EPZ-5676 30μM R05 exp233 [The Human Chemical-Genetic Interaction Map Project]

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====== EPZ-5676 30μM R05 exp233 ======
==== Mechanism of Action ====
Inhibits DOT1L lysine methyltransferase (H3K79me2)
  * **<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>** %%Pinometostat%%
    * **<color #00a2e8>Synonyms:</color>** EPZ-5676
    * **<color #00a2e8>CAS #:</color>** 1380288-87-8
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/57345410|57345410]]
    * **<color #00a2e8>IUPAC:</color>** %%(2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C30H42N8O3/c1-16(2)37(13-22-25(39)26(40)29(41-22)38-15-34-24-27(31)32-14-33-28(24)38)19-10-17(11-19)6-9-23-35-20-8-7-18(30(3,4)5)12-21(20)36-23/h7-8,12,14-17,19,22,25-26,29,39-40H,6,9-11,13H2,1-5H3,(H,35,36)(H2,31,32,33)/t17?,19?,22-,25-,26-,29-/m1/s1
    * **<color #00a2e8>INCHI Key:</color>** LXFOLMYKSYSZQS-XKHGBIBOSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 562.7
    * **<color #00a2e8>Canonical SMILES:</color>** CC(C)N(CC1C(C(C(O1)N2C=NC3=C(N=CN=C32)N)O)O)C4CC(C4)CCC5=NC6=C(N5)C=C(C=C6)C(C)(C)C
    * **<color #00a2e8>Isomeric SMILES:</color>** CC(C)N(C[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O)C4CC(C4)CCC5=NC6=C(N5)C=C(C=C6)C(C)(C)C
    * **<color #00a2e8>Molecular Formula:</color>** C30H42N8O3
{{:chemogenomics:structures:chem-0138.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 C30H42N8O3 563.34526; found 563.34668
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** EPZ-5676
    * **<color #00a2e8>Min:</color>** -0.8707; **<color #00a2e8>Max:</color>** 35.7028
{{:chemogenomics:dose_response:dr_264.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>**: 30µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 6.2
    * **<color #00a2e8>Numbers of reads</color>**: 16438702


==== 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^
|15/6|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/EPZ-5676_30uM_Round-5_exp233.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='EPZ-5676 30μM R05 exp233'>
{{:chemogenomics:cranks_plots:exp233.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:F:FLVCR1|FLVCR1]]|-3.78|<0.01|
|[[:human_genes:R:RER1|RER1]]|-3.34|<0.01|
|[[:human_genes:T:TCF4|TCF4]]|-3.27|<0.01|
|[[:human_genes:A:ARL1|ARL1]]|-3.24|<0.01|
|[[:human_genes:T:TMEM30A|TMEM30A]]|-3.10|<0.01|
|[[:human_genes:R:RSRC2|RSRC2]]|-3.05|0.06|
|[[:human_genes:C:CSK|CSK]]|-2.98|0.02|
|[[:human_genes:S:SPTLC1|SPTLC1]]|-2.87|<0.01|
|[[:human_genes:E:EIF1AX|EIF1AX]]|-2.71|0.03|
|[[:human_genes:V:VRK1|VRK1]]|-2.68|0.03|
|[[:human_genes:S:SCYL1|SCYL1]]|-2.65|0.02|
|[[:human_genes:G:GMPPB|GMPPB]]|-2.58|0.13|
|[[:human_genes:T:TEX29|TEX29]]|-2.56|0.05|
|[[:human_genes:M:MTF2|MTF2]]|-2.47|0.05|
|[[:human_genes:P:PCYT1A|PCYT1A]]|-2.47|0.04|
|[[:human_genes:R:RHOA|RHOA]]|-2.43|0.05|
|[[:human_genes:K:KIAA1432|KIAA1432]]|-2.41|0.05|
|[[:human_genes:B:BCL2|BCL2]]|-2.40|0.07|
|[[:human_genes:C:CLCN5|CLCN5]]|-2.39|0.05|
|[[:human_genes:G:GPN1|GPN1]]|-2.37|0.05|
|[[:human_genes:P:PTEN|PTEN]]|-2.35|0.05|
|[[:human_genes:S:SLC10A7|SLC10A7]]|-2.35|0.05|
|[[:human_genes:C:CEPT1|CEPT1]]|-2.34|0.05|
|[[:human_genes:S:SUMO2|SUMO2]]|-2.31|0.16|
|[[:human_genes:P:PHIP|PHIP]]|-2.27|0.07|
|[[:human_genes:C:CHKA|CHKA]]|-2.22|0.08|
|[[:human_genes:L:LRRC40|LRRC40]]|-2.21|0.08|
|[[:human_genes:L:LYPD8|LYPD8]]|-2.21|0.14|
|[[:human_genes:F:FDPS|FDPS]]|-2.21|0.14|
|[[:human_genes:S:SNRPD3|SNRPD3]]|-2.20|0.52|
|[[:human_genes:L:LARP7|LARP7]]|2.10|0.19|
|[[:human_genes:P:PRR7|PRR7]]|2.12|0.19|
|[[:human_genes:C:C12orf49|C12orf49]]|2.12|0.19|
|[[:human_genes:M:MED28|MED28]]|2.13|0.27|
|[[:human_genes:U:UBE2H|UBE2H]]|2.14|0.19|
|[[:human_genes:M:MDH1|MDH1]]|2.14|0.19|
|[[:human_genes:T:TIMM8A|TIMM8A]]|2.17|0.23|
|[[:human_genes:L:LRRC8A|LRRC8A]]|2.17|0.18|
|[[:human_genes:R:RNF113A|RNF113A]]|2.19|0.40|
|[[:human_genes:S:SPSB3|SPSB3]]|2.20|0.17|
|[[:human_genes:S:SLC25A20|SLC25A20]]|2.23|0.15|
|[[:human_genes:A:ANP32A|ANP32A]]|2.24|0.19|
|[[:human_genes:C:CDV3|CDV3]]|2.24|0.15|
|[[:human_genes:L:LRR1|LRR1]]|2.25|0.38|
|[[:human_genes:N:NDC80|NDC80]]|2.27|0.55|
|[[:human_genes:C:CDC20|CDC20]]|2.32|0.23|
|[[:human_genes:R:RBM23|RBM23]]|2.40|0.07|
|[[:human_genes:N:NPRL2|NPRL2]]|2.40|0.07|
|[[:human_genes:C:CCNA2|CCNA2]]|2.40|0.19|
|[[:human_genes:D:DTL|DTL]]|2.41|0.30|
|[[:human_genes:C:C12orf66|C12orf66]]|2.41|0.07|
|[[:human_genes:G:GOT1|GOT1]]|2.45|0.07|
|[[:human_genes:D:DYNC1H1|DYNC1H1]]|2.54|0.55|
|[[:human_genes:C:CMAS|CMAS]]|2.57|0.04|
|[[:human_genes:S:SZT2|SZT2]]|2.58|0.04|
|[[:human_genes:D:DEPDC5|DEPDC5]]|2.59|0.04|
|[[:human_genes:M:MCL1|MCL1]]|2.74|0.04|
|[[:human_genes:N:NPRL3|NPRL3]]|2.78|0.07|
|[[:human_genes:P:PDS5B|PDS5B]]|2.92|0.01|
|[[:human_genes:K:KMT2D|KMT2D]]|3.82|<0.01|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp510|Nicotine 3000μM R08 exp510]]|0.084|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp530|Thioridazine 5μM R08 exp530]]|0.076|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp483|FTY720 3μM R08 exp483]]|0.074|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp506|Momordin-Ic 10μM R08 exp506]]|0.071|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp504|MK2206 4μM R08 exp504]]|0.07|<button type="primary" size="small" modal="5">View</button>|
|[[:results:exp216|Erlotinib 10μM R05 exp216]]|0.066|<button type="primary" size="small" modal="6">View</button>|
|[[:results:exp508|NN-Dimethylsphingosine 2.5μM R08 exp508]]|0.065|<button type="primary" size="small" modal="7">View</button>|
|[[:results:exp155|UNC1999 2μM R03 exp155]]|0.064|<button type="primary" size="small" modal="8">View</button>|
|[[:results:exp442|Ibrutinib 10μM R08 exp442]]|0.061|<button type="primary" size="small" modal="9">View</button>|
|[[:results:exp307|Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307]]|0.059|<button type="primary" size="small" modal="10">View</button>|
|[[:results:exp149|SB203580 25μM R03 exp149]]|0.057|<button type="primary" size="small" modal="11">View</button>|
|[[:results:exp422|Wiskostatin 3μM R07 exp422]]|0.057|<button type="primary" size="small" modal="12">View</button>|
|[[:results:exp90|WYE-354 6μM R02 exp90]]|0.057|<button type="primary" size="small" modal="13">View</button>|
|[[:results:exp30|Rapamycin 10μM R00 exp30]]|0.057|<button type="primary" size="small" modal="14">View</button>|
|[[:results:exp234|Ethanol 0.01 R05 exp234]]|0.056|<button type="primary" size="small" modal="15">View</button>|
|[[:results:exp480|ETC-159 50μM R08 exp480]]|0.055|<button type="primary" size="small" modal="16">View</button>|
|[[:results:exp151|SGC0946 7μM R03 exp151]]|0.054|<button type="primary" size="small" modal="17">View</button>|
|[[:results:exp47|Lapatinib 5μM R01 exp47]]|0.054|<button type="primary" size="small" modal="18">View</button>|
|[[:results:exp242|Radicicol 0.16μM R05 exp242]]|0.053|<button type="primary" size="small" modal="19">View</button>|
|[[:results:exp77|Prochlorperazine 5.2μM R02 exp77]]|0.052|<button type="primary" size="small" modal="20">View</button>|
|[[:results:exp452|Azithromycin 100μM R08 exp452]]|0.087|<button type="primary" size="small" modal="21">View</button>|
|[[:results:exp224|CB-839 10μM R05 exp224]]|0.082|<button type="primary" size="small" modal="22">View</button>|
|[[:results:exp344|Chlorpromazine 10μM R07 exp344]]|0.079|<button type="primary" size="small" modal="23">View</button>|
|[[:results:exp467|CAY10603 0.55μM R08 exp467]]|0.068|<button type="primary" size="small" modal="24">View</button>|
|[[:results:exp461|BS-181 20μM R08 exp461]]|0.068|<button type="primary" size="small" modal="25">View</button>|
|[[:results:exp465|Cannabidiol 13μM R08 exp465]]|0.065|<button type="primary" size="small" modal="26">View</button>|
|[[:results:exp453|B02 10μM R08 exp453]]|0.059|<button type="primary" size="small" modal="27">View</button>|
|[[:results:exp225|Celastrol 0.12μM R05 exp225]]|0.057|<button type="primary" size="small" modal="28">View</button>|
|[[:results:exp169|BH1 1μM R04 exp169]]|0.055|<button type="primary" size="small" modal="29">View</button>|
|[[:results:exp269|Bisphenol A 100μM R06 exp269]]|0.055|<button type="primary" size="small" modal="30">View</button>|
|[[:results:exp326|CCT251545 20μM R07 exp326]]|0.052|<button type="primary" size="small" modal="31">View</button>|
</modal>


<modal id="1" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Nicotine 3000μM R08 exp510">
{{:chemogenomics:comparison_plots:exp233_vs_exp510.png?nolink |}}
</modal>

<modal id="2" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Thioridazine 5μM R08 exp530">
{{:chemogenomics:comparison_plots:exp233_vs_exp530.png?nolink |}}
</modal>

<modal id="3" size="lg" title="EPZ-5676 30μM R05 exp233  vs  FTY720 3μM R08 exp483">
{{:chemogenomics:comparison_plots:exp233_vs_exp483.png?nolink |}}
</modal>

<modal id="4" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Momordin-Ic 10μM R08 exp506">
{{:chemogenomics:comparison_plots:exp233_vs_exp506.png?nolink |}}
</modal>

<modal id="5" size="lg" title="EPZ-5676 30μM R05 exp233  vs  MK2206 4μM R08 exp504">
{{:chemogenomics:comparison_plots:exp233_vs_exp504.png?nolink |}}
</modal>

<modal id="6" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Erlotinib 10μM R05 exp216">
{{:chemogenomics:comparison_plots:exp216_vs_exp233.png?nolink |}}
</modal>

<modal id="7" size="lg" title="EPZ-5676 30μM R05 exp233  vs  NN-Dimethylsphingosine 2.5μM R08 exp508">
{{:chemogenomics:comparison_plots:exp233_vs_exp508.png?nolink |}}
</modal>

<modal id="8" size="lg" title="EPZ-5676 30μM R05 exp233  vs  UNC1999 2μM R03 exp155">
{{:chemogenomics:comparison_plots:exp155_vs_exp233.png?nolink |}}
</modal>

<modal id="9" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Ibrutinib 10μM R08 exp442">
{{:chemogenomics:comparison_plots:exp233_vs_exp442.png?nolink |}}
</modal>

<modal id="10" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307">
{{:chemogenomics:comparison_plots:exp233_vs_exp307.png?nolink |}}
</modal>

<modal id="11" size="lg" title="EPZ-5676 30μM R05 exp233  vs  SB203580 25μM R03 exp149">
{{:chemogenomics:comparison_plots:exp149_vs_exp233.png?nolink |}}
</modal>

<modal id="12" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Wiskostatin 3μM R07 exp422">
{{:chemogenomics:comparison_plots:exp233_vs_exp422.png?nolink |}}
</modal>

<modal id="13" size="lg" title="EPZ-5676 30μM R05 exp233  vs  WYE-354 6μM R02 exp90">
{{:chemogenomics:comparison_plots:exp233_vs_exp90.png?nolink |}}
</modal>

<modal id="14" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Rapamycin 10μM R00 exp30">
{{:chemogenomics:comparison_plots:exp233_vs_exp30.png?nolink |}}
</modal>

<modal id="15" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Ethanol 0.01 R05 exp234">
{{:chemogenomics:comparison_plots:exp233_vs_exp234.png?nolink |}}
</modal>

<modal id="16" size="lg" title="EPZ-5676 30μM R05 exp233  vs  ETC-159 50μM R08 exp480">
{{:chemogenomics:comparison_plots:exp233_vs_exp480.png?nolink |}}
</modal>

<modal id="17" size="lg" title="EPZ-5676 30μM R05 exp233  vs  SGC0946 7μM R03 exp151">
{{:chemogenomics:comparison_plots:exp151_vs_exp233.png?nolink |}}
</modal>

<modal id="18" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Lapatinib 5μM R01 exp47">
{{:chemogenomics:comparison_plots:exp233_vs_exp47.png?nolink |}}
</modal>

<modal id="19" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Radicicol 0.16μM R05 exp242">
{{:chemogenomics:comparison_plots:exp233_vs_exp242.png?nolink |}}
</modal>

<modal id="20" size="lg" title="EPZ-5676 30μM R05 exp233  vs  Prochlorperazine 5.2μM R02 exp77">
{{:chemogenomics:comparison_plots:exp233_vs_exp77.png?nolink |}}
</modal>

<modal id="21" size="lg" title="Azithromycin 100μM R08 exp452  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp233_vs_exp452.png?nolink |}}
</modal>

<modal id="22" size="lg" title="CB-839 10μM R05 exp224  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp224_vs_exp233.png?nolink |}}
</modal>

<modal id="23" size="lg" title="Chlorpromazine 10μM R07 exp344  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp233_vs_exp344.png?nolink |}}
</modal>

<modal id="24" size="lg" title="CAY10603 0.55μM R08 exp467  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp233_vs_exp467.png?nolink |}}
</modal>

<modal id="25" size="lg" title="BS-181 20μM R08 exp461  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp233_vs_exp461.png?nolink |}}
</modal>

<modal id="26" size="lg" title="Cannabidiol 13μM R08 exp465  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp233_vs_exp465.png?nolink |}}
</modal>

<modal id="27" size="lg" title="B02 10μM R08 exp453  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp233_vs_exp453.png?nolink |}}
</modal>

<modal id="28" size="lg" title="Celastrol 0.12μM R05 exp225  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp225_vs_exp233.png?nolink |}}
</modal>

<modal id="29" size="lg" title="BH1 1μM R04 exp169  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp169_vs_exp233.png?nolink |}}
</modal>

<modal id="30" size="lg" title="Bisphenol A 100μM R06 exp269  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp233_vs_exp269.png?nolink |}}
</modal>

<modal id="31" size="lg" title="CCT251545 20μM R07 exp326  vs  EPZ-5676 30μM R05 exp233">
{{:chemogenomics:comparison_plots:exp233_vs_exp326.png?nolink |}}
</modal>



<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">
^GO Term^Fold Change^Genes^
|CDP-choline pathway|318.65|PCYT1A,CEPT1,CHKA|
|phosphatidylcholine biosynthetic process|79.66|PCYT1A,CEPT1,CHKA|
|phospholipid biosynthetic process|16.41|SPTLC1,PCYT1A,PTEN,CEPT1,CHKA,FDPS|
</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">
^GO Term^Fold Change^Genes^
|GATOR1 complex|552.33|NPRL3,NPRL2|
|meiotic cell cycle phase transition|368.22|CDC20,NDC80|
|Seh1-associated complex|236.71|NPRL3,DEPDC5,NPRL2|
|negative regulation of TORC1 signaling|53.89|NPRL3,DEPDC5,SZT2,NPRL2|
|cellular response to amino acid starvation|47.01|NPRL3,DEPDC5,SZT2,NPRL2|
|response to amino acid starvation|44.19|NPRL3,DEPDC5,SZT2,NPRL2|
|negative regulation of TOR signaling|33.47|NPRL3,DEPDC5,SZT2,NPRL2|
|regulation of TORC1 signaling|25.69|NPRL3,DEPDC5,SZT2,NPRL2|
</modal>