GSK2606414 1μM R05 exp236 [The Human Chemical-Genetic Interaction Map Project]

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====== GSK2606414 1μM R05 exp236 ======
==== Mechanism of Action ====
Inhibits PERK, also KIT receptor
  * **<color #00a2e8>Class / Subclass 1:</color>** Signal Transduction / Kinase Inhibitor




==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Compound References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%CID 53469448%%
    * **<color #00a2e8>Synonyms:</color>** N/A
    * **<color #00a2e8>CAS #:</color>** 1337531-36-8
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/53469448|53469448]]
    * **<color #00a2e8>IUPAC:</color>** %%1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C24H20F3N5O/c1-31-12-18(21-22(28)29-13-30-23(21)31)15-5-6-19-16(11-15)7-8-32(19)20(33)10-14-3-2-4-17(9-14)24(25,26)27/h2-6,9,11-13H,7-8,10H2,1H3,(H2,28,29,30)
    * **<color #00a2e8>INCHI Key:</color>** SIXVRXARNAVBTC-UHFFFAOYSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 451.4
    * **<color #00a2e8>Canonical SMILES:</color>** CN1C=C(C2=C(N=CN=C21)N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F
    * **<color #00a2e8>Isomeric SMILES:</color>** N/A
    * **<color #00a2e8>Molecular Formula:</color>** C24H20F3N5O
{{:chemogenomics:structures:chem-0141.svg?nolink}}
</panel>


<panel title='Compound Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** N/A
    * **<color #00a2e8>Catalog #:</color>** N/A
    * **<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 C21H21F3N5O 452.1693; found 452.1682
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** GSK2606414
    * **<color #00a2e8>Min:</color>** -5.0193; **<color #00a2e8>Max:</color>** 14.8932
{{:chemogenomics:dose_response:dr_224.png?nolink&500 |}}
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|< 300px 100px 200px >|
^ IC   ^ Concentration (µM) ^
| IC10  |N/A    |
| IC20  |N/A    |
| IC30  |N/A    |
| IC40  |N/A    |
| IC50  |N/A    |
| IC60  |N/A    |
| IC70  |N/A    |
| IC80  |N/A    |
| IC90  |N/A    |
\\ 
</panel>
</accordion>
==== Screen Summary ====
    * **<color #00a2e8>Round</color>**: 05
    * **<color #00a2e8>Dose</color>**: 1µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 6.8
    * **<color #00a2e8>Numbers of reads</color>**: 13642122


==== 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^
|1/1|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/GSK2606414_1uM_Round-5_exp236.txt|Scores]]</color>|<button type="primary" size="sm" modal="ScorePlot">View</button>|<button type="primary" size="sm" modal="modal_hits">View</button>|<button type="default" size="sm" modal="modal_screen_similarity">View</button>|<button type="primary" 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='GSK2606414 1μM R05 exp236'>
{{:chemogenomics:cranks_plots:exp236.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:T:TTC37|TTC37]]|-3.12|0.03|
|[[:human_genes:A:ASB3|ASB3]]|-2.63|0.07|
|[[:human_genes:M:MBTPS2|MBTPS2]]|-2.61|0.07|
|[[:human_genes:D:DEXI|DEXI]]|-2.50|0.08|
|[[:human_genes:F:FRRS1|FRRS1]]|-2.49|0.15|
|[[:human_genes:R:RHOA|RHOA]]|-2.48|0.08|
|[[:human_genes:M:MCM9|MCM9]]|-2.37|0.23|
|[[:human_genes:S:SREK1|SREK1]]|-2.21|0.23|
|[[:human_genes:P:PCYT1A|PCYT1A]]|-2.20|0.23|
|[[:human_genes:M:MBTPS1|MBTPS1]]|-2.19|0.36|
|[[:human_genes:H:HAUS8|HAUS8]]|-2.19|0.23|
|[[:human_genes:C:CDIPT|CDIPT]]|-2.17|0.36|
|[[:human_genes:C:C20orf96|C20orf96]]|-2.17|0.23|
|[[:human_genes:C:CTU1|CTU1]]|-2.16|0.23|
|[[:human_genes:F:FOXJ3|FOXJ3]]|-2.15|0.23|
|[[:human_genes:A:AGMAT|AGMAT]]|-2.13|0.23|
|[[:human_genes:H:HMBS|HMBS]]|-2.12|0.32|
|[[:human_genes:P:PPHLN1|PPHLN1]]|-2.12|0.32|
|[[:human_genes:P:PMM2|PMM2]]|-2.07|0.31|
|[[:human_genes:E:EPT1|EPT1]]|-2.06|0.31|
|[[:human_genes:D:DNAJC5G|DNAJC5G]]|-2.05|0.31|
|[[:human_genes:E:EEF2|EEF2]]|-2.04|0.72|
|[[:human_genes:F:FBXW7|FBXW7]]|-2.04|0.31|
|[[:human_genes:L:LEO1|LEO1]]|-2.03|0.36|
|[[:human_genes:F:FTSJ1|FTSJ1]]|-2.03|0.31|
|[[:human_genes:S:SOD1|SOD1]]|-2.01|0.57|
|[[:human_genes:A:ARMS2|ARMS2]]|-2.01|0.32|
|[[:human_genes:E:EIF2A|EIF2A]]|-1.97|0.36|
|[[:human_genes:F:FAM219A|FAM219A]]|-1.95|0.36|
|[[:human_genes:S:SCN10A|SCN10A]]|-1.95|0.36|
|[[:human_genes:D:DDTL|DDTL]]|1.98|0.48|
|[[:human_genes:C:C4orf33|C4orf33]]|1.98|0.48|
|[[:human_genes:A:AUP1|AUP1]]|2.00|0.58|
|[[:human_genes:C:C21orf91|C21orf91]]|2.02|0.49|
|[[:human_genes:A:ARCN1|ARCN1]]|2.02|0.58|
|[[:human_genes:S:STX8|STX8]]|2.04|0.58|
|[[:human_genes:A:ATXN2|ATXN2]]|2.05|0.48|
|[[:human_genes:P:PLK2|PLK2]]|2.06|0.47|
|[[:human_genes:C:CCDC58|CCDC58]]|2.06|0.48|
|[[:human_genes:P:PLSCR2|PLSCR2]]|2.07|0.47|
|[[:human_genes:F:FAM13A|FAM13A]]|2.10|0.47|
|[[:human_genes:P:PAN2|PAN2]]|2.10|0.47|
|[[:human_genes:G:GLTSCR2|GLTSCR2]]|2.11|0.58|
|[[:human_genes:R:RPS2|RPS2]]|2.12|0.47|
|[[:human_genes:R:RPS14|RPS14]]|2.15|0.58|
|[[:human_genes:N:NFATC3|NFATC3]]|2.16|0.48|
|[[:human_genes:S:SNRNP70|SNRNP70]]|2.17|0.58|
|[[:human_genes:F:FAM231B|FAM231B]]|2.21|0.47|
|[[:human_genes:M:MARVELD1|MARVELD1]]|2.24|0.69|
|[[:human_genes:R:RBM39|RBM39]]|2.25|0.67|
|[[:human_genes:T:TSPY8|TSPY8]]|2.26|0.69|
|[[:human_genes:O:OR4A16|OR4A16]]|2.30|0.47|
|[[:human_genes:U:UGGT1|UGGT1]]|2.35|0.47|
|[[:human_genes:L:LLGL1|LLGL1]]|2.39|0.47|
|[[:human_genes:C:CDC73|CDC73]]|2.41|0.48|
|[[:human_genes:X:XAB2|XAB2]]|2.43|0.69|
|[[:human_genes:C:CKAP5|CKAP5]]|2.44|0.58|
|[[:human_genes:C:COPB1|COPB1]]|2.57|0.48|
|[[:human_genes:U:UTP6|UTP6]]|2.82|0.47|
|[[:human_genes:D:DNAJC30|DNAJC30]]|3.04|0.04|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
No correlation data above threshold. (correlation > 0.05)
</modal>


<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">
^GO Term^Fold Change^Genes^
|regulation of cholesterol biosynthetic process|115.07|MBTPS2,MBTPS1,SOD1|
|regulation of sterol biosynthetic process|115.07|MBTPS2,MBTPS1,SOD1|
|ER-nucleus signaling pathway|73.97|MBTPS2,MBTPS1,EIF2A|
</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">No GO term hits below threshold. (FDR <0.05)</modal>