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view-simple-page-conent"> <div class="container"> <article id="post-273" class="post-273 page type-page status-publish hentry" itemtype="https://schema.org/CreativeWork" itemscope=""> <div class="entry-content entry-content-servises "> <h1>Kinase Panel Screening and Profiling Service</h1> <div class="text-mit-bild-text"> <div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"> <p>Broad kinase screening is crucial for the identification of selective and potent kinase inhibitors. Determination and improvement of the selectivity of a compound by screening a large part of the kinome are of pivotal importance in the discovery process of novel kinase inhibitors e.g. to reduce the risk of adverse side effects or both, kinase inhibitors and compounds inhibiting non-kinase targets.</p> <ul> <li>Reaction Biology offers the largest kinase panel for kinase profiling in the industry ensuring the most reliable results for your inhibitor selectivity screening covering most of the human kinome.</li> <li>Kinase selectivity profiling is performed on a monthly (³³PanQinase™) or bi-weekly (HotSpot™) schedule, which allows us to offer very competitive pricing.</li> <li><strong>HotSpot kinase screening service now available at physiologically relevant 1mM ATP for 340 <i>wild type</i> kinases, in addition to existing standard concentrations of 1μM, 10μM or apparent ATP-Km up to 100μM</strong></li> <li>Specialty panels comprise a selection of kinase-specific mutants or our CDK panel.</li> <li>Kinase panel reports from the US facility include a free control compound’s IC50 curve.</li> </ul> <p>Reaction Biology’s kinase assays were ranked highest in the Kinase Profiling Trends Survey by HTStec <span lang="EN-US" xml:lang="EN-US">for a reason: Our contract research organization accelerates the drug discovery and development process in two global facilities: one in Pennsylvania, one in Germany. We learn about what our clients want to achieve in their research and match it with our most suitable kinase selectivity profiling service.</span></p> <p><span lang="EN-US" xml:lang="EN-US">As our panels of kinases continue to grow, we consistently demonstrate the most reliable kinase selectivity screening services for clients worldwide based on accurate kinase activity data. </span>Contact us today to discuss <span lang="EN-US" xml:lang="EN-US">how our kinase panel assays can aid </span>your project!</p> </div> <div class="contact-buttons"> <div class="color-scheme-turquoise block block-block-content block-block-content9594f627-1f8b-4f13-b65e-979c19e399c0"> <a href="https://www.reactionbiology.com/contact/contact-us"> <div class="field field--name-field-icon field--type-image field--label-hidden field__items"> <img decoding="async" src="https://www.reactionbiology.com/wp-content/themes/Divi-child/images/icons-email.svg" alt="E-Mail" title="E-Mail" typeof="foaf:Image"> </div> <div 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src="https://www.reactionbiology.com/wp-content/themes/Divi-child/images/icons-meeting.svg" alt="Meet us at your next conference" title="Meet us at your next conference" typeof="foaf:Image"> </div> <div class="field field--name-field-text field--type-string field--label-hidden field__items"> Meet us at your next conference </div> </a> </div> <div class="color-scheme-turquoise block block-block-content block-block-contentff27f1d7-2f17-4dd2-ad72-3ef66b6982de"> <a href="/cdn-cgi/l/email-protection#5a65292f38303f392e67137a2d3b342e7a2e357a29323b283f7a2e3233297a083f3b392e3335347a18333536353d237a363334317a2d332e327a23352f7c3b372a6138353e2367322e2e2a296075752d2d2d74283f3b392e33353438333536353d237439353775293f282c33393f29753133343b293f773b29293b2329753133343b293f772a3b343f36772939283f3f3433343d75"> <div class="field field--name-field-icon field--type-image field--label-hidden field__items"> <img decoding="async" src="https://www.reactionbiology.com/wp-content/themes/Divi-child/images/icons-share.svg" alt="Share" title="Share" typeof="foaf:Image"> </div> <div class="field field--name-field-text field--type-string field--label-hidden field__items"> Share </div> </a> </div> </div> </div> </div> </article> </div> </div> <div id="_anchor" class="paragraph weiss black paragraph--type--paragraph-container paragraph--view-mode--default"><div id="kps-id" class="paragraph text-right images-1 headline-right contact-buttons- paragraph--type--text-with-image paragraph--view-mode--default"><div class="container center"><div class="text-wrapper"><h3>New Poster: Kinase drug discovery 20 years after imatinib</h3> <div class="text-mit-bild-text"> <div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"> <p>Reaction Biology sponsored a poster authored by Philip Cohen, Darren Cross, and Pasi Jänne that was published by Nature Reviews Drug Discovery.</p> <p>The peer-reviewed poster illustrates the tremendous progress made over the last 20 years towards the development of new kinase inhibitors.</p> <p><a class="magnific-popup-kinase-nature" href="/form/2022-kinase-nature-poster-download">Download our Poster</a></p> </div> </div> <div class="text-mit-bild-bild field field--name-field-images field--type-image field--label-hidden field__items"> <div class="text-mit-bild-bild-rahmen"> <div class="field__item"> <p><img loading="lazy" decoding="async" class="aligncenter size-full wp-image-91" src="https://www.reactionbiology.com/wp-content/uploads/2023/06/nrdKinase-Inhibitor-poster-WEB.jpg" alt="" width="570" height="389" srcset="https://www.reactionbiology.com/wp-content/uploads/2023/06/nrdKinase-Inhibitor-poster-WEB.jpg 570w, https://www.reactionbiology.com/wp-content/uploads/2023/06/nrdKinase-Inhibitor-poster-WEB-300x205.jpg 300w" sizes="(max-width: 570px) 100vw, 570px" /></p> <div class="caption">RB Kinase Drug Discovery Poster</div> </div> </div> </div> </div></div></div><div id="kps-id2" class="paragraph paragraph--type--table paragraph--view-mode--default"><div class="container center"><h2>Selectivity Kinase Panels from Reaction Biology are the Largest in the Industry with 700+ Kinases</h2> <div class="field field--name-field-table field--type-tablefield field--label-hidden field__items"> <div class="field__item"> <div id="tablefield-wrapper-paragraph-38552-field_table-0" class="tablefield-wrapper"> <div id="tablefield-paragraph-38552-field_table-0_wrapper" class="dataTables_wrapper no-footer"> <table id="tablefield-paragraph-38552-field_table-0" class="tablefield dataTable no-footer dtr-inline" role="grid" data-striping="1"> <caption>Panels run at US facility</caption> <thead> <tr role="row"> <th class="row_0 col_0 all control sorting_asc" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-0" aria-sort="ascending" aria-label="Panels run at US facility: activate to sort column descending">Panels run at US facility</th> <th class="row_0 col_1 min-fablet sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-0" aria-label="Panel size: activate to sort column ascending">Panel size</th> <th class="row_0 col_2 min-fablet sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-0" aria-label="Panel: activate to sort column ascending">ATP options</th> <th class="row_0 col_2 min-fablet sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-0" aria-label="Panel: activate to sort column ascending">Testing options</th> <th class="row_0 col_2 min-fablet sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-0" aria-label="Panel: activate to sort column ascending">Panel</th> </tr> </thead> <tbody> <tr class="odd" role="row"> <td class="row_1 col_0 all control sorting_1" tabindex="0">Wild Type Kinase Panel</td> <td class="row_1 col_1 min-fablet" align="center">384</td> <td class="row_1 col_2 link min-fablet" align="center">1μM, 10μM, Km and 1mM</td> <td class="row_1 col_2 link min-fablet" align="center">1 & 10 doses</td> <td class="row_1 col_2 link min-fablet" align="center"><a class="link" href="https://www.reactionbiology.com/list-kinase-targets-us-facility?panel=Bi-weekly%20Wild%20Type%20Panel">view panel</a></td> </tr> <tr class="even" role="row"> <td class="row_2 col_0 all control sorting_1" tabindex="0">Diversify Panel</td> <td class="row_2 col_1 min-fablet" align="center">69</td> <td class="row_2 col_2 link min-fablet" align="center">Km & 1mM</td> <td class="row_2 col_2 link min-fablet" align="center">1 & 10 doses</td> <td class="row_2 col_2 link min-fablet" align="center"><a class="link" href="https://www.reactionbiology.com/list-kinase-targets-us-facility/?panel=Diversify Panel">view panel</a></td> </tr> <tr class="odd" role="row"> <td class="row_3 col_0 all control sorting_1" tabindex="0">Mutant Kinase Panel</td> <td class="row_3 col_1 min-fablet" align="center">355</td> <td class="row_3 col_2 link min-fablet" align="center">1μM, 10μM, Km</td> <td class="row_3 col_2 link min-fablet" align="center">1 & 10 doses</td> <td class="row_3 col_2 link min-fablet" align="center"><a class="link" href="https://www.reactionbiology.com/list-kinase-targets-us-facility/?panel=Bi-weekly%20Mutant%20Panel">view panel</a></td> </tr> <tr class="even" role="row"> <td class="row_4 col_0 all control sorting_1" tabindex="0">Atypical Kinase Panel</td> <td class="row_4 col_1 min-fablet" align="center">24</td> <td class="row_4 col_2 link min-fablet" align="center">1μM, 10μM, Km</td> <td class="row_4 col_2 link min-fablet" align="center">1 & 10 doses</td> <td class="row_4 col_2 link min-fablet" align="center"><a class="link" href="https://www.reactionbiology.com/list-kinase-targets-us-facility/?panel=Bi-weekly%20Atypical%20Panel">view panel</a></td> </tr> <tr class="odd" role="row"> <td class="row_5 col_0 all control sorting_1" tabindex="0">Lipid Kinase Panel</td> <td class="row_5 col_1 min-fablet" align="center">23</td> <td class="row_5 col_2 link min-fablet" align="center">1μM, 10μM, Km</td> <td class="row_5 col_2 link min-fablet" align="center">1 & 10 doses</td> <td class="row_5 col_2 link min-fablet" align="center"><a class="link" href="https://www.reactionbiology.com/list-kinase-targets-us-facility/?panel=Bi-weekly%20Lipid%20Kinase%20Panel">view panel</a></td> </tr> <tr class="odd" role="row"> <td class="row_5 col_0 all control sorting_1" tabindex="0">Diacylglycerol Kinase Panel</td> <td class="row_5 col_1 min-fablet" align="center">10</td> <td class="row_5 col_2 link min-fablet" align="center">50μM, 200μM, Km & 1mM</td> <td class="row_5 col_2 link min-fablet" align="center">1 & 10 doses</td> <td class="row_5 col_2 link min-fablet" align="center"><a class="link" href="https://www.reactionbiology.com/list-kinase-targets-us-facility/?panel=Bi-weekly%20DGK%20Panel">view panel</a></td> </tr> </tbody> </table> </div> </div> </div> <div class="field__item"> <div id="tablefield-wrapper-paragraph-38552-field_table-1" class="tablefield-wrapper"> <div id="tablefield-paragraph-38552-field_table-1_wrapper" class="dataTables_wrapper no-footer"> <table id="tablefield-paragraph-38552-field_table-1" class="tablefield dataTable no-footer dtr-inline" role="grid" data-striping="1"> <caption>Kinase Selectivity Assay Panels</caption> <thead> <tr role="row"> <th class="row_0 col_0 all control sorting_asc" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-1" aria-sort="ascending" aria-label="Panels run at German facility: activate to sort column descending">Panels run at German facility</th> <th class="row_0 col_1 min-fablet sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-1" aria-label="Panel size: activate to sort column ascending">Panel size</th> <th class="row_0 col_2 min-fablet sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-1" aria-label="Panel: activate to sort column ascending">ATP options</th> <th class="row_0 col_2 min-fablet sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-1" aria-label="Panel: activate to sort column ascending">Testing options</th> <th class="row_0 col_2 min-fablet sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-38552-field_table-1" aria-label="Panel: activate to sort column ascending">Panel</th> </tr> </thead> <tbody> <tr class="odd" role="row"> <td class="row_1 col_0 all control sorting_1" tabindex="0">Wild Type Kinase Panel</td> <td class="row_1 col_1 min-fablet" align="center">350</td> <td class="row_1 col_2 link min-fablet" align="center">Km</td> <td class="row_1 col_2 link min-fablet" align="center">1 & 10 doses</td> <td class="row_1 col_2 link min-fablet" align="center"><a class="link" href="https://www.reactionbiology.com/list-kinase-targets-german-facility/?panel=Monthly%20Wild%20Type%20Panel">view panel</a></td> </tr> <tr class="even" role="row"> <td class="row_2 col_0 all control sorting_1" tabindex="0">Mutant Kinase Panel</td> <td class="row_2 col_1 min-fablet" align="center">96</td> <td class="row_2 col_2 link min-fablet" align="center">Km</td> <td class="row_2 col_2 link min-fablet" align="center">1 & 10 doses</td> <td class="row_2 col_2 link min-fablet" align="center"><a class="link" href="https://www.reactionbiology.com/list-kinase-targets-german-facility/?panel=Monthly%20Mutant%20Panel">view panel</a></td> </tr> <tr class="odd" role="row"> <td class="row_3 col_0 all control sorting_1" tabindex="0">Lipid Kinase Panel</td> <td class="row_3 col_1 min-fablet" align="center">14</td> <td class="row_3 col_2 link min-fablet" align="center">Km</td> <td class="row_3 col_2 link min-fablet" align="center">1 & 10 doses</td> <td class="row_3 col_2 link min-fablet" align="center"><a class="link" href="https://www.reactionbiology.com/list-kinase-targets-german-facility/?panel=Monthly%20Lipid%20Kinase%20Panel">view panel</a></td> </tr> </tbody> </table> </div> </div> </div> </div> </div></div><div id="kps-id3" class="paragraph paragraph--type--table paragraph--view-mode--default"><div class="container center"><h2>Specialty Kinase Profiling</h2> <div class="text-mit-bild-text"> <div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"> <p>In addition to broad kinome selectivity panels, we perform screening of specialty panels on an on-demand basis.</p> </div> </div> <div class="field field--name-field-table field--type-tablefield field--label-hidden field__items"> <div class="field__item"> <div id="tablefield-wrapper-paragraph-2540-field_table-0" class="tablefield-wrapper"> <table id="tablefield-paragraph-2540-field_table-0" class="tablefield" data-striping="1"> <thead> <tr> <th class="row_0 col_0">Panels run at US facility</th> <th class="row_0 col_1">Panel size</th> <th class="row_0 col_2">Data</th> </tr> </thead> <tbody> <tr class="odd"> <td class="row_1 col_0">ABL1 Mutant Profiler</td> <td class="row_1 col_1">15</td> <td class="row_1 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/abl1_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even"> <td class="row_2 col_0">ALK Mutant Profiler</td> <td class="row_2 col_1">29</td> <td class="row_2 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/alk_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd"> <td class="row_3 col_0">BRAF Mutant Profiler</td> <td class="row_3 col_1">16</td> <td class="row_3 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/braf_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even"> <td class="row_4 col_0">c-KIT Mutant Profiler</td> <td class="row_4 col_1">24</td> <td class="row_4 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/c-kit_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd"> <td class="row_5 col_0">c-MET Mutant Profiler</td> <td class="row_5 col_1">32</td> <td class="row_5 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/c-met_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even"> <td class="row_6 col_0">CDK Profiler</td> <td class="row_6 col_1">35</td> <td class="row_6 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/cdk_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd"> <td class="row_7 col_0">EGFR Mutant Profiler</td> <td class="row_7 col_1">65</td> <td class="row_7 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/egfr_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even"> <td class="row_8 col_0">ERBB2 Mutant Profiler</td> <td class="row_8 col_1">10</td> <td class="row_8 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/erbb2_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd"> <td class="row_9 col_0">FGFR2 Mutant Profiler</td> <td class="row_9 col_1">19</td> <td class="row_9 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/fgfr2_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even"> <td class="row_10 col_0">FGFR3 Mutant Profiler</td> <td class="row_10 col_1">6</td> <td class="row_10 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/fgfr3_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd"> <td class="row_11 col_0">FGFR4 Mutant Profiler</td> <td class="row_11 col_1">5</td> <td class="row_11 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/fgfr4_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even"> <td class="row_12 col_0">FLT3 Mutant Profiler</td> <td class="row_12 col_1">13</td> <td class="row_12 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/flt3_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd"> <td class="row_13 col_0">RET Mutant Profiler</td> <td class="row_13 col_1">36</td> <td class="row_13 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/ret_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even"> <td class="row_14 col_0">TIE Mutant Profiler</td> <td class="row_14 col_1">10</td> <td class="row_14 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/tie_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd"> <td class="row_15 col_0">TRKA Mutant Profiler</td> <td class="row_15 col_1">15</td> <td class="row_15 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/trka_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even"> <td class="row_16 col_0">TRKC Mutant Profiler</td> <td class="row_16 col_1">6</td> <td class="row_16 col_2 datasheet"><a class="datasheet overlay" href="/datasheet/trkc_kin_mut_malvern" target="_blank" rel="noopener">Data sheet</a></td> </tr> </tbody> </table> </div> </div> <div class="field__item"> <div id="tablefield-wrapper-paragraph-2540-field_table-1" class="tablefield-wrapper"> <div id="tablefield-paragraph-2540-field_table-1_wrapper" class="dataTables_wrapper no-footer"> <table id="tablefield-paragraph-2540-field_table-1" class="tablefield dataTable no-footer dtr-inline" role="grid" data-striping="1"> <thead> <tr role="row"> <th class="row_0 col_0 all control sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-2540-field_table-1" aria-label="Panels run at German facility: activate to sort column ascending">Panels run at German facility</th> <th class="row_0 col_1 min-fablet sorting_desc" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-2540-field_table-1" aria-sort="descending" aria-label="Panel size: activate to sort column ascending">Panel size</th> <th class="row_0 col_2 min-fablet sorting" tabindex="0" colspan="1" rowspan="1" aria-controls="tablefield-paragraph-2540-field_table-1" aria-label="Data: activate to sort column ascending">Data</th> </tr> </thead> <tbody> <tr class="odd" role="row"> <td class="row_3 col_0 all control" tabindex="0">CDK Profiler</td> <td class="row_3 col_1 min-fablet sorting_1">32</td> <td class="row_3 col_2 pdf min-fablet"><a class="pdf" href="https://www.reactionbiology.com/wp-content/uploads/2023/09/Profiler_PanQinase_CDK.pdf" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even" role="row"> <td class="row_6 col_0 all control" tabindex="0">Lipid Kinase Profiler</td> <td class="row_6 col_1 min-fablet sorting_1">14</td> <td class="row_6 col_2 pdf min-fablet"><a class="pdf" href="https://www.reactionbiology.com/wp-content/uploads/2023/09/target_specific_assays_biochem_v4.pdf" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd" role="row"> <td class="row_4 col_0 all control" tabindex="0">EGFR Mutant Profiler</td> <td class="row_4 col_1 min-fablet sorting_1">11</td> <td class="row_4 col_2 pdf min-fablet"><a class="pdf" href="https://www.reactionbiology.com/wp-content/uploads/2023/09/Mutant_Profiler_PanQinase_EGFR.pdf" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even" role="row"> <td class="row_5 col_0 all control" tabindex="0">KIT Mutant Profiler</td> <td class="row_5 col_1 min-fablet sorting_1">10</td> <td class="row_5 col_2 pdf min-fablet"><a class="pdf" href="https://www.reactionbiology.com/wp-content/uploads/2023/09/Mutant_Profiler_PanQinase_KIT.pdf" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd" role="row"> <td class="row_7 col_0 all control" tabindex="0">MET Mutant Profiler</td> <td class="row_7 col_1 min-fablet sorting_1">10</td> <td class="row_7 col_2 pdf min-fablet"><a class="pdf" href="https://www.reactionbiology.com/wp-content/uploads/2023/09/Mutant_Profiler_PanQinase_MET.pdf" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even" role="row"> <td class="row_8 col_0 all control" tabindex="0">RET Mutant Profiler</td> <td class="row_8 col_1 min-fablet sorting_1">10</td> <td class="row_8 col_2 pdf min-fablet"><a class="pdf" href="https://www.reactionbiology.com/wp-content/uploads/2023/09/Mutant_Profiler_PanQinase_RET.pdf" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="odd" role="row"> <td class="row_1 col_0 all control" tabindex="0">ABL1 Mutant Profiler</td> <td class="row_1 col_1 min-fablet sorting_1">9</td> <td class="row_1 col_2 pdf min-fablet"><a class="pdf" href="https://www.reactionbiology.com/wp-content/uploads/2023/09/Mutant_Profiler_PanQinase_ABL1.pdf" target="_blank" rel="noopener">Data sheet</a></td> </tr> <tr class="even" role="row"> <td class="row_2 col_0 all control" tabindex="0">ALK Mutant Profiler</td> <td class="row_2 col_1 min-fablet sorting_1">8</td> <td class="row_2 col_2 pdf min-fablet"><a class="pdf" href="https://www.reactionbiology.com/wp-content/uploads/2023/09/Mutant_Profiler_PanQinase_ALK.pdf" target="_blank" rel="noopener">Data sheet</a></td> </tr> </tbody> </table> </div> </div> </div> </div> </div></div><div id="kps-id4" class="paragraph paragraph--type--tab-container paragraph--view-mode--default"><div class="container center"><h2>Kinase Panel Screening Details</h2> <div class="tab-container"><ul class="tab-navigation"><li class="tab-active" data-id="#tab-kps-id441">Assay Formats</li><li data-id="#tab-kps-id442">Reproducibility</li><li data-id="#tab-kps-id443">Assay Setup (US facility) </li><li data-id="#tab-kps-id444">Assay Setup (German facility)</li><li data-id="#tab-kps-id445">Screening Schedule</li><li data-id="#tab-kps-id446">Why profiling with IC50 values?</li><li data-id="#tab-kps-id447">Selectivity and Toxicity</li></ul><div class="field field--name-field-paragraph field--type-entity-reference-revisions field--label-hidden field__items"><div id="tab-kps-id441" class="tab-content-active paragraph paragraph--type--tab-text-with-image paragraph--view-mode--default"><div class="field field--name-field-title field--type-string field--label-hidden field__items">Assay Formats</div><div class="tab-content"><div class="tab-content-wrapper"><div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"><div class="tab-content"> <div class="tab-content-wrapper"> <div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"> <div class="field__item"> <h4>HotSpot™ and ³³PanQinase™: two radiometric assay formats</h4> <p><img loading="lazy" decoding="async" class="aligncenter wp-image-1094" src="https://www.reactionbiology.com/wp-content/uploads/2023/06/191126_Mehdi_kinase-reaction.png" alt="" width="500" height="217" srcset="https://www.reactionbiology.com/wp-content/uploads/2023/06/191126_Mehdi_kinase-reaction.png 2000w, https://www.reactionbiology.com/wp-content/uploads/2023/06/191126_Mehdi_kinase-reaction-300x130.png 300w, https://www.reactionbiology.com/wp-content/uploads/2023/06/191126_Mehdi_kinase-reaction-1024x444.png 1024w, https://www.reactionbiology.com/wp-content/uploads/2023/06/191126_Mehdi_kinase-reaction-768x333.png 768w, https://www.reactionbiology.com/wp-content/uploads/2023/06/191126_Mehdi_kinase-reaction-1536x667.png 1536w, https://www.reactionbiology.com/wp-content/uploads/2023/06/191126_Mehdi_kinase-reaction-1080x469.png 1080w" sizes="(max-width: 500px) 100vw, 500px" /></p> <p>Reaction Biology offers two radiometric assay formats that are performed in our screening facilities located in Malvern, PA, USA, and Freiburg, Germany. Both assays are based on the transfer of ³³P-labelled phosphate from ATP to the kinase substrate. The methods, however, differ with respect to retention and detection of the phosphorylated substrates. Proteins and peptides in the HotSpot™ assay (performed in the US) are captured via spotting of the reaction mix on a filter membrane. The ³³PanQinase™ assay (performed in Germany) is performed with <span lang="EN-US" xml:lang="EN-US">ScintiPlate</span> microtiter plates, which are coated with scintillant for detection.</p> <h4>Lipid kinases are screened with ADP-Glo (Promega) at both facilities.</h4> </div> </div> </div> </div> </div></div></div></div><div id="tab-kps-id442" class=" paragraph paragraph--type--tab-text-with-image paragraph--view-mode--default"><div class="field field--name-field-title field--type-string field--label-hidden field__items">Reproducibility</div><div class="tab-content"><div class="tab-content-wrapper"><div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"><div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"> <div class="field__item"> <p style="float: left;"><img loading="lazy" decoding="async" class="wp-image-1115 size-medium alignleft" src="https://www.reactionbiology.com/wp-content/uploads/2023/06/reproducibility-panqinase-WT-profiler-300x203.png" alt="" width="300" height="203" srcset="https://www.reactionbiology.com/wp-content/uploads/2023/06/reproducibility-panqinase-WT-profiler-300x203.png 300w, https://www.reactionbiology.com/wp-content/uploads/2023/06/reproducibility-panqinase-WT-profiler-1024x692.png 1024w, https://www.reactionbiology.com/wp-content/uploads/2023/06/reproducibility-panqinase-WT-profiler-768x519.png 768w, https://www.reactionbiology.com/wp-content/uploads/2023/06/reproducibility-panqinase-WT-profiler-1080x730.png 1080w, https://www.reactionbiology.com/wp-content/uploads/2023/06/reproducibility-panqinase-WT-profiler.png 1136w" sizes="(max-width: 300px) 100vw, 300px" /></p> <p> </p> <p>The IC50 values of a BCR-ABL kinase inhibitor were determined for 320 wild type kinases in two independent experiments and compared. The high R<sup>2</sup> value shows a high correlation of data. IC50 value determination was performed with 6 compound concentrations in singlicate with the ³³PanQinase™ assay.</p> <div style="clear: both; height: 0; margin: 0;"></div> <p style="float: left;"><img loading="lazy" decoding="async" class="alignleft wp-image-1116 size-medium" src="https://www.reactionbiology.com/wp-content/uploads/2023/06/stauro-reproducibility-300x262.png" alt="" width="300" height="262" srcset="https://www.reactionbiology.com/wp-content/uploads/2023/06/stauro-reproducibility-300x262.png 300w, https://www.reactionbiology.com/wp-content/uploads/2023/06/stauro-reproducibility.png 550w" sizes="(max-width: 300px) 100vw, 300px" /></p> <p>The control compound Staurosporine was tested over the course of 6 months in 12 independent experiments. IC50 determination was performed with 10 compound concentrations in singlicate with the HotSpot™ assay.</p> </div> </div> </div></div></div></div><div id="tab-kps-id443" class=" paragraph paragraph--type--tab-text-with-image paragraph--view-mode--default"><div class="field field--name-field-title field--type-string field--label-hidden field__items">Assay Setup (US facility) </div><div class="tab-content"><div class="tab-content-wrapper"><div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"><div class="tab-content"> <div class="tab-content-wrapper"> <div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"> <div class="field__item"> <p><strong>Screening formats</strong>: 2 data point projects with 1 concentration in duplicates and 5 to 10-doses response curves.</p> <p><strong>Assays:</strong> Protein kinases are screened via radiometric HotSpot™ assay. Lipid kinases are screened via ADP-Glo (Promega) assay. The assay protocol for the HotSpot™ assay is available <a href="/assay-protocol-hotspot">here</a>.</p> <p><strong>ATP concentrations:</strong> 1mM, 1μM, 10μM, or apparent ATP-Km up to 100μM</p> <p><strong>Controls:</strong> No inhibitor (DMSO vehicle) control. For every kinase, we include the screening of one kinase-specific control compound in 10-dose IC50 format.</p> <p><strong>Timelines:</strong> Selectivity panel screening is performed twice per month. Reports are sent 2 to 3 weeks after the project start.</p> <p><strong>Screening dates: </strong>Upcoming selectivity panel screening dates are shown <a href="/services/kinase-assays/kinase-panel-screening/kinase-schedule-us-facility/">here</a>.</p> <p><strong>Report:</strong> The raw data, % enzyme activity and control compound IC50 values will be reported in Excel format. Assay conditions, target, and substrate information are available upon request. Requirements for this information should be noted prior to the commencement of the study.</p> <p><strong>Mapper:</strong> The results of the selectivity of compounds can be graphically presented with our <a href="/tools/kinase-mapper/">mapper tool</a>.</p> <p><strong>Compound requirements:</strong> In brief, for kinase panel profiling 100 ul of a 10 mM DMSO stock or solid material is needed. Shipping information can be found in our <a href="/faq/">FAQs</a>.</p> </div> </div> <div class="field field--name-field-pdf field--type-file field--label-hidden field__items"> <div class="field__item"><span class="file file--mime-application-vnd-openxmlformats-officedocument-spreadsheetml-sheet file--x-office-spreadsheet"> <a title="FAQ Assay Condition Form" href="https://www.reactionbiology.com/faq/" target="_blank" rel="noopener">Please see our FAQ page to access our assay condition form (US facility).</a></span></div> </div> </div> </div> </div></div></div></div><div id="tab-kps-id444" class=" paragraph paragraph--type--tab-text-with-image paragraph--view-mode--default"><div class="field field--name-field-title field--type-string field--label-hidden field__items">Assay Setup (German facility)</div><div class="tab-content"><div class="tab-content-wrapper"><div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"><div class="tab-content"> <div class="tab-content-wrapper"> <div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"> <div class="field__item"> <p><strong>Screening formats:</strong> 2 data point projects are performed with 1 concentration in duplicates or 2 concentrations in singlicates. IC50 projects are performed with 6 concentrations in singlicate.</p> <p><strong>Assays:</strong> Protein kinases are screened via radiometric ³³PanQinase™ assay. Lipid kinases are screened via ADP-Glo™ (Promega) assay. The assay protocol for the ³³PanQinase™ assay is available <a href="/assay-protocol-panqinase/">here</a>.</p> <p><strong>ATP concentrations:</strong> apparent ATP-K<sub>m</sub></p> <p><strong>Controls:</strong> DMSO only as full enzymatic activity control.</p> <p><strong>Timelines:</strong> Selectivity panel screening is performed once per month or on-demand. Reports are sent 10 business days after the project start.</p> <p><strong>Screening dates:</strong> Upcoming profiling dates are shown <a href="/services/kinase-assays/kinase-panel-screening/kinase-full-panel-schedule-german-facility/">here</a>.</p> <p><strong>Report</strong>: A detailed report will be provided including assay conditions, target, and substrate information. The raw data and % enzyme activity will be reported in Excel format including IC50 values and curve fitting, if applicable. Compound selectivity on wild type protein kinases will be graphically presented with the <a href="/tools/kinase-mapper/">mapper tool</a>.</p> <p><strong>Compound requirements: </strong>For testing with 1 concentration in duplicate, 1700 µl of a 100x stock solution is required. For testing with 2 concentrations in singlicate, 850 µl of a 100x stock solution of each concentration is required. For IC50 testing, 1000 µl of 100x stock solution is required. Solid material is also accepted.</p> </div> </div> <div class="field field--name-field-pdf field--type-file field--label-hidden field__items"> <div class="field__item"><span class="file file--mime-application-vnd-openxmlformats-officedocument-spreadsheetml-sheet file--x-office-spreadsheet"> <a title="FAQ Assay Condition Form" href="https://www.reactionbiology.com/faq/" target="_blank" rel="noopener">Please see our FAQ page to access our biochemical assay condition form (German facility) for further details on compound preparation and shipping.</a></span></div> </div> </div> </div> </div></div></div></div><div id="tab-kps-id445" class=" paragraph paragraph--type--tab-text-with-image paragraph--view-mode--default"><div class="field field--name-field-title field--type-string field--label-hidden field__items">Screening Schedule</div><div class="tab-content"><div class="tab-content-wrapper"><div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"><div class="tab-content"> <div class="tab-content-wrapper"> <div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"> <div class="field__item"> <p><strong>Selectivity kinase panels are screened bi-weekly or on a monthly basis</strong></p> <p>See the screening schedule of the US facility <a href="/services/kinase-assays/kinase-panel-screening/kinase-full-panel-schedule-us-facility/">here</a>.</p> <p>See the screening schedule of the German facility <a href="/services/kinase-assays/kinase-panel-screening/kinase-full-panel-schedule-german-facility/">here</a>.</p> <p> </p> <p><strong>Specialty kinase panels are screened on demand.</strong></p> </div> </div> </div> </div> </div></div></div></div><div id="tab-kps-id446" class=" paragraph paragraph--type--tab-text-with-image paragraph--view-mode--default"><div class="field field--name-field-title field--type-string field--label-hidden field__items">Why profiling with IC50 values?</div><div class="tab-content"><div class="tab-content-wrapper"><div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"><p><img loading="lazy" decoding="async" class="aligncenter size-full wp-image-1114" src="https://www.reactionbiology.com/wp-content/uploads/2023/06/IC50-profiler.png" alt="" width="2000" height="521" srcset="https://www.reactionbiology.com/wp-content/uploads/2023/06/IC50-profiler.png 2000w, https://www.reactionbiology.com/wp-content/uploads/2023/06/IC50-profiler-300x78.png 300w, https://www.reactionbiology.com/wp-content/uploads/2023/06/IC50-profiler-1024x267.png 1024w, https://www.reactionbiology.com/wp-content/uploads/2023/06/IC50-profiler-768x200.png 768w, https://www.reactionbiology.com/wp-content/uploads/2023/06/IC50-profiler-1536x400.png 1536w, https://www.reactionbiology.com/wp-content/uploads/2023/06/IC50-profiler-1080x281.png 1080w" sizes="(max-width: 2000px) 100vw, 2000px" /></p> <p>Example of an FLT3 inhibitor with ³³PanQinase™ assay: IC50 values of 320 wild type protein kinases are shown with values of lower than 10<sup>-4</sup>. IC50 value determination for selectivity profiling helps assess differences in the potency of a given compound and allows a precise judgment on the selectivity of kinase inhibitors.<br /> Only the targets with the lowest IC50 values are named.</p> <p>IC50 based profiling is designed to:</p> <ol type="a"> <li>Obtain an accurate guiding parameter for optimization of kinase selectivity during the medicinal chemical optimization phase</li> <li>Ensure that observed functional effects of a kinase inhibitor are not due to the inhibition of off-target-kinases and to identify potential adverse side effects of the drug</li> <li>Provide accurate comparison to a reference compound</li> </ol> </div></div></div></div><div id="tab-kps-id447" class=" paragraph paragraph--type--tab-text-with-image paragraph--view-mode--default"><div class="field field--name-field-title field--type-string field--label-hidden field__items">Selectivity and Toxicity</div><div class="tab-content"><div class="tab-content-wrapper"><div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"><div class="tab-content"> <div class="tab-content-wrapper"> <div class="clearfix text-formatted field field--name-field-text field--type-text-long field--label-hidden field__items"> <div class="field__item"> <p>Protein kinases share a common catalytic core and thus usually display sequence and structural similarity, which can result to a lack of selectivity and to off-target toxicity of drug candidates. The lack of selectivity can be beneficial but can also cause adverse toxicities which result in the discontinuation of promising drug candidates.</p> </div> </div> <div class="field field--name-field-pdf field--type-file field--label-hidden field__items"> <div class="field__item"><span class="file file--mime-application-pdf file--application-pdf"> <a title="2021_Grossman_Protein Kinase Inhibitors-selectivity or toxicity.pdf" href="https://www.reactionbiology.com/wp-content/uploads/2023/10/2021_Grossman_Protein-Kinase-Inhibitors-selectivity-or-toxicity1.pdf" target="_blank" rel="noopener" type="application/pdf; length=845635">Book chapter about selectivity and toxicity issues of protein kinase inhibitors</a></span></div> </div> </div> </div> </div></div></div></div></div></div></div></div><div id="kps-id5" class="paragraph paragraph--type--related-resources-reference paragraph--view-mode--default"><div class="container center"><h2>Related Resources</h2><div class="field--name-field-paragraph related-resources-reference-wrapper"><div class="paragraph--type--related-resource node--type-related-resource"><div class="related-resource-wrapper"><div class="field--name-field-image"><div class="field field--name-field-image field--type-image field--label-hidden field__items"><img src="https://www.reactionbiology.com/wp-content/uploads/2023/07/KinaseSelectivityPanelThumbnail.png" alt="Kinase Selectivity Panels " title="Kinase Selectivity Panels " typeof="foaf:Image" class="image-style-large"></div></div><div class="related-resource-text"> <div class="field--name-field-resource-category"> Info sheet </div> <div class="field--name-field-title"> <span class="field field--name-title field--type-string field--label-hidden"> Kinase Selectivity Panels </span> </div> <div class="field--name-field-download"> <span class="pdfpreview-image-wrapper"> <a href="https://www.reactionbiology.com/sites/default/files/PDF/Kinase%20Selectivity%20Panels.pdf" target="_blank">Download PDF</a> </span> </div> </div></div></div><div class="paragraph--type--related-resource node--type-related-resource"><div class="related-resource-wrapper"><div class="field--name-field-image"><div class="field field--name-field-image field--type-image field--label-hidden field__items"><img src="https://www.reactionbiology.com/wp-content/uploads/2023/06/natire_biotech_2011_thumb.png" alt="Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nature Biotechnology, 2011 " title="Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nature Biotechnology, 2011 " typeof="foaf:Image" class="image-style-large"></div></div><div class="related-resource-text"> <div class="field--name-field-resource-category"> Publication </div> <div class="field--name-field-title"> <span class="field field--name-title field--type-string field--label-hidden"> Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. 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