====== Bortezomib 0.05μM R00 exp7 ======
==== Mechanism of Action ====
Inhibits 26S proteasome, binds reversibly to chymotrypsin-like catalytic sites
  * **<color #00a2e8>Class / Subclass 1:</color>** Proteostasis / Proteasome Inhibitor




==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Protein References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%Bortezomib%%
    * **<color #00a2e8>Synonyms:</color>** PS-341; Brotezamide; DPBA; LDP 341; MG 341; Radiciol; NSC 681239
    * **<color #00a2e8>CAS #:</color>** 179324-69-7
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/387447|387447]]
    * **<color #00a2e8>IUPAC:</color>** %%[(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1
    * **<color #00a2e8>INCHI Key:</color>** GXJABQQUPOEUTA-RDJZCZTQSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 384.2
    * **<color #00a2e8>Canonical SMILES:</color>** B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
    * **<color #00a2e8>Isomeric SMILES:</color>** B([C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
    * **<color #00a2e8>Molecular Formula:</color>** C19H25BN4O4
{{:chemogenomics:structures:chem-0004.svg?nolink}}
</panel>


<panel title='Protein Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** LC Laboratories
    * **<color #00a2e8>Catalog #:</color>** B-1408
    * **<color #00a2e8>Lot #:</color>** BBZ-113
</panel>


<panel title='Protein Characterization' collapsed='true'>
    * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** [M+H-H2O]+ Calcd for C19H24BN4O3 367.1936; found 367.1966
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** Bortezomib
    * **<color #00a2e8>Min:</color>** -9.7617; **<color #00a2e8>Max:</color>** 99.4238
{{:chemogenomics:dose_response:dr_256.png?nolink&500 |}}
\\ 
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|< 300px 100px 200px >|
^ IC   ^ Concentration (µM) ^
| IC10  |N/A    |
| IC20  |0.0070    |
| IC30  |0.0072    |
| IC40  |0.0073    |
| IC50  |0.0074    |
| IC60  |N/A    |
| IC70  |N/A    |
| IC80  |N/A    |
| IC90  |N/A    |
\\ 
</panel>
</accordion>
==== Screen Summary ====
    * **<color #00a2e8>Round</color>**: 00
    * **<color #00a2e8>Dose</color>**: 50nM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 0.3
    * **<color #00a2e8>Numbers of reads</color>**: 12274814


==== 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^
|31/20|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Bortezomib_0.05uM_Round-0_exp7.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='Bortezomib 0.05μM R00 exp7'>
{{:chemogenomics:cranks_plots:exp7.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:C:CNOT2|CNOT2]]|-3.80|<0.01|
|[[:human_genes:A:ARID4B|ARID4B]]|-3.73|<0.01|
|[[:human_genes:A:ATP6V0A2|ATP6V0A2]]|-3.47|<0.01|
|[[:human_genes:P:POLR2J3|POLR2J3]]|-3.28|0.04|
|[[:human_genes:A:ATP6V1B2|ATP6V1B2]]|-3.19|<0.01|
|[[:human_genes:X:XKR8|XKR8]]|-3.16|<0.01|
|[[:human_genes:T:TSPYL1|TSPYL1]]|-2.95|0.02|
|[[:human_genes:V:VPS51|VPS51]]|-2.83|0.02|
|[[:human_genes:A:ATP6V1A|ATP6V1A]]|-2.82|0.02|
|[[:human_genes:P:PCYT1A|PCYT1A]]|-2.79|<0.01|
|[[:human_genes:S:SMG5|SMG5]]|-2.72|0.33|
|[[:human_genes:S:STUB1|STUB1]]|-2.69|0.02|
|[[:human_genes:P:PSMB8|PSMB8]]|-2.65|0.02|
|[[:human_genes:B:BRD2|BRD2]]|-2.63|0.02|
|[[:human_genes:S:SLC16A1|SLC16A1]]|-2.59|0.04|
|[[:human_genes:U:USP37|USP37]]|-2.58|0.05|
|[[:human_genes:C:COG3|COG3]]|-2.58|0.02|
|[[:human_genes:R:RPL35|RPL35]]|-2.49|0.04|
|[[:human_genes:D:DHX15|DHX15]]|-2.48|0.28|
|[[:human_genes:V:VPS52|VPS52]]|-2.45|0.04|
|[[:human_genes:T:TMEM189|TMEM189]]|-2.45|0.04|
|[[:human_genes:Y:YY1|YY1]]|-2.43|0.09|
|[[:human_genes:P:PDS5B|PDS5B]]|-2.43|0.04|
|[[:human_genes:P:POLR2J2|POLR2J2]]|-2.43|0.21|
|[[:human_genes:C:COX7A2L|COX7A2L]]|-2.38|0.04|
|[[:human_genes:C:COG1|COG1]]|-2.37|0.04|
|[[:human_genes:D:DFFB|DFFB]]|-2.37|0.04|
|[[:human_genes:B:BCOR|BCOR]]|-2.36|0.06|
|[[:human_genes:G:GIMAP7|GIMAP7]]|-2.36|0.04|
|[[:human_genes:P:PSMB2|PSMB2]]|-2.35|0.24|
|[[:human_genes:I:INTS3|INTS3]]|2.10|0.43|
|[[:human_genes:S:SLIT1|SLIT1]]|2.15|0.20|
|[[:human_genes:B:BIRC5|BIRC5]]|2.17|0.20|
|[[:human_genes:E:EIF4A1|EIF4A1]]|2.18|0.19|
|[[:human_genes:T:TLK2|TLK2]]|2.20|0.19|
|[[:human_genes:U:UBA5|UBA5]]|2.34|0.10|
|[[:human_genes:R:RPL11|RPL11]]|2.34|0.41|
|[[:human_genes:B:BAK1|BAK1]]|2.35|0.05|
|[[:human_genes:E:EED|EED]]|2.42|0.03|
|[[:human_genes:M:MMP16|MMP16]]|2.49|0.02|
|[[:human_genes:W:WSB1|WSB1]]|2.49|0.02|
|[[:human_genes:S:ST20|ST20]]|2.54|0.40|
|[[:human_genes:F:FBXL20|FBXL20]]|2.54|0.02|
|[[:human_genes:H:HIST1H1B|HIST1H1B]]|2.60|0.03|
|[[:human_genes:S:SUZ12|SUZ12]]|2.63|0.01|
|[[:human_genes:U:UBE2K|UBE2K]]|2.68|<0.01|
|[[:human_genes:R:RPL36A-HNRNPH2|RPL36A-HNRNPH2]]|2.70|0.41|
|[[:human_genes:F:FER1L5|FER1L5]]|2.73|<0.01|
|[[:human_genes:P:PRC1|PRC1]]|2.88|<0.01|
|[[:human_genes:E:ECT2|ECT2]]|2.90|<0.01|
|[[:human_genes:R:RBM14-RBM4|RBM14-RBM4]]|2.90|<0.01|
|[[:human_genes:R:RBM14|RBM14]]|2.92|<0.01|
|[[:human_genes:M:MEAF6|MEAF6]]|2.93|<0.01|
|[[:human_genes:A:AURKB|AURKB]]|2.95|0.09|
|[[:human_genes:A:APAF1|APAF1]]|3.04|<0.01|
|[[:human_genes:E:ENY2|ENY2]]|3.06|<0.01|
|[[:human_genes:E:ESPL1|ESPL1]]|3.17|<0.01|
|[[:human_genes:E:ENO1|ENO1]]|3.35|<0.01|
|[[:human_genes:E:EZH2|EZH2]]|3.41|<0.01|
|[[:human_genes:C:CSNK2B|CSNK2B]]|4.06|<0.01|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp17|DABN 20μM R00 exp17]]|0.119|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp28|Pimelic-diphenylamide-106 5μM R00 exp28]]|0.102|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp19|Etoposide 1μM R00 exp19]]|0.095|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp22|MLN-4924 2μM R00 exp22]]|0.092|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp34|Rotenone 20μM R00 exp34]]|0.086|<button type="primary" size="small" modal="5">View</button>|
|[[:results:exp26|Oligomycin-A 20μM R00 exp26]]|0.072|<button type="primary" size="small" modal="6">View</button>|
|[[:results:exp8|Brefeldin A 0.02μM R00 exp8]]|0.072|<button type="primary" size="small" modal="7">View</button>|
|[[:results:exp199|Etoposide 0.3μM R05 exp199]]|0.058|<button type="primary" size="small" modal="8">View</button>|
|[[:results:exp24|Nocodazole 0.2μM R00 exp24]]|0.055|<button type="primary" size="small" modal="9">View</button>|
|[[:results:exp126|GSK461364A 0.1μM R03 exp126]]|0.055|<button type="primary" size="small" modal="10">View</button>|
|[[:results:exp79|Q15 2.7μM R02 exp79]]|0.051|<button type="primary" size="small" modal="11">View</button>|
|[[:results:exp357|Dorsomorphin 5μM R07 exp357]]|0.051|<button type="primary" size="small" modal="12">View</button>|
|[[:results:exp2|5-Fluorouracil 20μM R00 exp2]]|0.088|<button type="primary" size="small" modal="13">View</button>|
|[[:results:exp3|Actinomycin-D 0.001μM R00 exp3]]|0.074|<button type="primary" size="small" modal="14">View</button>|
|[[:results:exp4|Actinomycin-D 0.01μM R00 exp4]]|0.072|<button type="primary" size="small" modal="15">View</button>|
</modal>


<modal id="1" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  DABN 20μM R00 exp17">
{{:chemogenomics:comparison_plots:exp17_vs_exp7.png?nolink |}}
</modal>

<modal id="2" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  Pimelic-diphenylamide-106 5μM R00 exp28">
{{:chemogenomics:comparison_plots:exp28_vs_exp7.png?nolink |}}
</modal>

<modal id="3" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  Etoposide 1μM R00 exp19">
{{:chemogenomics:comparison_plots:exp19_vs_exp7.png?nolink |}}
</modal>

<modal id="4" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  MLN-4924 2μM R00 exp22">
{{:chemogenomics:comparison_plots:exp22_vs_exp7.png?nolink |}}
</modal>

<modal id="5" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  Rotenone 20μM R00 exp34">
{{:chemogenomics:comparison_plots:exp34_vs_exp7.png?nolink |}}
</modal>

<modal id="6" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  Oligomycin-A 20μM R00 exp26">
{{:chemogenomics:comparison_plots:exp26_vs_exp7.png?nolink |}}
</modal>

<modal id="7" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  Brefeldin A 0.02μM R00 exp8">
{{:chemogenomics:comparison_plots:exp7_vs_exp8.png?nolink |}}
</modal>

<modal id="8" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  Etoposide 0.3μM R05 exp199">
{{:chemogenomics:comparison_plots:exp199_vs_exp7.png?nolink |}}
</modal>

<modal id="9" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  Nocodazole 0.2μM R00 exp24">
{{:chemogenomics:comparison_plots:exp24_vs_exp7.png?nolink |}}
</modal>

<modal id="10" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  GSK461364A 0.1μM R03 exp126">
{{:chemogenomics:comparison_plots:exp126_vs_exp7.png?nolink |}}
</modal>

<modal id="11" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  Q15 2.7μM R02 exp79">
{{:chemogenomics:comparison_plots:exp7_vs_exp79.png?nolink |}}
</modal>

<modal id="12" size="lg" title="Bortezomib 0.05μM R00 exp7  vs  Dorsomorphin 5μM R07 exp357">
{{:chemogenomics:comparison_plots:exp357_vs_exp7.png?nolink |}}
</modal>

<modal id="13" size="lg" title="5-Fluorouracil 20μM R00 exp2  vs  Bortezomib 0.05μM R00 exp7">
{{:chemogenomics:comparison_plots:exp2_vs_exp7.png?nolink |}}
</modal>

<modal id="14" size="lg" title="Actinomycin-D 0.001μM R00 exp3  vs  Bortezomib 0.05μM R00 exp7">
{{:chemogenomics:comparison_plots:exp3_vs_exp7.png?nolink |}}
</modal>

<modal id="15" size="lg" title="Actinomycin-D 0.01μM R00 exp4  vs  Bortezomib 0.05μM R00 exp7">
{{:chemogenomics:comparison_plots:exp4_vs_exp7.png?nolink |}}
</modal>



<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">
^GO Term^Fold Change^Genes^
|GARP complex|394.79|VPS51,VPS52|
|proton-transporting ATPase activity, rotational mechanism|77.24|ATP6V0A2,ATP6V1B2,ATP6V1A|
|ATPase-coupled ion transmembrane transporter activity|77.24|ATP6V0A2,ATP6V1B2,ATP6V1A|
|ATPase activity, coupled to transmembrane movement of ions, rotational mechanism|77.24|ATP6V0A2,ATP6V1B2,ATP6V1A|
|vacuolar proton-transporting V-type ATPase complex|74.02|ATP6V0A2,ATP6V1B2,ATP6V1A|
|proton-transporting V-type ATPase complex|65.80|ATP6V0A2,ATP6V1B2,ATP6V1A|
|vacuolar acidification|53.83|ATP6V0A2,ATP6V1B2,ATP6V1A|
|vesicle tethering complex|43.87|VPS51,COG3,VPS52,COG1|
|trans-Golgi network membrane|23.22|VPS51,COG3,VPS52,COG1|
|proton transmembrane transport|22.43|ATP6V0A2,ATP6V1B2,ATP6V1A,SLC16A1,COX7A2L|
|proton transmembrane transporter activity|22.26|ATP6V0A2,ATP6V1B2,ATP6V1A,SLC16A1,COX7A2L|
</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">
^GO Term^Fold Change^Genes^
|mitotic spindle midzone assembly|165.81|AURKB,PRC1,BIRC5|
|mitotic spindle elongation|165.81|AURKB,PRC1,BIRC5|
|spindle elongation|138.18|AURKB,PRC1,BIRC5|
|spindle midzone assembly|127.55|AURKB,PRC1,BIRC5|
|positive regulation of mitotic sister chromatid separation|103.63|ESPL1,AURKB,BIRC5|
|regulation of attachment of spindle microtubules to kinetochore|82.91|AURKB,ECT2,BIRC5|
|positive regulation of chromosome separation|61.41|ESPL1,AURKB,BIRC5|
|transcription corepressor binding|49.13|EZH2,ENO1,SUZ12,EED|
|PcG protein complex|46.06|EZH2,SUZ12,EED|
|mitotic cytokinesis|27.64|ESPL1,AURKB,ECT2,BIRC5|
|regulation of cytokinesis|24.56|AURKB,ECT2,PRC1,BIRC5|
|cytoskeleton-dependent cytokinesis|20.66|ESPL1,AURKB,ECT2,BIRC5|
|cytokinesis|20.28|ESPL1,AURKB,ECT2,BIRC5|
|transcription coregulator binding|20.10|EZH2,ENO1,SUZ12,EED|
|cellular response to radiation|16.55|AURKB,ECT2,ST20,BAK1,TLK2|
|mitotic cell cycle process|7.51|EZH2,ESPL1,AURKB,ECT2,PRC1,BIRC5,INTS3|
|regulation of cell cycle process|6.38|EZH2,ESPL1,AURKB,RBM14,ECT2,PRC1,BIRC5,INTS3|
|chromatin organization|6.26|EZH2,ENY2,MEAF6,RBM14,SUZ12,H1-5,EED,TLK2|
|protein-DNA complex organization|5.64|EZH2,ENY2,MEAF6,RBM14,SUZ12,H1-5,EED,TLK2|
</modal>