====== Bortezomib 0.005μM R00 exp6 ======
==== 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>**: 5nM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 3.6
    * **<color #00a2e8>Numbers of reads</color>**: 13211930


==== 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^
|123/76|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Bortezomib_0.005uM_Round-0_exp6.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 0.005μM R00 exp6'>
{{:chemogenomics:cranks_plots:exp6.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:P:PSMB8|PSMB8]]|-6.68|<0.01|
|[[:human_genes:P:PSMB5|PSMB5]]|-6.46|<0.01|
|[[:human_genes:R:RNF181|RNF181]]|-5.61|<0.01|
|[[:human_genes:K:KIAA0368|KIAA0368]]|-4.70|<0.01|
|[[:human_genes:C:CNOT8|CNOT8]]|-4.50|<0.01|
|[[:human_genes:S:SOX4|SOX4]]|-4.49|<0.01|
|[[:human_genes:P:PSMB6|PSMB6]]|-4.45|<0.01|
|[[:human_genes:K:KIAA0922|KIAA0922]]|-4.45|<0.01|
|[[:human_genes:T:TMEM39A|TMEM39A]]|-4.31|<0.01|
|[[:human_genes:O:OSER1|OSER1]]|-4.25|<0.01|
|[[:human_genes:K:KDSR|KDSR]]|-3.54|<0.01|
|[[:human_genes:P:PSMB7|PSMB7]]|-3.54|<0.01|
|[[:human_genes:N:NGLY1|NGLY1]]|-3.49|<0.01|
|[[:human_genes:C:CAPRIN1|CAPRIN1]]|-3.45|<0.01|
|[[:human_genes:I:IRF2|IRF2]]|-3.41|<0.01|
|[[:human_genes:Z:ZFY|ZFY]]|-3.38|<0.01|
|[[:human_genes:S:SMEK1|SMEK1]]|-3.31|<0.01|
|[[:human_genes:P:PSMG3|PSMG3]]|-3.30|<0.01|
|[[:human_genes:M:MAFK|MAFK]]|-3.29|<0.01|
|[[:human_genes:R:RBM5|RBM5]]|-3.27|<0.01|
|[[:human_genes:U:UFC1|UFC1]]|-3.16|<0.01|
|[[:human_genes:A:ARID4B|ARID4B]]|-3.14|<0.01|
|[[:human_genes:A:ACTB|ACTB]]|-3.11|<0.01|
|[[:human_genes:P:POMP|POMP]]|-3.05|<0.01|
|[[:human_genes:P:PPIA|PPIA]]|-3.03|<0.01|
|[[:human_genes:G:GPCPD1|GPCPD1]]|-3.00|<0.01|
|[[:human_genes:S:SEC31A|SEC31A]]|-2.99|<0.01|
|[[:human_genes:P:PDS5B|PDS5B]]|-2.93|<0.01|
|[[:human_genes:I:INTS12|INTS12]]|-2.92|<0.01|
|[[:human_genes:U:UBE2K|UBE2K]]|-2.88|<0.01|
|[[:human_genes:U:UBE4A|UBE4A]]|2.88|<0.01|
|[[:human_genes:P:PPIP5K2|PPIP5K2]]|2.89|<0.01|
|[[:human_genes:P:PGP|PGP]]|2.95|<0.01|
|[[:human_genes:C:CDK2|CDK2]]|2.95|<0.01|
|[[:human_genes:K:KAT7|KAT7]]|3.02|<0.01|
|[[:human_genes:D:DPH5|DPH5]]|3.04|<0.01|
|[[:human_genes:P:POU2AF1|POU2AF1]]|3.14|<0.01|
|[[:human_genes:Y:YBX1|YBX1]]|3.15|<0.01|
|[[:human_genes:P:PPP3R1|PPP3R1]]|3.16|<0.01|
|[[:human_genes:F:FAF2|FAF2]]|3.22|<0.01|
|[[:human_genes:Y:YLPM1|YLPM1]]|3.26|<0.01|
|[[:human_genes:D:DNAJC24|DNAJC24]]|3.31|<0.01|
|[[:human_genes:L:LSM12|LSM12]]|3.34|<0.01|
|[[:human_genes:D:DPH6|DPH6]]|3.40|<0.01|
|[[:human_genes:U:UBQLN1|UBQLN1]]|3.48|<0.01|
|[[:human_genes:S:SAMD1|SAMD1]]|3.49|<0.01|
|[[:human_genes:R:RBM27|RBM27]]|3.52|<0.01|
|[[:human_genes:B:BAK1|BAK1]]|3.60|<0.01|
|[[:human_genes:E:EBF1|EBF1]]|3.62|<0.01|
|[[:human_genes:E:EIF4G1|EIF4G1]]|3.67|<0.01|
|[[:human_genes:P:PTMA|PTMA]]|3.98|<0.01|
|[[:human_genes:S:SRM|SRM]]|4.10|<0.01|
|[[:human_genes:A:AZIN1|AZIN1]]|4.15|<0.01|
|[[:human_genes:P:PSMB9|PSMB9]]|4.28|<0.01|
|[[:human_genes:P:PRRC2C|PRRC2C]]|5.07|<0.01|
|[[:human_genes:D:DDX3X|DDX3X]]|5.20|<0.01|
|[[:human_genes:A:ATXN2L|ATXN2L]]|5.35|<0.01|
|[[:human_genes:E:EIF4H|EIF4H]]|5.48|<0.01|
|[[:human_genes:C:CNBP|CNBP]]|5.75|<0.01|
|[[:human_genes:E:EIF4A1|EIF4A1]]|7.24|<0.01|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp468|CB-5083 0.4μM R08 exp468]]|0.076|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp234|Ethanol 0.01 R05 exp234]]|0.075|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp407|Thapsigargin 0.005μM R07 exp407]]|0.061|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp505|ML-792 0.2μM R08 exp505]]|0.06|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp512|Olaparib 4μM R08 exp512]]|0.06|<button type="primary" size="small" modal="5">View</button>|
|[[:results:exp416|Tubacin 1.6μM R07 exp416]]|0.058|<button type="primary" size="small" modal="6">View</button>|
|[[:results:exp122|Golgicide-A 4μM R03 exp122]]|0.058|<button type="primary" size="small" modal="7">View</button>|
|[[:results:exp36|TRAIL 50ng/ml R00 exp36]]|0.058|<button type="primary" size="small" modal="8">View</button>|
|[[:results:exp35|TRAIL 5ng/ml R00 exp35]]|0.056|<button type="primary" size="small" modal="9">View</button>|
|[[:results:exp517|Quercetin 20μM R08 exp517]]|0.054|<button type="primary" size="small" modal="10">View</button>|
|[[:results:exp356|Docosahexaenoic-acid 50μM R07 exp356]]|0.051|<button type="primary" size="small" modal="11">View</button>|
|[[:results:exp134|MS023 2μM R03 exp134]]|0.051|<button type="primary" size="small" modal="12">View</button>|
|[[:results:exp175|3-Bromopyruvate 7μM R04 exp175]]|0.053|<button type="primary" size="small" modal="13">View</button>|
</modal>


<modal id="1" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  CB-5083 0.4μM R08 exp468">
{{:chemogenomics:comparison_plots:exp468_vs_exp6.png?nolink |}}
</modal>

<modal id="2" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  Ethanol 0.01 R05 exp234">
{{:chemogenomics:comparison_plots:exp234_vs_exp6.png?nolink |}}
</modal>

<modal id="3" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  Thapsigargin 0.005μM R07 exp407">
{{:chemogenomics:comparison_plots:exp407_vs_exp6.png?nolink |}}
</modal>

<modal id="4" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  ML-792 0.2μM R08 exp505">
{{:chemogenomics:comparison_plots:exp505_vs_exp6.png?nolink |}}
</modal>

<modal id="5" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  Olaparib 4μM R08 exp512">
{{:chemogenomics:comparison_plots:exp512_vs_exp6.png?nolink |}}
</modal>

<modal id="6" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  Tubacin 1.6μM R07 exp416">
{{:chemogenomics:comparison_plots:exp416_vs_exp6.png?nolink |}}
</modal>

<modal id="7" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  Golgicide-A 4μM R03 exp122">
{{:chemogenomics:comparison_plots:exp122_vs_exp6.png?nolink |}}
</modal>

<modal id="8" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  TRAIL 50ng/ml R00 exp36">
{{:chemogenomics:comparison_plots:exp36_vs_exp6.png?nolink |}}
</modal>

<modal id="9" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  TRAIL 5ng/ml R00 exp35">
{{:chemogenomics:comparison_plots:exp35_vs_exp6.png?nolink |}}
</modal>

<modal id="10" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  Quercetin 20μM R08 exp517">
{{:chemogenomics:comparison_plots:exp517_vs_exp6.png?nolink |}}
</modal>

<modal id="11" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  Docosahexaenoic-acid 50μM R07 exp356">
{{:chemogenomics:comparison_plots:exp356_vs_exp6.png?nolink |}}
</modal>

<modal id="12" size="lg" title="Bortezomib 0.005μM R00 exp6  vs  MS023 2μM R03 exp134">
{{:chemogenomics:comparison_plots:exp134_vs_exp6.png?nolink |}}
</modal>

<modal id="13" size="lg" title="3-Bromopyruvate 7μM R04 exp175  vs  Bortezomib 0.005μM R00 exp6">
{{:chemogenomics:comparison_plots:exp175_vs_exp6.png?nolink |}}
</modal>



<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">
^GO Term^Fold Change^Genes^
|proteasome core complex, beta-subunit complex|228.70|PSMB8,PSMB5,PSMB6,PSMB7|
|threonine-type endopeptidase activity|214.41|PSMB8,PSMB5,PSMB6|
|proteasome core complex|120.37|PSMB8,PSMB5,PSMB6,PSMB7|
|threonine-type peptidase activity|100.90|PSMB8,PSMB5,PSMB7|
|proteasome complex|47.65|PSMB8,PSMB5,ECPAS,PSMB6,PSMB7|
|endopeptidase complex|34.03|PSMB8,PSMB5,ECPAS,PSMB6,PSMB7|
|peptidase complex|24.02|PSMB8,PSMB5,ECPAS,PSMB6,PSMB7|
</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">
^GO Term^Fold Change^Genes^
|positive regulation of translation in response to endoplasmic reticulum stress|276.35|DDX3X,EIF4G1|
|eukaryotic translation initiation factor 4F complex|150.74|EIF4A1,EIF4H,EIF4G1|
|RNA cap binding complex|92.12|EIF4A1,EIF4H,EIF4G1|
|stress granule assembly|69.09|ATXN2L,DDX3X,PRRC2C|
|translational initiation|34.54|EIF4A1,EIF4H,DDX3X,EIF4G1|
|cytoplasmic stress granule|32.90|ATXN2L,DDX3X,PRRC2C,EIF4G1,YBX1|
|response to endoplasmic reticulum stress|14.80|DDX3X,EIF4G1,BAK1,UBQLN1,FAF2,UBE4A|
|intracellular protein-containing complex|6.31|EIF4A1,EIF4H,PSMB9,EIF4G1,UBQLN1,PPP3R1,YBX1,KAT7,UBE4A,UBR2|
</modal>