Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists
N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high throughput screen (HTS) of a sub-set of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent starting point for a CCR4 receptor antagonist p...
| Main Authors: | , , , , , , , , , , , , , , , , , |
|---|---|
| Format: | Article |
| Published: |
American Chemical Society
2017
|
| Subjects: | |
| Online Access: | https://eprints.nottingham.ac.uk/45586/ |
| _version_ | 1848797160889384960 |
|---|---|
| author | Kindon, Nicholas Andrews, Glen Baxter, Andrew Cheshire, David Hemsley, Paul Johnson, Timothy Liu, Yu-Zhen McGinnity, Dermot McHale, Mark Mete, Antonio Reuberson, James Roberts, Bryan Steele, John Teobald, Barry Unitt, John Vaughan, Deborah Walters, Iain Stocks, Michael J. |
| author_facet | Kindon, Nicholas Andrews, Glen Baxter, Andrew Cheshire, David Hemsley, Paul Johnson, Timothy Liu, Yu-Zhen McGinnity, Dermot McHale, Mark Mete, Antonio Reuberson, James Roberts, Bryan Steele, John Teobald, Barry Unitt, John Vaughan, Deborah Walters, Iain Stocks, Michael J. |
| author_sort | Kindon, Nicholas |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high throughput screen (HTS) of a sub-set of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent starting point for a CCR4 receptor antagonist program and enabled the rapid progression through the Lead Identification and Lead Optimization phases resulting in the discovery of two bioavailable CCR4 receptor antagonist candidate drugs. |
| first_indexed | 2025-11-14T19:59:28Z |
| format | Article |
| id | nottingham-45586 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T19:59:28Z |
| publishDate | 2017 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-455862020-05-04T19:03:23Z https://eprints.nottingham.ac.uk/45586/ Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists Kindon, Nicholas Andrews, Glen Baxter, Andrew Cheshire, David Hemsley, Paul Johnson, Timothy Liu, Yu-Zhen McGinnity, Dermot McHale, Mark Mete, Antonio Reuberson, James Roberts, Bryan Steele, John Teobald, Barry Unitt, John Vaughan, Deborah Walters, Iain Stocks, Michael J. N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high throughput screen (HTS) of a sub-set of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent starting point for a CCR4 receptor antagonist program and enabled the rapid progression through the Lead Identification and Lead Optimization phases resulting in the discovery of two bioavailable CCR4 receptor antagonist candidate drugs. American Chemical Society 2017-09-01 Article PeerReviewed Kindon, Nicholas, Andrews, Glen, Baxter, Andrew, Cheshire, David, Hemsley, Paul, Johnson, Timothy, Liu, Yu-Zhen, McGinnity, Dermot, McHale, Mark, Mete, Antonio, Reuberson, James, Roberts, Bryan, Steele, John, Teobald, Barry, Unitt, John, Vaughan, Deborah, Walters, Iain and Stocks, Michael J. (2017) Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists. ACS Medicinal Chemistry Letters . ISSN 1948-5875 Chemokine receptor 4; MDC; TARC; CCR4; Antagonist https://doi.org/10.1021/acsmedchemlett.7b00315 doi:10.1021/acsmedchemlett.7b00315 doi:10.1021/acsmedchemlett.7b00315 |
| spellingShingle | Chemokine receptor 4; MDC; TARC; CCR4; Antagonist Kindon, Nicholas Andrews, Glen Baxter, Andrew Cheshire, David Hemsley, Paul Johnson, Timothy Liu, Yu-Zhen McGinnity, Dermot McHale, Mark Mete, Antonio Reuberson, James Roberts, Bryan Steele, John Teobald, Barry Unitt, John Vaughan, Deborah Walters, Iain Stocks, Michael J. Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists |
| title | Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists |
| title_full | Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists |
| title_fullStr | Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists |
| title_full_unstemmed | Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists |
| title_short | Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists |
| title_sort | discovery of azd-2098 and azd-1678, two potent and bioavailable ccr4 receptor antagonists |
| topic | Chemokine receptor 4; MDC; TARC; CCR4; Antagonist |
| url | https://eprints.nottingham.ac.uk/45586/ https://eprints.nottingham.ac.uk/45586/ https://eprints.nottingham.ac.uk/45586/ |