Synonyms: CE-224,535 | CE-224535 | compound 3 [PMID: 21782426] | compound 33 [PMID: 21565499]
Compound class:
Synthetic organic
Comment: PF-04905428 is an investigational purinergic receptor 2 (P2X7) antagonist [2,4], with potential antiinflammatory action in various conditions such as arthritis, allergies, asthma, COPD, autoimmune diseases and other disorders.. PF-04905428 is one of the compounds claimed in patent US6974812 [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. Dombroski MA, Duplantier AJ. (2005)
Benzamide inhibitors of the P2X7 receptor. Patent number: US6974812 B2. Assignee: Pfizer Inc.. Priority date: 31/12/2002. Publication date: 13/12/2005. |
2. Duplantier AJ, Dombroski MA, Subramanyam C, Beaulieu AM, Chang SP, Gabel CA, Jordan C, Kalgutkar AS, Kraus KG, Labasi JM et al.. (2011)
Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. Bioorg Med Chem Lett, 21 (12): 3708-11. [PMID:21565499] |
3. Stock TC, Bloom BJ, Wei N, Ishaq S, Park W, Wang X, Gupta P, Mebus CA. (2012)
Efficacy and safety of CE-224,535, an antagonist of P2X7 receptor, in treatment of patients with rheumatoid arthritis inadequately controlled by methotrexate. J Rheumatol, 39 (4): 720-7. [PMID:22382341] |
4. Subramanyam C, Duplantier AJ, Dombroski MA, Chang SP, Gabel CA, Whitney-Pickett C, Perregaux DG, Labasi JM, Yoon K, Shepard RM et al.. (2011)
Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X₇ receptor. Bioorg Med Chem Lett, 21 (18): 5475-9. [PMID:21782426] |