UMK57 1μM R01 exp59 [The Human Chemical-Genetic Interaction Map Project]

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====== UMK57 1μM R01 exp59 ======
==== Mechanism of Action ====
Potentiates kinesin-13 (MCAK), destabilizes kinetochore-MT attachment, suppresses chromosome mis-segregation
  * **<color #00a2e8>Class / Subclass 1:</color>** Cell Cycle / Mitotic Inhibitor
  * **<color #00a2e8>Class / Subclass 2:</color>** Organelle Function / Cytoskeletal Inhibitor



==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Protein References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%5-(4-Methylphenyl)-4-pyrrolidinylthiopheno[2,3-d]pyrimidine%%
    * **<color #00a2e8>Synonyms:</color>** N/A
    * **<color #00a2e8>CAS #:</color>** 342595-74-8
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/693939|693939]]
    * **<color #00a2e8>IUPAC:</color>** %%5-(4-methylphenyl)-4-pyrrolidin-1-ylthieno[2,3-d]pyrimidine%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C17H17N3S/c1-12-4-6-13(7-5-12)14-10-21-17-15(14)16(18-11-19-17)20-8-2-3-9-20/h4-7,10-11H,2-3,8-9H2,1H3
    * **<color #00a2e8>INCHI Key:</color>** VOAWQTDHSSKEKA-UHFFFAOYSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 295.4
    * **<color #00a2e8>Canonical SMILES:</color>** CC1=CC=C(C=C1)C2=CSC3=NC=NC(=C23)N4CCCC4
    * **<color #00a2e8>Isomeric SMILES:</color>** N/A
    * **<color #00a2e8>Molecular Formula:</color>** C17H17N3S
{{:chemogenomics:structures:chem-0039.svg?nolink}}
</panel>


<panel title='Protein Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** In house - University of Montreal - Chemistry Platform
    * **<color #00a2e8>Catalog #:</color>** N/A
    * **<color #00a2e8>Lot #:</color>** N/A
</panel>


<panel title='Protein Characterization' collapsed='true'>
    * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** [M+H]+ Calcd for C17H18N3S 296.1216; found  296.1142
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** UMK57
    * **<color #00a2e8>Min:</color>** -2.8530; **<color #00a2e8>Max:</color>** 75.4945
{{:chemogenomics:dose_response:dr_159.png?nolink&500 |}}
\\ 
\\ 
\\ 
\\ 
|< 300px 100px 200px >|
^ IC   ^ Concentration (µM) ^
| IC10  |N/A    |
| IC20  |0.3698    |
| IC30  |0.6436    |
| IC40  |1.0136    |
| IC50  |1.5379    |
| IC60  |N/A    |
| IC70  |N/A    |
| IC80  |N/A    |
| IC90  |N/A    |
\\ 
</panel>
</accordion>
==== Screen Summary ====
    * **<color #00a2e8>Round</color>**: 01
    * **<color #00a2e8>Dose</color>**: 1µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 5.2
    * **<color #00a2e8>Numbers of reads</color>**: 15049192


==== 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^
|27/49|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/UMK57_1uM_Round-1_exp59.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='UMK57 1μM R01 exp59'>
{{:chemogenomics:cranks_plots:exp59.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:D:DLGAP5|DLGAP5]]|-3.66|<0.01|
|[[:human_genes:Y:YPEL5|YPEL5]]|-3.46|<0.01|
|[[:human_genes:A:ARID4B|ARID4B]]|-3.31|<0.01|
|[[:human_genes:W:WDR61|WDR61]]|-3.27|0.02|
|[[:human_genes:A:ASPM|ASPM]]|-3.17|0.03|
|[[:human_genes:P:PDS5B|PDS5B]]|-3.10|0.01|
|[[:human_genes:T:TRIP13|TRIP13]]|-3.09|0.01|
|[[:human_genes:B:BRD1|BRD1]]|-3.08|<0.01|
|[[:human_genes:R:RNF111|RNF111]]|-3.06|<0.01|
|[[:human_genes:G:GTSE1|GTSE1]]|-2.98|0.02|
|[[:human_genes:P:PCGF1|PCGF1]]|-2.96|0.01|
|[[:human_genes:I:IPO11|IPO11]]|-2.92|0.03|
|[[:human_genes:I:ITPK1|ITPK1]]|-2.86|0.03|
|[[:human_genes:C:CNOT2|CNOT2]]|-2.83|0.03|
|[[:human_genes:N:NELFE|NELFE]]|-2.76|0.03|
|[[:human_genes:U:UBE2H|UBE2H]]|-2.74|0.03|
|[[:human_genes:W:WDR26|WDR26]]|-2.74|0.05|
|[[:human_genes:Z:ZNF367|ZNF367]]|-2.70|0.03|
|[[:human_genes:R:RBM26|RBM26]]|-2.62|0.04|
|[[:human_genes:M:MSI2|MSI2]]|-2.60|0.03|
|[[:human_genes:N:NMRK2|NMRK2]]|-2.58|0.05|
|[[:human_genes:G:GAK|GAK]]|-2.56|0.03|
|[[:human_genes:T:TCF4|TCF4]]|-2.54|0.03|
|[[:human_genes:P:PPIL1|PPIL1]]|-2.54|0.10|
|[[:human_genes:I:IKZF2|IKZF2]]|-2.54|0.03|
|[[:human_genes:M:MAFF|MAFF]]|-2.53|0.19|
|[[:human_genes:C:CTTNBP2|CTTNBP2]]|-2.53|0.05|
|[[:human_genes:D:DNAJC9|DNAJC9]]|-2.51|0.04|
|[[:human_genes:C:CD2BP2|CD2BP2]]|-2.45|0.22|
|[[:human_genes:R:RING1|RING1]]|-2.44|0.05|
|[[:human_genes:T:TLE4|TLE4]]|2.82|0.03|
|[[:human_genes:C:CYB5R4|CYB5R4]]|2.83|<0.01|
|[[:human_genes:A:ATXN7L3|ATXN7L3]]|2.83|0.01|
|[[:human_genes:C:C21orf140|C21orf140]]|2.84|0.03|
|[[:human_genes:L:LDLR|LDLR]]|2.84|<0.01|
|[[:human_genes:C:CBX3|CBX3]]|2.87|<0.01|
|[[:human_genes:S:SP3|SP3]]|2.87|0.01|
|[[:human_genes:K:KHDRBS1|KHDRBS1]]|2.88|0.01|
|[[:human_genes:K:KIFC1|KIFC1]]|2.88|<0.01|
|[[:human_genes:P:PPP1R2|PPP1R2]]|2.94|<0.01|
|[[:human_genes:A:ARIH1|ARIH1]]|3.02|0.01|
|[[:human_genes:A:ATP1A1|ATP1A1]]|3.05|<0.01|
|[[:human_genes:P:PPP6R3|PPP6R3]]|3.05|<0.01|
|[[:human_genes:S:SLC25A51|SLC25A51]]|3.10|<0.01|
|[[:human_genes:S:SETDB1|SETDB1]]|3.14|<0.01|
|[[:human_genes:A:ATF7IP|ATF7IP]]|3.18|<0.01|
|[[:human_genes:P:PPP2R4|PPP2R4]]|3.37|<0.01|
|[[:human_genes:A:AMBRA1|AMBRA1]]|3.39|<0.01|
|[[:human_genes:K:KIF2A|KIF2A]]|3.41|<0.01|
|[[:human_genes:M:MAPRE1|MAPRE1]]|3.58|<0.01|
|[[:human_genes:I:ID3|ID3]]|3.59|<0.01|
|[[:human_genes:C:CCNF|CCNF]]|3.82|<0.01|
|[[:human_genes:T:TP53|TP53]]|3.86|<0.01|
|[[:human_genes:P:PPME1|PPME1]]|4.11|<0.01|
|[[:human_genes:T:TIPRL|TIPRL]]|4.15|<0.01|
|[[:human_genes:K:KIF2C|KIF2C]]|4.44|<0.01|
|[[:human_genes:A:ATAT1|ATAT1]]|5.14|<0.01|
|[[:human_genes:P:PPP2R1A|PPP2R1A]]|5.14|<0.01|
|[[:human_genes:L:LCMT1|LCMT1]]|5.73|<0.01|
|[[:human_genes:K:KIF18B|KIF18B]]|7.13|<0.01|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp60|Vinblastine 0.002μM R01 exp60]]|0.126|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp190|Vincristine 0.0005μM R04 exp190]]|0.07|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp217|Mdivi-1 15μM R05 exp217]]|0.216|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp460|BML-284 0.09μM R08 exp460]]|0.172|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp106|UM131593 0.2μM R03 exp106]]|0.14|<button type="primary" size="small" modal="5">View</button>|
|[[:results:exp312|2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312]]|0.13|<button type="primary" size="small" modal="6">View</button>|
|[[:results:exp46|HMS-I1 1μM R01 exp46]]|0.12|<button type="primary" size="small" modal="7">View</button>|
|[[:results:exp517|Quercetin 20μM R08 exp517]]|0.105|<button type="primary" size="small" modal="8">View</button>|
|[[:results:exp67|BVD-523 15μM R02 exp67]]|0.098|<button type="primary" size="small" modal="9">View</button>|
|[[:results:exp179|Combretastatin A4 0.002 to 0.003μM day4 R04 exp179]]|0.096|<button type="primary" size="small" modal="10">View</button>|
|[[:results:exp215|Colchicine 0.009μM R05 exp215]]|0.085|<button type="primary" size="small" modal="11">View</button>|
|[[:results:exp228|Demecolcine 0.03μM R05 exp228]]|0.081|<button type="primary" size="small" modal="12">View</button>|
|[[:results:exp311|2-Methoxyestradiol 0.55 to 0.75μM  on day4 R07 exp311]]|0.08|<button type="primary" size="small" modal="13">View</button>|
|[[:results:exp103|Taxol 0.004μM R03 exp103]]|0.078|<button type="primary" size="small" modal="14">View</button>|
|[[:results:exp184|Ixabepilone 0.004 to 0.005μM on day4 R04 exp184]]|0.074|<button type="primary" size="small" modal="15">View</button>|
|[[:results:exp310|2-Methoxyestradiol 0.55μM R07 exp310]]|0.074|<button type="primary" size="small" modal="16">View</button>|
|[[:results:exp80|RO-3307 4.7μM R02 exp80]]|0.069|<button type="primary" size="small" modal="17">View</button>|
|[[:results:exp500|LY2090314 0.003μM R08 exp500 no dilution day6]]|0.06|<button type="primary" size="small" modal="18">View</button>|
|[[:results:exp502|Milciclib 2μM R08 exp502]]|0.058|<button type="primary" size="small" modal="19">View</button>|
|[[:results:exp175|3-Bromopyruvate 7μM R04 exp175]]|0.058|<button type="primary" size="small" modal="20">View</button>|
|[[:results:exp329|Hydroxyurea 100μM R07 exp329]]|0.055|<button type="primary" size="small" modal="21">View</button>|
|[[:results:exp78|Pterostilbene 16μM R02 exp78]]|0.054|<button type="primary" size="small" modal="22">View</button>|
|[[:results:exp45|Docetaxel 0.002μM R01 exp45]]|0.054|<button type="primary" size="small" modal="23">View</button>|
|[[:results:exp529|Thimerosal 0.85μM R08 exp529]]|0.053|<button type="primary" size="small" modal="24">View</button>|
|[[:results:exp231|Epothilone-B 0.0015μM R05 exp231]]|0.053|<button type="primary" size="small" modal="25">View</button>|
|[[:results:exp3|Actinomycin-D 0.001μM R00 exp3]]|0.052|<button type="primary" size="small" modal="26">View</button>|
|[[:results:exp290|LLY-283 2.6μM R06 exp290]]|0.051|<button type="primary" size="small" modal="27">View</button>|
</modal>


<modal id="1" size="lg" title="UMK57 1μM R01 exp59  vs  Vinblastine 0.002μM R01 exp60">
{{:chemogenomics:comparison_plots:exp59_vs_exp60.png?nolink |}}
</modal>

<modal id="2" size="lg" title="UMK57 1μM R01 exp59  vs  Vincristine 0.0005μM R04 exp190">
{{:chemogenomics:comparison_plots:exp190_vs_exp59.png?nolink |}}
</modal>

<modal id="3" size="lg" title="Mdivi-1 15μM R05 exp217  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp217_vs_exp59.png?nolink |}}
</modal>

<modal id="4" size="lg" title="BML-284 0.09μM R08 exp460  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp460_vs_exp59.png?nolink |}}
</modal>

<modal id="5" size="lg" title="UM131593 0.2μM R03 exp106  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp106_vs_exp59.png?nolink |}}
</modal>

<modal id="6" size="lg" title="2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp312_vs_exp59.png?nolink |}}
</modal>

<modal id="7" size="lg" title="HMS-I1 1μM R01 exp46  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp46_vs_exp59.png?nolink |}}
</modal>

<modal id="8" size="lg" title="Quercetin 20μM R08 exp517  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp517_vs_exp59.png?nolink |}}
</modal>

<modal id="9" size="lg" title="BVD-523 15μM R02 exp67  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp59_vs_exp67.png?nolink |}}
</modal>

<modal id="10" size="lg" title="Combretastatin A4 0.002 to 0.003μM day4 R04 exp179  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp179_vs_exp59.png?nolink |}}
</modal>

<modal id="11" size="lg" title="Colchicine 0.009μM R05 exp215  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp215_vs_exp59.png?nolink |}}
</modal>

<modal id="12" size="lg" title="Demecolcine 0.03μM R05 exp228  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp228_vs_exp59.png?nolink |}}
</modal>

<modal id="13" size="lg" title="2-Methoxyestradiol 0.55 to 0.75μM  on day4 R07 exp311  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp311_vs_exp59.png?nolink |}}
</modal>

<modal id="14" size="lg" title="Taxol 0.004μM R03 exp103  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp103_vs_exp59.png?nolink |}}
</modal>

<modal id="15" size="lg" title="Ixabepilone 0.004 to 0.005μM on day4 R04 exp184  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp184_vs_exp59.png?nolink |}}
</modal>

<modal id="16" size="lg" title="2-Methoxyestradiol 0.55μM R07 exp310  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp310_vs_exp59.png?nolink |}}
</modal>

<modal id="17" size="lg" title="RO-3307 4.7μM R02 exp80  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp59_vs_exp80.png?nolink |}}
</modal>

<modal id="18" size="lg" title="LY2090314 0.003μM R08 exp500 no dilution day6  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp500_vs_exp59.png?nolink |}}
</modal>

<modal id="19" size="lg" title="Milciclib 2μM R08 exp502  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp502_vs_exp59.png?nolink |}}
</modal>

<modal id="20" size="lg" title="3-Bromopyruvate 7μM R04 exp175  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp175_vs_exp59.png?nolink |}}
</modal>

<modal id="21" size="lg" title="Hydroxyurea 100μM R07 exp329  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp329_vs_exp59.png?nolink |}}
</modal>

<modal id="22" size="lg" title="Pterostilbene 16μM R02 exp78  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp59_vs_exp78.png?nolink |}}
</modal>

<modal id="23" size="lg" title="Docetaxel 0.002μM R01 exp45  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp45_vs_exp59.png?nolink |}}
</modal>

<modal id="24" size="lg" title="Thimerosal 0.85μM R08 exp529  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp529_vs_exp59.png?nolink |}}
</modal>

<modal id="25" size="lg" title="Epothilone-B 0.0015μM R05 exp231  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp231_vs_exp59.png?nolink |}}
</modal>

<modal id="26" size="lg" title="Actinomycin-D 0.001μM R00 exp3  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp3_vs_exp59.png?nolink |}}
</modal>

<modal id="27" size="lg" title="LLY-283 2.6μM R06 exp290  vs  UMK57 1μM R01 exp59">
{{:chemogenomics:comparison_plots:exp290_vs_exp59.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^
|microtubule plus-end|71.99|KIF18B,KIF2C,MAPRE1|
|regulation of phosphoprotein phosphatase activity|51.34|TIPRL,PTPA,PPP6R3,PPP1R2|
|kinesin complex|50.17|KIF18B,KIF2C,KIF2A,KIFC1|
|regulation of phosphatase activity|38.73|TIPRL,PTPA,PPP6R3,PPP1R2|
|regulation of protein dephosphorylation|38.33|TIPRL,AMBRA1,PTPA,PPP6R3,PPP1R2|
|microtubule motor activity|33.45|KIF18B,KIF2C,KIF2A,KIFC1|
|protein phosphatase regulator activity|32.85|PPP2R1A,PPME1,PTPA,PPP6R3,PPP1R2|
|phosphatase regulator activity|28.74|PPP2R1A,PPME1,PTPA,PPP6R3,PPP1R2|
|regulation of dephosphorylation|27.87|TIPRL,AMBRA1,PTPA,PPP6R3,PPP1R2|
|mitotic sister chromatid segregation|24.71|KIF18B,PPP2R1A,KIF2C,MAPRE1,KIF2A,KIFC1|
|sister chromatid segregation|24.00|KIF18B,PPP2R1A,KIF2C,MAPRE1,KIF2A,KIFC1|
|protein phosphatase binding|20.29|PPME1,TP53,AMBRA1,PTPA,PPP6R3|
|mitotic nuclear division|17.14|KIF18B,KIF2C,MAPRE1,KIF2A,KIFC1|
|nuclear chromosome segregation|15.33|KIF18B,PPP2R1A,KIF2C,MAPRE1,KIF2A,KIFC1|
|mitotic cell cycle process|12.94|KIF18B,LCMT1,PPP2R1A,KIF2C,PPME1,TP53,CCNF,MAPRE1,KIF2A,PTPA,KIFC1,KHDRBS1|
|mitotic cell cycle|11.11|KIF18B,LCMT1,PPP2R1A,KIF2C,PPME1,TP53,CCNF,MAPRE1,KIF2A,PTPA,KIFC1,KHDRBS1|
|spindle|9.35|KIF18B,ATAT1,KIF2C,MAPRE1,KIF2A,KIFC1,CBX3|
|microtubule cytoskeleton organization|8.24|KIF18B,PPP2R1A,ATAT1,KIF2C,MAPRE1,KIF2A,PTPA,KIFC1|
|cell cycle process|7.64|KIF18B,LCMT1,PPP2R1A,KIF2C,PPME1,TP53,CCNF,MAPRE1,KIF2A,PTPA,KIFC1,KHDRBS1|
</modal>