Synonyms: AZD 1981 | AZD-1981
Compound class:
Synthetic organic
Comment: AZD1981 was an investigational compound being assessed as a potential treatment for asthma. Mechanistically it is a potent, orally active, selective and reversible antagonist of the DP2 receptor (CRTH2).
This compound is now included for repurposing in the AstaZeneca's Open Innovation Pharmacology Toolbox. It was also Case Study (2) in the AZ 2014 review paper [1]. 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. ✖ |
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References |
1. Cook D, Brown D, Alexander R, March R, Morgan P, Satterthwaite G, Pangalos MN. (2014)
Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework. Nat Rev Drug Discov, 13 (6): 419-31. [PMID:24833294] |
2. Kuna P, Bjermer L, Tornling G. (2016)
Two Phase II randomized trials on the CRTh2 antagonist AZD1981 in adults with asthma. Drug Des Devel Ther, 10: 2759-70. [PMID:27621597] |
3. Luker T, Bonnert R, Brough S, Cook AR, Dickinson MR, Dougall I, Logan C, Mohammed RT, Paine S, Sanganee HJ et al.. (2011)
Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981. Bioorg Med Chem Lett, 21 (21): 6288-92. [PMID:21944852] |
4. Oliver ET, Chichester K, Devine K, Sterba PM, Wegner C, Vonakis BM, Saini SS. (2019)
Effects of an Oral CRTh2 Antagonist (AZD1981) on Eosinophil Activity and Symptoms in Chronic Spontaneous Urticaria. Int Arch Allergy Immunol, 179 (1): 21-30. [PMID:30879003] |
5. Schmidt JA, Bell FM, Akam E, Marshall C, Dainty IA, Heinemann A, Dougall IG, Bonnert RV, Sargent CA. (2013)
Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma. Br J Pharmacol, 168 (7): 1626-38. [PMID:23146091] |
6. Snell N, Foster M, Vestbo J. (2013)
Efficacy and safety of AZD1981, a CRTH2 receptor antagonist, in patients with moderate to severe COPD. Respir Med, 107 (11): 1722-30. [PMID:23827726] |