KU-0063794 3.8μM R02 exp71 [The Human Chemical-Genetic Interaction Map Project]

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====== KU-0063794 3.8μM R02 exp71 ======
==== Mechanism of Action ====
ATP-competitive mTORC1 and mTORC2 inhibitor
  * **<color #00a2e8>Class / Subclass 1:</color>** Proteostasis / mTOR inhibitor
  * **<color #00a2e8>Class / Subclass 2:</color>** Signal Transduction / Kinase Inhibitor



==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Compound References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%Ku-0063794%%
    * **<color #00a2e8>Synonyms:</color>** N/A
    * **<color #00a2e8>CAS #:</color>** 938440-64-3
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/16736978|16736978]]
    * **<color #00a2e8>IUPAC:</color>** %%[5-[2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]-4-morpholin-4-ylpyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C25H31N5O4/c1-16-13-30(14-17(2)34-16)25-27-23-20(24(28-25)29-8-10-33-11-9-29)5-6-21(26-23)18-4-7-22(32-3)19(12-18)15-31/h4-7,12,16-17,31H,8-11,13-15H2,1-3H3/t16-,17+
    * **<color #00a2e8>INCHI Key:</color>** RFSMUFRPPYDYRD-CALCHBBNSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 465.5
    * **<color #00a2e8>Canonical SMILES:</color>** CC1CN(CC(O1)C)C2=NC3=C(C=CC(=N3)C4=CC(=C(C=C4)OC)CO)C(=N2)N5CCOCC5
    * **<color #00a2e8>Isomeric SMILES:</color>** C[C@@H]1CN(C[C@@H](O1)C)C2=NC3=C(C=CC(=N3)C4=CC(=C(C=C4)OC)CO)C(=N2)N5CCOCC5
    * **<color #00a2e8>Molecular Formula:</color>** C25H31N5O4
{{:chemogenomics:structures:chem-0047.svg?nolink}}
</panel>


<panel title='Compound Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** Selleck Chemicals
    * **<color #00a2e8>Catalog #:</color>** S1226
    * **<color #00a2e8>Lot #:</color>** N/A
</panel>


<panel title='Compound Characterization' collapsed='true'>
    * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+H)+ Calcd for C25H31N5O4 466.24488; found 466.246
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** KU-0063794
    * **<color #00a2e8>Min:</color>** -18.4031; **<color #00a2e8>Max:</color>** 67.0870
{{:chemogenomics:dose_response:dr_12.png?nolink&500 |}}
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|< 300px 100px 200px >|
^ IC   ^ Concentration (µM) ^
| IC10  |N/A    |
| IC20  |1.9729    |
| IC30  |2.9378    |
| IC40  |4.0717    |
| IC50  |5.4936    |
| IC60  |N/A    |
| IC70  |N/A    |
| IC80  |N/A    |
| IC90  |N/A    |
\\ 
</panel>
</accordion>
==== Screen Summary ====
    * **<color #00a2e8>Round</color>**: 02
    * **<color #00a2e8>Dose</color>**: 3.8µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 3.3
    * **<color #00a2e8>Numbers of reads</color>**: 7908560


==== 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^
|4/3|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/KU-0063794_3.8uM_Round-2_exp71.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="default" size="sm" modal="modal_go_resistant">View</button>|
<modal id='ScorePlot' size='lg' title='KU-0063794 3.8μM R02 exp71'>
{{:chemogenomics:cranks_plots:exp71.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:U:UXS1|UXS1]]|-3.90|<0.01|
|[[:human_genes:R:RRAGA|RRAGA]]|-3.07|<0.01|
|[[:human_genes:L:LAMTOR2|LAMTOR2]]|-3.07|<0.01|
|[[:human_genes:C:CDK6|CDK6]]|-2.85|0.01|
|[[:human_genes:X:XPO1|XPO1]]|-2.69|0.61|
|[[:human_genes:C:CFAP45|CFAP45]]|-2.69|0.54|
|[[:human_genes:O:OR51B4|OR51B4]]|-2.59|0.11|
|[[:human_genes:S:SRBD1|SRBD1]]|-2.43|0.31|
|[[:human_genes:S:SOX4|SOX4]]|-2.40|0.31|
|[[:human_genes:E:ERCC2|ERCC2]]|-2.35|0.54|
|[[:human_genes:P:POTEF|POTEF]]|-2.35|0.16|
|[[:human_genes:L:LAS1L|LAS1L]]|-2.33|0.78|
|[[:human_genes:A:ACBD5|ACBD5]]|-2.25|0.24|
|[[:human_genes:K:KAT2A|KAT2A]]|-2.20|0.28|
|[[:human_genes:Q:QARS|QARS]]|-2.19|0.72|
|[[:human_genes:C:CCDC23|CCDC23]]|-2.18|0.37|
|[[:human_genes:B:BMP5|BMP5]]|-2.12|0.31|
|[[:human_genes:R:RPTN|RPTN]]|-2.11|0.31|
|[[:human_genes:C:CUTC|CUTC]]|-2.09|0.33|
|[[:human_genes:P:PSMD6|PSMD6]]|-2.08|0.65|
|[[:human_genes:D:DCAF7|DCAF7]]|-2.08|0.54|
|[[:human_genes:U:USP17L17|USP17L17]]|-2.07|0.78|
|[[:human_genes:I:IQGAP3|IQGAP3]]|-2.04|0.47|
|[[:human_genes:Z:ZBTB25|ZBTB25]]|-2.02|0.42|
|[[:human_genes:F:FBXO7|FBXO7]]|-2.01|0.42|
|[[:human_genes:P:PLEKHH3|PLEKHH3]]|-1.99|0.44|
|[[:human_genes:R:RFX1|RFX1]]|-1.98|0.44|
|[[:human_genes:R:RHEB|RHEB]]|-1.97|0.44|
|[[:human_genes:A:ALPK1|ALPK1]]|-1.96|0.44|
|[[:human_genes:A:ASH2L|ASH2L]]|-1.95|0.58|
|[[:human_genes:D:DNLZ|DNLZ]]|2.13|0.21|
|[[:human_genes:Z:ZFC3H1|ZFC3H1]]|2.15|0.24|
|[[:human_genes:C:CXorf56|CXorf56]]|2.15|0.24|
|[[:human_genes:Z:ZNF439|ZNF439]]|2.16|0.19|
|[[:human_genes:T:TMEM165|TMEM165]]|2.16|0.24|
|[[:human_genes:R:RPS11|RPS11]]|2.18|0.41|
|[[:human_genes:E:EGR2|EGR2]]|2.18|0.28|
|[[:human_genes:M:MARCH1|MARCH1]]|2.18|0.18|
|[[:human_genes:D:DARS2|DARS2]]|2.18|0.28|
|[[:human_genes:R:RSPH3|RSPH3]]|2.20|0.23|
|[[:human_genes:U:UTP6|UTP6]]|2.22|0.36|
|[[:human_genes:A:ADIPOR1|ADIPOR1]]|2.22|0.18|
|[[:human_genes:T:TAF1L|TAF1L]]|2.23|0.22|
|[[:human_genes:C:C6orf120|C6orf120]]|2.32|0.18|
|[[:human_genes:A:ABO|ABO]]|2.33|0.28|
|[[:human_genes:H:HK2|HK2]]|2.33|0.37|
|[[:human_genes:A:AFM|AFM]]|2.34|0.18|
|[[:human_genes:T:TAZ|TAZ]]|2.34|0.58|
|[[:human_genes:P:PPP5C|PPP5C]]|2.34|0.12|
|[[:human_genes:H:HIVEP2|HIVEP2]]|2.37|0.18|
|[[:human_genes:B:BTK|BTK]]|2.39|0.18|
|[[:human_genes:P:POLD2|POLD2]]|2.45|0.33|
|[[:human_genes:I:IPO9|IPO9]]|2.55|0.06|
|[[:human_genes:F:FIBP|FIBP]]|2.57|0.09|
|[[:human_genes:K:KIAA0195|KIAA0195]]|2.71|0.06|
|[[:human_genes:R:RPL36A-HNRNPH2|RPL36A-HNRNPH2]]|2.76|0.41|
|[[:human_genes:S:SEPSECS|SEPSECS]]|2.84|0.06|
|[[:human_genes:E:EDC4|EDC4]]|2.89|0.01|
|[[:human_genes:P:PPP3R1|PPP3R1]]|3.50|<0.01|
|[[:human_genes:P:PPP3CA|PPP3CA]]|3.80|<0.01|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp82|Torin1 0.08μM R02 exp82]]|0.071|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp29|Rapamycin 1μM R00 exp29]]|0.054|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp70|INK128 0.2μM R02 exp70]]|0.094|<button type="primary" size="small" modal="3">View</button>|
</modal>


<modal id="1" size="lg" title="KU-0063794 3.8μM R02 exp71  vs  Torin1 0.08μM R02 exp82">
{{:chemogenomics:comparison_plots:exp71_vs_exp82.png?nolink |}}
</modal>

<modal id="2" size="lg" title="KU-0063794 3.8μM R02 exp71  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp29_vs_exp71.png?nolink |}}
</modal>

<modal id="3" size="lg" title="INK128 0.2μM R02 exp70  vs  KU-0063794 3.8μM R02 exp71">
{{:chemogenomics:comparison_plots:exp70_vs_exp71.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">No GO term hits below threshold. (FDR <0.05)</modal>