LLY-283 2.6μM R06 exp290 [The Human Chemical-Genetic Interaction Map Project]

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====== LLY-283 2.6μM R06 exp290 ======
==== Mechanism of Action ====
Inhibits protein arginine methyltransferase PRMT5, inactive control is LLY-284
  * **<color #00a2e8>Class / Subclass 1:</color>** Gene Regulation / Epigenetic Inhibitor




==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Compound References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%(2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol%%
    * **<color #00a2e8>Synonyms:</color>** N/A
    * **<color #00a2e8>CAS #:</color>** 2040291-27-6
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/122669401|122669401]]
    * **<color #00a2e8>IUPAC:</color>** %%(2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C17H18N4O4/c18-15-10-6-7-21(16(10)20-8-19-15)17-13(24)12(23)14(25-17)11(22)9-4-2-1-3-5-9/h1-8,11-14,17,22-24H,(H2,18,19,20)/t11-,12+,13-,14-,17-/m1/s1
    * **<color #00a2e8>INCHI Key:</color>** WWOOWAHTEXIWBO-QFRSUPTLSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 342.35
    * **<color #00a2e8>Canonical SMILES:</color>** C1=CC=C(C=C1)C(C2C(C(C(O2)N3C=CC4=C(N=CN=C43)N)O)O)O
    * **<color #00a2e8>Isomeric SMILES:</color>** C1=CC=C(C=C1)[C@H]([C@@H]2[C@H]([C@H]([C@@H](O2)N3C=CC4=C(N=CN=C43)N)O)O)O
    * **<color #00a2e8>Molecular Formula:</color>** C17H18N4O4
{{:chemogenomics:structures:chem-0178.svg?nolink}}
</panel>


<panel title='Compound 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='Compound Characterization' collapsed='true'>
    * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+H)+ Calcd for C17H18N4O4 343.14008; found 343.14031
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** LLY-283
    * **<color #00a2e8>Min:</color>** -21.8158; **<color #00a2e8>Max:</color>** -5.0973
{{:chemogenomics:dose_response:dr_291.png?nolink&500 |}}
\\ 
\\ 
\\ 
\\ 
|< 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>**: 06
    * **<color #00a2e8>Dose</color>**: 2.6µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 3.1
    * **<color #00a2e8>Numbers of reads</color>**: 26341968


==== 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^
|16/5|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/LLY-283_2.6uM_Round-6_exp290.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="primary" 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='LLY-283 2.6μM R06 exp290'>
{{:chemogenomics:cranks_plots:exp290.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:Z:ZC3H14|ZC3H14]]|-3.46|<0.01|
|[[:human_genes:S:SNRPB2|SNRPB2]]|-3.21|<0.01|
|[[:human_genes:D:DDX39A|DDX39A]]|-2.93|<0.01|
|[[:human_genes:K:KMT2E|KMT2E]]|-2.88|<0.01|
|[[:human_genes:Y:YLPM1|YLPM1]]|-2.84|0.03|
|[[:human_genes:A:API5|API5]]|-2.75|0.02|
|[[:human_genes:R:RNASEK|RNASEK]]|-2.74|0.03|
|[[:human_genes:N:NPRL2|NPRL2]]|-2.72|0.03|
|[[:human_genes:B:BRD1|BRD1]]|-2.71|0.02|
|[[:human_genes:P:PRPF38B|PRPF38B]]|-2.67|0.09|
|[[:human_genes:W:WDR73|WDR73]]|-2.62|0.02|
|[[:human_genes:P:PCBP2|PCBP2]]|-2.62|0.02|
|[[:human_genes:K:KIF18A|KIF18A]]|-2.60|0.04|
|[[:human_genes:S:SZT2|SZT2]]|-2.58|0.03|
|[[:human_genes:I:INTS12|INTS12]]|-2.45|0.04|
|[[:human_genes:T:TSC2|TSC2]]|-2.41|0.04|
|[[:human_genes:P:PDS5B|PDS5B]]|-2.40|0.04|
|[[:human_genes:T:TXNL4A|TXNL4A]]|-2.39|0.48|
|[[:human_genes:A:ANKRD11|ANKRD11]]|-2.37|0.05|
|[[:human_genes:A:ACIN1|ACIN1]]|-2.35|0.08|
|[[:human_genes:G:GAK|GAK]]|-2.35|0.05|
|[[:human_genes:Y:YPEL5|YPEL5]]|-2.34|0.05|
|[[:human_genes:C:CNOT2|CNOT2]]|-2.33|0.05|
|[[:human_genes:G:GFI1|GFI1]]|-2.30|0.06|
|[[:human_genes:T:TRPM4|TRPM4]]|-2.30|0.06|
|[[:human_genes:K:KIDINS220|KIDINS220]]|-2.29|0.06|
|[[:human_genes:A:AKAP17A|AKAP17A]]|-2.25|0.07|
|[[:human_genes:A:ACBD3|ACBD3]]|-2.23|0.12|
|[[:human_genes:P:PRPF4B|PRPF4B]]|-2.23|0.12|
|[[:human_genes:M:MYC|MYC]]|-2.20|0.46|
|[[:human_genes:G:GFM1|GFM1]]|2.27|0.12|
|[[:human_genes:S:SLC7A1|SLC7A1]]|2.27|0.16|
|[[:human_genes:E:EARS2|EARS2]]|2.27|0.08|
|[[:human_genes:C:CRLS1|CRLS1]]|2.27|0.08|
|[[:human_genes:O:OMA1|OMA1]]|2.27|0.08|
|[[:human_genes:M:MBD2|MBD2]]|2.28|0.08|
|[[:human_genes:B:BPTF|BPTF]]|2.28|0.12|
|[[:human_genes:R:RPL11|RPL11]]|2.29|0.43|
|[[:human_genes:B:BCS1L|BCS1L]]|2.30|0.08|
|[[:human_genes:D:DARS2|DARS2]]|2.31|0.16|
|[[:human_genes:U:UNC79|UNC79]]|2.32|0.12|
|[[:human_genes:C:COX17|COX17]]|2.34|0.21|
|[[:human_genes:U:USP39|USP39]]|2.34|0.16|
|[[:human_genes:D:DPH6|DPH6]]|2.36|0.07|
|[[:human_genes:R:RPL36A|RPL36A]]|2.38|0.07|
|[[:human_genes:A:ALG6|ALG6]]|2.39|0.07|
|[[:human_genes:T:TRMT61A|TRMT61A]]|2.39|0.13|
|[[:human_genes:S:SLC11A2|SLC11A2]]|2.43|0.07|
|[[:human_genes:Y:YARS2|YARS2]]|2.44|0.07|
|[[:human_genes:I:IMPDH2|IMPDH2]]|2.49|0.07|
|[[:human_genes:G:GNPAT|GNPAT]]|2.50|0.07|
|[[:human_genes:M:MRPS6|MRPS6]]|2.56|0.07|
|[[:human_genes:R:RARS2|RARS2]]|2.56|0.07|
|[[:human_genes:T:TMED2|TMED2]]|2.59|0.05|
|[[:human_genes:T:TMED10|TMED10]]|2.92|0.02|
|[[:human_genes:T:TP53|TP53]]|3.05|0.01|
|[[:human_genes:R:RPS8|RPS8]]|3.13|0.16|
|[[:human_genes:R:RPL36A-HNRNPH2|RPL36A-HNRNPH2]]|3.31|0.12|
|[[:human_genes:I:ILKAP|ILKAP]]|3.57|<0.01|
|[[:human_genes:P:PTPMT1|PTPMT1]]|4.11|<0.01|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp529|Thimerosal 0.85μM R08 exp529]]|0.096|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp492|iCRT14 30μM R08 exp492]]|0.074|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp84|UM0125461 0.74μM R02 exp84]]|0.065|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp106|UM131593 0.2μM R03 exp106]]|0.064|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp439|QNZ 0.01μM R08 exp439]]|0.063|<button type="primary" size="small" modal="5">View</button>|
|[[:results:exp25|Oligomycin-A 2μM R00 exp25]]|0.06|<button type="primary" size="small" modal="6">View</button>|
|[[:results:exp515|PU-H71 1μM R08 exp515]]|0.058|<button type="primary" size="small" modal="7">View</button>|
|[[:results:exp517|Quercetin 20μM R08 exp517]]|0.051|<button type="primary" size="small" modal="8">View</button>|
|[[:results:exp59|UMK57 1μM R01 exp59]]|0.051|<button type="primary" size="small" modal="9">View</button>|
|[[:results:exp212|Phenformin 20μM R05 exp212]]|0.051|<button type="primary" size="small" modal="10">View</button>|
|[[:results:exp128|GSK591 2.6μM R03 exp128]]|0.089|<button type="primary" size="small" modal="11">View</button>|
|[[:results:exp468|CB-5083 0.4μM R08 exp468]]|0.068|<button type="primary" size="small" modal="12">View</button>|
|[[:results:exp440|Aphidicolin 0.4μM R08 exp440]]|0.062|<button type="primary" size="small" modal="13">View</button>|
|[[:results:exp329|Hydroxyurea 100μM R07 exp329]]|0.061|<button type="primary" size="small" modal="14">View</button>|
|[[:results:exp312|2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312]]|0.058|<button type="primary" size="small" modal="15">View</button>|
|[[:results:exp460|BML-284 0.09μM R08 exp460]]|0.057|<button type="primary" size="small" modal="16">View</button>|
|[[:results:exp478|Doxorubicin 0.02μM R08 exp478]]|0.055|<button type="primary" size="small" modal="17">View</button>|
|[[:results:exp441|GSK-J4 1.5μM R08 exp441]]|0.053|<button type="primary" size="small" modal="18">View</button>|
|[[:results:exp66|BI-D1870 3.15μM R02 exp66]]|0.052|<button type="primary" size="small" modal="19">View</button>|
|[[:results:exp264|Arsenate 40μM R06 exp264]]|0.051|<button type="primary" size="small" modal="20">View</button>|
</modal>


<modal id="1" size="lg" title="LLY-283 2.6μM R06 exp290  vs  Thimerosal 0.85μM R08 exp529">
{{:chemogenomics:comparison_plots:exp290_vs_exp529.png?nolink |}}
</modal>

<modal id="2" size="lg" title="LLY-283 2.6μM R06 exp290  vs  iCRT14 30μM R08 exp492">
{{:chemogenomics:comparison_plots:exp290_vs_exp492.png?nolink |}}
</modal>

<modal id="3" size="lg" title="LLY-283 2.6μM R06 exp290  vs  UM0125461 0.74μM R02 exp84">
{{:chemogenomics:comparison_plots:exp290_vs_exp84.png?nolink |}}
</modal>

<modal id="4" size="lg" title="LLY-283 2.6μM R06 exp290  vs  UM131593 0.2μM R03 exp106">
{{:chemogenomics:comparison_plots:exp106_vs_exp290.png?nolink |}}
</modal>

<modal id="5" size="lg" title="LLY-283 2.6μM R06 exp290  vs  QNZ 0.01μM R08 exp439">
{{:chemogenomics:comparison_plots:exp290_vs_exp439.png?nolink |}}
</modal>

<modal id="6" size="lg" title="LLY-283 2.6μM R06 exp290  vs  Oligomycin-A 2μM R00 exp25">
{{:chemogenomics:comparison_plots:exp25_vs_exp290.png?nolink |}}
</modal>

<modal id="7" size="lg" title="LLY-283 2.6μM R06 exp290  vs  PU-H71 1μM R08 exp515">
{{:chemogenomics:comparison_plots:exp290_vs_exp515.png?nolink |}}
</modal>

<modal id="8" size="lg" title="LLY-283 2.6μM R06 exp290  vs  Quercetin 20μM R08 exp517">
{{:chemogenomics:comparison_plots:exp290_vs_exp517.png?nolink |}}
</modal>

<modal id="9" 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="10" size="lg" title="LLY-283 2.6μM R06 exp290  vs  Phenformin 20μM R05 exp212">
{{:chemogenomics:comparison_plots:exp212_vs_exp290.png?nolink |}}
</modal>

<modal id="11" size="lg" title="GSK591 2.6μM R03 exp128  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp128_vs_exp290.png?nolink |}}
</modal>

<modal id="12" size="lg" title="CB-5083 0.4μM R08 exp468  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp290_vs_exp468.png?nolink |}}
</modal>

<modal id="13" size="lg" title="Aphidicolin 0.4μM R08 exp440  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp290_vs_exp440.png?nolink |}}
</modal>

<modal id="14" size="lg" title="Hydroxyurea 100μM R07 exp329  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp290_vs_exp329.png?nolink |}}
</modal>

<modal id="15" size="lg" title="2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp290_vs_exp312.png?nolink |}}
</modal>

<modal id="16" size="lg" title="BML-284 0.09μM R08 exp460  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp290_vs_exp460.png?nolink |}}
</modal>

<modal id="17" size="lg" title="Doxorubicin 0.02μM R08 exp478  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp290_vs_exp478.png?nolink |}}
</modal>

<modal id="18" size="lg" title="GSK-J4 1.5μM R08 exp441  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp290_vs_exp441.png?nolink |}}
</modal>

<modal id="19" size="lg" title="BI-D1870 3.15μM R02 exp66  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp290_vs_exp66.png?nolink |}}
</modal>

<modal id="20" size="lg" title="Arsenate 40μM R06 exp264  vs  LLY-283 2.6μM R06 exp290">
{{:chemogenomics:comparison_plots:exp264_vs_exp290.png?nolink |}}
</modal>



<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">
^GO Term^Fold Change^Genes^
|spliceosomal complex|17.77|SNRPB2,API5,PRPF38B,TXNL4A,AKAP17A,PRPF4B|
|nuclear speck|14.08|ZC3H14,SNRPB2,DDX39A,KMT2E,YLPM1,API5,BRD1,ACIN1,AKAP17A,PRPF4B|
|RNA splicing|11.14|SNRPB2,DDX39A,PRPF38B,TXNL4A,ACIN1,AKAP17A,PRPF4B|
|mRNA metabolic process|8.76|SNRPB2,DDX39A,PRPF38B,PCBP2,TXNL4A,ACIN1,CNOT2,AKAP17A,PRPF4B|
|nuclear body|7.76|ZC3H14,SNRPB2,DDX39A,KMT2E,YLPM1,API5,BRD1,ACIN1,GFI1,AKAP17A,PRPF4B|
|ribonucleoprotein complex|6.63|ZC3H14,SNRPB2,API5,PRPF38B,PCBP2,TXNL4A,AKAP17A,PRPF4B|
</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">
^GO Term^Fold Change^Genes^
|tRNA aminoacylation for mitochondrial protein translation|236.74|YARS2,DARS2,EARS2|
|ligase activity, forming carbon-oxygen bonds|59.72|RARS2,YARS2,DARS2,EARS2|
|aminoacyl-tRNA ligase activity|59.72|RARS2,YARS2,DARS2,EARS2|
|tRNA aminoacylation for protein translation|59.72|RARS2,YARS2,DARS2,EARS2|
|tRNA aminoacylation|55.24|RARS2,YARS2,DARS2,EARS2|
|amino acid activation|53.89|RARS2,YARS2,DARS2,EARS2|
|mitochondrial translation|36.14|RARS2,MRPS6,YARS2,DARS2,MRPL57,EARS2,GFM1|
|mitochondrial gene expression|27.82|RARS2,MRPS6,YARS2,DARS2,MRPL57,EARS2,GFM1|
|catalytic activity, acting on a tRNA|22.27|RARS2,YARS2,TRMT61A,DARS2,EARS2|
|ligase activity|20.98|RARS2,YARS2,DPH6,DARS2,ATP5F1A,EARS2|
|translation|15.47|RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1|
|peptide biosynthetic process|14.46|RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1|
|peptide metabolic process|11.65|RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1|
|amide biosynthetic process|10.98|RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1|
|mitochondrial matrix|10.51|TP53,RARS2,MRPS6,YARS2,DARS2,ATP5F1A,MRPL57,EARS2,GFM1|
|ncRNA metabolic process|8.79|RPS8,TP53,RARS2,YARS2,TRMT61A,DARS2,RPL11,EARS2|
|mitochondrial envelope|7.36|PTPMT1,MRPS6,GNPAT,SLC11A2,COX17,BCS1L,ATP5F1A,MRPL57,OMA1,CRLS1|
|amide metabolic process|7.30|RPS8,RARS2,MRPS6,YARS2,RPL36A,DARS2,RPL11,MRPL57,EARS2,GFM1|
|mitochondrial membrane|7.05|PTPMT1,MRPS6,GNPAT,SLC11A2,BCS1L,ATP5F1A,MRPL57,OMA1,CRLS1|
</modal>