====== Tozasertib 0.1μM R07 exp414 ======
==== Mechanism of Action ====
Inhibits Aurora A,B,C kinases, blocks cytokinesis, also inhibits RIPK1 and blocks necroptosis
  * **<color #00a2e8>Class / Subclass 1:</color>** Cell Cycle / Cytokinesis Inhibitor
  * **<color #00a2e8>Class / Subclass 2:</color>** Signal Transduction / Kinase Inhibitor



==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Protein References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%Tozasertib%%
    * **<color #00a2e8>Synonyms:</color>** VX 680; MK-0457
    * **<color #00a2e8>CAS #:</color>** 639089-54-6
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/5494449|5494449]]
    * **<color #00a2e8>IUPAC:</color>** %%N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C23H28N8OS/c1-15-13-20(29-28-15)25-19-14-21(31-11-9-30(2)10-12-31)27-23(26-19)33-18-7-5-17(6-8-18)24-22(32)16-3-4-16/h5-8,13-14,16H,3-4,9-12H2,1-2H3,(H,24,32)(H2,25,26,27,28,29)
    * **<color #00a2e8>INCHI Key:</color>** GCIKSSRWRFVXBI-UHFFFAOYSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 464.6
    * **<color #00a2e8>Canonical SMILES:</color>** CC1=CC(=NN1)NC2=CC(=NC(=N2)SC3=CC=C(C=C3)NC(=O)C4CC4)N5CCN(CC5)C
    * **<color #00a2e8>Isomeric SMILES:</color>** N/A
    * **<color #00a2e8>Molecular Formula:</color>** C23H28N8OS
{{:chemogenomics:structures:chem-0247.svg?nolink}}
</panel>


<panel title='Protein Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** Toronto Research Chemicals
    * **<color #00a2e8>Catalog #:</color>** T700000
    * **<color #00a2e8>Lot #:</color>** 14-GHZ-9-1
</panel>


<panel title='Protein Characterization' collapsed='true'>
    * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+H)+ Calcd for C23H28N8OS 465.21795; found 465.21974
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** Tosazertib
    * **<color #00a2e8>Min:</color>** -23.2513; **<color #00a2e8>Max:</color>** 58.2889
{{:chemogenomics:dose_response:dr_407.png?nolink&500 |}}
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|< 300px 100px 200px >|
^ IC   ^ Concentration (µM) ^
| IC10  |N/A    |
| IC20  |2.9341    |
| IC30  |3.8568    |
| IC40  |5.3417    |
| IC50  |2.7487    |
| IC60  |N/A    |
| IC70  |N/A    |
| IC80  |N/A    |
| IC90  |N/A    |
\\ 
</panel>
</accordion>
==== Screen Summary ====
    * **<color #00a2e8>Round</color>**: 07
    * **<color #00a2e8>Dose</color>**: 100nM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: -0.1
    * **<color #00a2e8>Numbers of reads</color>**: 17969844


==== Screen Results ====


^Sensitive/Resistant hits (FDR<0.05)^CRANKS^Score Plot^Top 30 Genes^Screen Similarity^Top 30 Sensitive GO terms^Top 30 Resistant GO terms^
|0/75|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Tozasertib_0.1uM_Round-7_exp414.txt|Scores]]</color>|<button type="primary" size="sm" modal="ScorePlot">View</button>|<button type="primary" size="sm" modal="modal_hits">View</button>|<button type="primary" size="sm" modal="modal_screen_similarity">View</button>|<button type="default" size="sm" modal="modal_go_sensitive">View</button>|<button type="primary" size="sm" modal="modal_go_resistant">View</button>|
<modal id='ScorePlot' size='lg' title='Tozasertib 0.1μM R07 exp414'>
{{:chemogenomics:cranks_plots:exp414.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:U:UPF2|UPF2]]|-2.69|0.41|
|[[:human_genes:M:MGA|MGA]]|-2.46|0.41|
|[[:human_genes:C:CCDC147|CCDC147]]|-2.40|0.41|
|[[:human_genes:K:KEAP1|KEAP1]]|-2.28|0.41|
|[[:human_genes:P:PSMD11|PSMD11]]|-2.28|0.41|
|[[:human_genes:P:PRPF18|PRPF18]]|-2.27|0.41|
|[[:human_genes:T:TFPT|TFPT]]|-2.25|0.41|
|[[:human_genes:L:LRR1|LRR1]]|-2.24|0.51|
|[[:human_genes:T:TCOF1|TCOF1]]|-2.24|0.41|
|[[:human_genes:P:PPP2R2A|PPP2R2A]]|-2.23|0.41|
|[[:human_genes:T:TLR7|TLR7]]|-2.14|0.41|
|[[:human_genes:T:TMSB15B|TMSB15B]]|-2.12|0.66|
|[[:human_genes:M:MFI2|MFI2]]|-2.12|0.41|
|[[:human_genes:S:SAMM50|SAMM50]]|-2.12|0.41|
|[[:human_genes:T:TRIM46|TRIM46]]|-2.09|0.41|
|[[:human_genes:M:MCM5|MCM5]]|-2.06|0.65|
|[[:human_genes:C:CCDC24|CCDC24]]|-2.06|0.51|
|[[:human_genes:G:GPR137|GPR137]]|-2.05|0.41|
|[[:human_genes:E:ERGIC2|ERGIC2]]|-2.04|0.41|
|[[:human_genes:R:RPL13|RPL13]]|-2.04|0.71|
|[[:human_genes:W:WDR45|WDR45]]|-2.04|0.41|
|[[:human_genes:P:PSMD13|PSMD13]]|-2.04|0.51|
|[[:human_genes:N:NELFA|NELFA]]|-2.03|0.45|
|[[:human_genes:P:PPP2R1A|PPP2R1A]]|-2.03|0.41|
|[[:human_genes:Z:ZNF407|ZNF407]]|-2.02|0.41|
|[[:human_genes:N:NUTF2|NUTF2]]|-2.02|0.71|
|[[:human_genes:P:PHACTR3|PHACTR3]]|-2.01|0.52|
|[[:human_genes:I:IAPP|IAPP]]|-1.99|0.41|
|[[:human_genes:P:PUS7|PUS7]]|-1.98|0.51|
|[[:human_genes:D:DDX3Y|DDX3Y]]|-1.97|0.41|
|[[:human_genes:C:CEP78|CEP78]]|3.62|0.00|
|[[:human_genes:C:CEP152|CEP152]]|3.64|0.00|
|[[:human_genes:K:KIAA0586|KIAA0586]]|3.71|0.00|
|[[:human_genes:W:WBP11|WBP11]]|3.72|0.00|
|[[:human_genes:T:TUBD1|TUBD1]]|4.06|0.00|
|[[:human_genes:C:CEP44|CEP44]]|4.15|0.00|
|[[:human_genes:B:BUB3|BUB3]]|4.17|0.00|
|[[:human_genes:H:HYLS1|HYLS1]]|4.40|0.00|
|[[:human_genes:E:EIF4A1|EIF4A1]]|4.63|0.00|
|[[:human_genes:F:FOPNL|FOPNL]]|4.63|0.00|
|[[:human_genes:T:TUBE1|TUBE1]]|4.71|0.00|
|[[:human_genes:T:TP53|TP53]]|4.91|0.00|
|[[:human_genes:R:RTTN|RTTN]]|5.19|0.00|
|[[:human_genes:S:SCLT1|SCLT1]]|5.31|0.00|
|[[:human_genes:C:C16orf59|C16orf59]]|5.65|0.00|
|[[:human_genes:N:NIN|NIN]]|5.81|0.00|
|[[:human_genes:C:CEP76|CEP76]]|5.94|0.00|
|[[:human_genes:C:CEP128|CEP128]]|6.02|0.00|
|[[:human_genes:C:CASP2|CASP2]]|6.27|0.00|
|[[:human_genes:C:C14orf80|C14orf80]]|6.42|0.00|
|[[:human_genes:O:ODF2|ODF2]]|6.48|0.00|
|[[:human_genes:A:ANKRD26|ANKRD26]]|6.62|0.00|
|[[:human_genes:P:PIDD|PIDD]]|6.68|0.00|
|[[:human_genes:C:CEP120|CEP120]]|6.68|0.00|
|[[:human_genes:C:CRADD|CRADD]]|6.90|0.00|
|[[:human_genes:O:OFD1|OFD1]]|6.93|0.00|
|[[:human_genes:C:CCDC41|CCDC41]]|7.41|0.00|
|[[:human_genes:P:PIBF1|PIBF1]]|7.55|0.00|
|[[:human_genes:K:KIAA0753|KIAA0753]]|7.75|0.00|
|[[:human_genes:C:C2CD3|C2CD3]]|7.94|0.00|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp374|Latrunculin-B 10μM R07 exp374]]|0.251|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp349|Cytochalasin-B 5μM R07 exp349]]|0.223|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp80|RO-3307 4.7μM R02 exp80]]|0.132|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.064|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp343|Centrinone 0.5μM R07 exp343]]|0.063|<button type="primary" size="small" modal="5">View</button>|
|[[:results:exp485|GSK626616 14μM R08 exp485]]|0.062|<button type="primary" size="small" modal="6">View</button>|
|[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.056|<button type="primary" size="small" modal="7">View</button>|
|[[:results:exp527|Tanespimycin 14μM R08 exp527]]|0.056|<button type="primary" size="small" modal="8">View</button>|
|[[:results:exp199|Etoposide 0.3μM R05 exp199]]|0.055|<button type="primary" size="small" modal="9">View</button>|
|[[:results:exp360|Genistein 15μM R07 exp360]]|0.054|<button type="primary" size="small" modal="10">View</button>|
|[[:results:exp478|Doxorubicin 0.02μM R08 exp478]]|0.052|<button type="primary" size="small" modal="11">View</button>|
|[[:results:exp211|AICAR 240μM R05 exp211]]|0.051|<button type="primary" size="small" modal="12">View</button>|
</modal>


<modal id="1" size="lg" title="Latrunculin-B 10μM R07 exp374  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp374_vs_exp414.png?nolink |}}
</modal>

<modal id="2" size="lg" title="Cytochalasin-B 5μM R07 exp349  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp349_vs_exp414.png?nolink |}}
</modal>

<modal id="3" size="lg" title="RO-3307 4.7μM R02 exp80  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp414_vs_exp80.png?nolink |}}
</modal>

<modal id="4" size="lg" title="Hippuristanol 0.12μM R08 exp489 no dilution day6  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp414_vs_exp489.png?nolink |}}
</modal>

<modal id="5" size="lg" title="Centrinone 0.5μM R07 exp343  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp343_vs_exp414.png?nolink |}}
</modal>

<modal id="6" size="lg" title="GSK626616 14μM R08 exp485  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp414_vs_exp485.png?nolink |}}
</modal>

<modal id="7" size="lg" title="Hippuristanol 0.12μM R08 exp488  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp414_vs_exp488.png?nolink |}}
</modal>

<modal id="8" size="lg" title="Tanespimycin 14μM R08 exp527  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp414_vs_exp527.png?nolink |}}
</modal>

<modal id="9" size="lg" title="Etoposide 0.3μM R05 exp199  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp199_vs_exp414.png?nolink |}}
</modal>

<modal id="10" size="lg" title="Genistein 15μM R07 exp360  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp360_vs_exp414.png?nolink |}}
</modal>

<modal id="11" size="lg" title="Doxorubicin 0.02μM R08 exp478  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp414_vs_exp478.png?nolink |}}
</modal>

<modal id="12" size="lg" title="AICAR 240μM R05 exp211  vs  Tozasertib 0.1μM R07 exp414">
{{:chemogenomics:comparison_plots:exp211_vs_exp414.png?nolink |}}
</modal>



<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">No GO term hits below threshold. (FDR <0.05)</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">
^GO Term^Fold Change^Genes^
|centriole-centriole cohesion|184.21|ODF2,NIN,RTTN,CEP44|
|centriole replication|138.16|C2CD3,KIAA0753,OFD1,RTTN,CEP44,CEP152|
|DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrest|130.03|CRADD,PIDD1,CASP2,TP53|
|centriole assembly|106.96|C2CD3,KIAA0753,OFD1,RTTN,CEP44,CEP152|
|centrosome duplication|94.74|C2CD3,KIAA0753,OFD1,RTTN,CEP44,CEP152|
|centriole|67.67|C2CD3,KIAA0753,CEP83,OFD1,CEP120,ODF2,CEP128,CEP76,NIN,SCLT1,RTTN,CEP20,HYLS1,CEP44,TUBD1,KIAA0586,CEP152,CEP78|
|centrosome cycle|61.40|C2CD3,KIAA0753,OFD1,CEP120,ODF2,NIN,RTTN,TUBE1,CEP44,CEP152|
|microtubule organizing center organization|51.65|C2CD3,KIAA0753,OFD1,CEP120,ODF2,NIN,RTTN,TUBE1,CEP44,CEP152|
|cilium organization|20.53|C2CD3,KIAA0753,PIBF1,CEP83,OFD1,ODF2,SCLT1,RTTN,CEP20,HYLS1,KIAA0586,CEP78|
|centrosome|18.90|C2CD3,KIAA0753,PIBF1,CEP83,OFD1,CEP120,ANKRD26,ODF2,CEP128,CEP76,NIN,SCLT1,RTTN,TP53,TUBE1,CEP20,HYLS1,CEP44,KIAA0586,CEP152,CEP78|
|cilium assembly|16.86|C2CD3,KIAA0753,PIBF1,CEP83,OFD1,SCLT1,CEP20,HYLS1,KIAA0586|
|microtubule organizing center|15.10|C2CD3,KIAA0753,PIBF1,CEP83,OFD1,CEP120,ANKRD26,ODF2,CEP128,CEP76,NIN,SCLT1,RTTN,TP53,TUBE1,CEP20,HYLS1,CEP44,TUBD1,KIAA0586,CEP152,CEP78|
|microtubule cytoskeleton organization|13.35|C2CD3,KIAA0753,PIBF1,OFD1,CEP120,ODF2,NIN,RTTN,TUBE1,CEP20,CEP44,TUBD1,CEP152|
|plasma membrane bounded cell projection assembly|12.59|C2CD3,KIAA0753,PIBF1,CEP83,OFD1,SCLT1,CEP20,HYLS1,KIAA0586|
|cell projection assembly|12.22|C2CD3,KIAA0753,PIBF1,CEP83,OFD1,SCLT1,CEP20,HYLS1,KIAA0586|
|cilium|10.58|C2CD3,CEP83,OFD1,ODF2,CEP128,NIN,SCLT1,RTTN,CEP20,HYLS1,TUBD1,KIAA0586,CEP78|
|cell cycle process|10.14|C2CD3,KIAA0753,PIBF1,OFD1,CRADD,CEP120,PIDD1,ODF2,CASP2,NIN,RTTN,TP53,TUBE1,BUB3,CEP44,CEP152|
|microtubule-based process|9.22|C2CD3,KIAA0753,PIBF1,OFD1,CEP120,ODF2,NIN,RTTN,TUBE1,CEP20,CEP44,TUBD1,CEP152|
|organelle assembly|8.37|C2CD3,KIAA0753,PIBF1,CEP83,OFD1,SCLT1,RTTN,CEP20,HYLS1,CEP44,KIAA0586,CEP152|
</modal>