====== GSK343 3μM R03 exp124 ======
==== Mechanism of Action ====
Inhibits EZH1 catalytic subunit of PRC2 histone methyltransferase (H3K27me3)
  * **<color #00a2e8>Class / Subclass 1:</color>** Gene Regulation / Epigenetic Inhibitor




==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Protein References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide%%
    * **<color #00a2e8>Synonyms:</color>** N/A
    * **<color #00a2e8>CAS #:</color>** 1346704-33-3
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/71268957|71268957]]
    * **<color #00a2e8>IUPAC:</color>** %%N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)
    * **<color #00a2e8>INCHI Key:</color>** ULNXAWLQFZMIHX-UHFFFAOYSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 541.7
    * **<color #00a2e8>Canonical SMILES:</color>** CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C
    * **<color #00a2e8>Isomeric SMILES:</color>** N/A
    * **<color #00a2e8>Molecular Formula:</color>** C31H39N7O2
{{:chemogenomics:structures:chem-0077.svg?nolink}}
</panel>


<panel title='Protein Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** Structural Genomics Consortium
    * **<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 C31H39N7O2 542.3238; found 542.3251
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** GSK343
    * **<color #00a2e8>Min:</color>** -1.8961; **<color #00a2e8>Max:</color>** 98.3550
{{:chemogenomics:dose_response:dr_82.png?nolink&500 |}}
\\ 
\\ 
\\ 
\\ 
|< 300px 100px 200px >|
^ IC   ^ Concentration (µM) ^
| IC10  |N/A    |
| IC20  |1.9378    |
| IC30  |2.9381    |
| IC40  |4.1327    |
| IC50  |5.6521    |
| IC60  |N/A    |
| IC70  |N/A    |
| IC80  |N/A    |
| IC90  |N/A    |
\\ 
</panel>
</accordion>
==== Screen Summary ====
    * **<color #00a2e8>Round</color>**: 03
    * **<color #00a2e8>Dose</color>**: 3µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 7.3
    * **<color #00a2e8>Numbers of reads</color>**: 10394618


==== 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^
|4/0|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/GSK343_3uM_Round-3_exp124.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='GSK343 3μM R03 exp124'>
{{:chemogenomics:cranks_plots:exp124.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:K:KDSR|KDSR]]|-4.49|<0.01|
|[[:human_genes:T:TCF4|TCF4]]|-3.35|<0.01|
|[[:human_genes:A:ADAMDEC1|ADAMDEC1]]|-2.98|<0.01|
|[[:human_genes:Z:ZBTB2|ZBTB2]]|-2.95|0.02|
|[[:human_genes:T:TPK1|TPK1]]|-2.43|0.32|
|[[:human_genes:R:RBM14|RBM14]]|-2.35|0.32|
|[[:human_genes:R:RIF1|RIF1]]|-2.32|0.32|
|[[:human_genes:R:RBM14-RBM4|RBM14-RBM4]]|-2.32|0.32|
|[[:human_genes:U:USP7|USP7]]|-2.23|0.32|
|[[:human_genes:F:FDPS|FDPS]]|-2.20|0.33|
|[[:human_genes:F:FDFT1|FDFT1]]|-2.16|0.32|
|[[:human_genes:M:MCM9|MCM9]]|-2.16|0.32|
|[[:human_genes:P:PEX7|PEX7]]|-2.13|0.32|
|[[:human_genes:R:RPP21|RPP21]]|-2.12|0.32|
|[[:human_genes:M:MVD|MVD]]|-2.09|0.33|
|[[:human_genes:B:BTBD10|BTBD10]]|-2.08|0.32|
|[[:human_genes:D:DNAJC9|DNAJC9]]|-2.07|0.33|
|[[:human_genes:F:FGFBP2|FGFBP2]]|-2.07|0.42|
|[[:human_genes:F:FLVCR1|FLVCR1]]|-2.06|0.32|
|[[:human_genes:C:C21orf58|C21orf58]]|-2.06|0.33|
|[[:human_genes:C:CXorf58|CXorf58]]|-2.04|0.32|
|[[:human_genes:R:RPS17L|RPS17L]]|-2.02|0.63|
|[[:human_genes:B:BRWD1|BRWD1]]|-2.02|0.32|
|[[:human_genes:F:FBXW7|FBXW7]]|-2.02|0.42|
|[[:human_genes:P:PRKCDBP|PRKCDBP]]|-2.01|0.32|
|[[:human_genes:I:IQGAP2|IQGAP2]]|-2.01|0.32|
|[[:human_genes:C:C16orf62|C16orf62]]|-2.00|0.32|
|[[:human_genes:G:GPR107|GPR107]]|-2.00|0.32|
|[[:human_genes:M:MTMR4|MTMR4]]|-1.99|0.32|
|[[:human_genes:C:CTSK|CTSK]]|-1.99|0.32|
|[[:human_genes:S:SLC5A11|SLC5A11]]|1.93|0.81|
|[[:human_genes:A:AFF1|AFF1]]|1.93|0.81|
|[[:human_genes:L:LCE3C|LCE3C]]|1.94|0.81|
|[[:human_genes:H:HEPHL1|HEPHL1]]|1.94|0.81|
|[[:human_genes:C:CTTNBP2|CTTNBP2]]|1.94|0.81|
|[[:human_genes:C:CPSF6|CPSF6]]|1.95|0.81|
|[[:human_genes:C:CD47|CD47]]|1.97|0.81|
|[[:human_genes:N:NPRL3|NPRL3]]|2.00|0.81|
|[[:human_genes:B:BBIP1|BBIP1]]|2.00|0.81|
|[[:human_genes:N:NOL9|NOL9]]|2.01|0.81|
|[[:human_genes:I:ITGAX|ITGAX]]|2.02|0.81|
|[[:human_genes:P:PZP|PZP]]|2.05|0.81|
|[[:human_genes:C:CDK1|CDK1]]|2.05|0.81|
|[[:human_genes:A:ASB11|ASB11]]|2.06|0.81|
|[[:human_genes:P:POLD3|POLD3]]|2.09|0.81|
|[[:human_genes:T:TBC1D3I|TBC1D3I]]|2.12|0.81|
|[[:human_genes:T:TBC1D3E|TBC1D3E]]|2.12|0.81|
|[[:human_genes:T:TBC1D3K|TBC1D3K]]|2.13|0.81|
|[[:human_genes:T:TBC1D3L|TBC1D3L]]|2.13|0.81|
|[[:human_genes:X:XPO4|XPO4]]|2.15|0.81|
|[[:human_genes:S:SCAF11|SCAF11]]|2.15|0.81|
|[[:human_genes:A:ANKHD1-EIF4EBP3|ANKHD1-EIF4EBP3]]|2.23|0.81|
|[[:human_genes:P:PRPF19|PRPF19]]|2.24|0.81|
|[[:human_genes:N:NOP16|NOP16]]|2.25|0.81|
|[[:human_genes:N:NUP88|NUP88]]|2.29|0.81|
|[[:human_genes:A:APBA1|APBA1]]|2.37|0.81|
|[[:human_genes:E:EIF3B|EIF3B]]|2.38|0.81|
|[[:human_genes:R:RPL30|RPL30]]|2.42|0.81|
|[[:human_genes:Z:ZFP82|ZFP82]]|2.46|0.47|
|[[:human_genes:A:ATP6V0B|ATP6V0B]]|2.70|0.81|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp151|SGC0946 7μM R03 exp151]]|0.084|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp155|UNC1999 2μM R03 exp155]]|0.076|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp508|NN-Dimethylsphingosine 2.5μM R08 exp508]]|0.067|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp530|Thioridazine 5μM R08 exp530]]|0.06|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp506|Momordin-Ic 10μM R08 exp506]]|0.053|<button type="primary" size="small" modal="5">View</button>|
|[[:results:exp442|Ibrutinib 10μM R08 exp442]]|0.052|<button type="primary" size="small" modal="6">View</button>|
|[[:results:exp185|L-BMAA 500 to 750μM on day4 R04 exp185]]|0.052|<button type="primary" size="small" modal="7">View</button>|
|[[:results:exp348|Cyclosporin-A 3μM R07 exp348]]|0.056|<button type="primary" size="small" modal="8">View</button>|
</modal>


<modal id="1" size="lg" title="GSK343 3μM R03 exp124  vs  SGC0946 7μM R03 exp151">
{{:chemogenomics:comparison_plots:exp124_vs_exp151.png?nolink |}}
</modal>

<modal id="2" size="lg" title="GSK343 3μM R03 exp124  vs  UNC1999 2μM R03 exp155">
{{:chemogenomics:comparison_plots:exp124_vs_exp155.png?nolink |}}
</modal>

<modal id="3" size="lg" title="GSK343 3μM R03 exp124  vs  NN-Dimethylsphingosine 2.5μM R08 exp508">
{{:chemogenomics:comparison_plots:exp124_vs_exp508.png?nolink |}}
</modal>

<modal id="4" size="lg" title="GSK343 3μM R03 exp124  vs  Thioridazine 5μM R08 exp530">
{{:chemogenomics:comparison_plots:exp124_vs_exp530.png?nolink |}}
</modal>

<modal id="5" size="lg" title="GSK343 3μM R03 exp124  vs  Momordin-Ic 10μM R08 exp506">
{{:chemogenomics:comparison_plots:exp124_vs_exp506.png?nolink |}}
</modal>

<modal id="6" size="lg" title="GSK343 3μM R03 exp124  vs  Ibrutinib 10μM R08 exp442">
{{:chemogenomics:comparison_plots:exp124_vs_exp442.png?nolink |}}
</modal>

<modal id="7" size="lg" title="GSK343 3μM R03 exp124  vs  L-BMAA 500 to 750μM on day4 R04 exp185">
{{:chemogenomics:comparison_plots:exp124_vs_exp185.png?nolink |}}
</modal>

<modal id="8" size="lg" title="Cyclosporin-A 3μM R07 exp348  vs  GSK343 3μM R03 exp124">
{{:chemogenomics:comparison_plots:exp124_vs_exp348.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>