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models.
J Immunol, 202 (10): 2888-2906. [PMID:30988116]
3. Hodous B, Liu-Bujalski L, Jones R, Bankston D, Johnson TL, Mochalkin I, Nguyen N, Qiu H, Goutopoulos A, Brugger N. (2012)
Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity.
Patent number: WO2012170976. Assignee: Merck Patent Gmbh. Priority date: 10/06/2011. Publication date: 13/12/2012.
4. Montalban X, Arnold DL, Weber MS, Staikov I, Piasecka-Stryczynska K, Willmer J, Martin EC, Dangond F, Syed S, Wolinsky JS et al.. (2019)
Placebo-Controlled Trial of an Oral BTK Inhibitor in Multiple Sclerosis.
N Engl J Med, 380 (25): 2406-2417. [PMID:31075187]