Fluvastatin 2.2μM R06 exp282 [The Human Chemical-Genetic Interaction Map Project]

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====== Fluvastatin 2.2μM R06 exp282 ======
==== Mechanism of Action ====
Inhibits HMG-CoA reductase, decreases cholesterol biogenesis, upregulates LDL-receptors
  * **<color #00a2e8>Class / Subclass 1:</color>** Metabolism / Metabolic Enzyme Inhibitor




==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Compound References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%Fluvastatin sodium%%
    * **<color #00a2e8>Synonyms:</color>** XU 62320 sodium
    * **<color #00a2e8>CAS #:</color>** 93957-55-2
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/23663976|23663976]]
    * **<color #00a2e8>IUPAC:</color>** %%sodium;(E,3R,5S)-7-[3-(4-fluorophenyl)-1-propan-2-ylindol-2-yl]-3,5-dihydroxyhept-6-enoate%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C24H26FNO4.Na/c1-15(2)26-21-6-4-3-5-20(21)24(16-7-9-17(25)10-8-16)22(26)12-11-18(27)13-19(28)14-23(29)30;/h3-12,15,18-19,27-28H,13-14H2,1-2H3,(H,29,30);/q;+1/p-1/b12-11+;/t18-,19-;/m1./s1
    * **<color #00a2e8>INCHI Key:</color>** ZGGHKIMDNBDHJB-NRFPMOEYSA-M
    * **<color #00a2e8>Molecular Weight:</color>** 433.4
    * **<color #00a2e8>Canonical SMILES:</color>** CC(C)N1C2=CC=CC=C2C(=C1C=CC(CC(CC(=O)[O-])O)O)C3=CC=C(C=C3)F.[Na+]
    * **<color #00a2e8>Isomeric SMILES:</color>** CC(C)N1C2=CC=CC=C2C(=C1/C=C/[C@H](C[C@H](CC(=O)[O-])O)O)C3=CC=C(C=C3)F.[Na+]
    * **<color #00a2e8>Molecular Formula:</color>** C24H25FNNaO4
{{:chemogenomics:structures:chem-0172.svg?nolink}}
</panel>


<panel title='Compound Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** Abcam
    * **<color #00a2e8>Catalog #:</color>** AB120651
    * **<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 C24H26FNO4 412.19186; found 412.19479
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** Fluvastatin
    * **<color #00a2e8>Min:</color>** -13.5075; **<color #00a2e8>Max:</color>** 81.9703
{{:chemogenomics:dose_response:dr_223.png?nolink&500 |}}
\\ 
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|< 300px 100px 200px >|
^ IC   ^ Concentration (µM) ^
| IC10  |N/A    |
| IC20  |1.5813    |
| IC30  |2.1754    |
| IC40  |2.8255    |
| IC50  |3.5917    |
| 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>**: 2.2µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 3.9
    * **<color #00a2e8>Numbers of reads</color>**: 30579784


==== 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^
|37/75|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Fluvastatin_2.2uM_Round-6_exp282.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='Fluvastatin 2.2μM R06 exp282'>
{{:chemogenomics:cranks_plots:exp282.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:U:UNC50|UNC50]]|-4.81|0.00|
|[[:human_genes:S:SCAP|SCAP]]|-4.15|0.00|
|[[:human_genes:C:C12orf49|C12orf49]]|-4.09|0.00|
|[[:human_genes:S:SLC39A9|SLC39A9]]|-3.77|0.00|
|[[:human_genes:E:ENTPD4|ENTPD4]]|-3.77|0.00|
|[[:human_genes:S:SREBF2|SREBF2]]|-3.75|<0.01|
|[[:human_genes:O:OTUB1|OTUB1]]|-3.69|0.00|
|[[:human_genes:R:RAB1B|RAB1B]]|-3.66|0.00|
|[[:human_genes:Y:YPEL5|YPEL5]]|-3.63|0.00|
|[[:human_genes:A:ACAT2|ACAT2]]|-3.55|0.00|
|[[:human_genes:M:MCTS1|MCTS1]]|-3.54|0.00|
|[[:human_genes:U:USO1|USO1]]|-3.52|0.00|
|[[:human_genes:A:ARL1|ARL1]]|-3.50|0.00|
|[[:human_genes:M:MBTPS2|MBTPS2]]|-3.43|0.00|
|[[:human_genes:S:SQLE|SQLE]]|-3.16|0.00|
|[[:human_genes:N:NADK|NADK]]|-3.16|<0.01|
|[[:human_genes:S:SLC10A7|SLC10A7]]|-3.13|0.00|
|[[:human_genes:C:COG7|COG7]]|-3.06|<0.01|
|[[:human_genes:P:PITPNB|PITPNB]]|-3.06|0.00|
|[[:human_genes:M:MBTPS1|MBTPS1]]|-2.88|0.01|
|[[:human_genes:R:RABGGTA|RABGGTA]]|-2.86|<0.01|
|[[:human_genes:T:TCF4|TCF4]]|-2.86|<0.01|
|[[:human_genes:S:SEC31A|SEC31A]]|-2.82|<0.01|
|[[:human_genes:R:RAB1A|RAB1A]]|-2.75|<0.01|
|[[:human_genes:G:GOLGA2|GOLGA2]]|-2.75|<0.01|
|[[:human_genes:E:EXOSC6|EXOSC6]]|-2.71|0.17|
|[[:human_genes:C:CTCF|CTCF]]|-2.67|0.01|
|[[:human_genes:G:GSK3B|GSK3B]]|-2.60|<0.01|
|[[:human_genes:H:HMGCR|HMGCR]]|-2.58|0.22|
|[[:human_genes:S:SLC35E1|SLC35E1]]|-2.58|<0.01|
|[[:human_genes:A:AUP1|AUP1]]|2.84|0.01|
|[[:human_genes:P:PEX12|PEX12]]|2.85|<0.01|
|[[:human_genes:R:RMND5A|RMND5A]]|2.87|<0.01|
|[[:human_genes:U:UBE2H|UBE2H]]|2.88|<0.01|
|[[:human_genes:P:PEX1|PEX1]]|2.94|<0.01|
|[[:human_genes:P:PEX3|PEX3]]|2.94|<0.01|
|[[:human_genes:K:KLF16|KLF16]]|2.97|<0.01|
|[[:human_genes:C:CREBBP|CREBBP]]|2.98|0.00|
|[[:human_genes:M:MKLN1|MKLN1]]|3.04|0.00|
|[[:human_genes:S:STT3A|STT3A]]|3.13|<0.01|
|[[:human_genes:P:PEX2|PEX2]]|3.15|0.00|
|[[:human_genes:A:ACACA|ACACA]]|3.17|0.00|
|[[:human_genes:M:MAEA|MAEA]]|3.17|0.00|
|[[:human_genes:A:ACTR5|ACTR5]]|3.19|0.00|
|[[:human_genes:C:C7orf26|C7orf26]]|3.29|0.00|
|[[:human_genes:R:RPRD1B|RPRD1B]]|3.33|<0.01|
|[[:human_genes:R:RER1|RER1]]|3.38|0.00|
|[[:human_genes:A:ACSL3|ACSL3]]|3.41|0.00|
|[[:human_genes:I:INO80C|INO80C]]|3.43|0.00|
|[[:human_genes:I:INTS10|INTS10]]|3.51|0.00|
|[[:human_genes:H:HSP90B1|HSP90B1]]|3.52|0.00|
|[[:human_genes:F:FDFT1|FDFT1]]|3.53|0.00|
|[[:human_genes:A:ARMC8|ARMC8]]|3.91|0.00|
|[[:human_genes:A:ASUN|ASUN]]|4.01|0.00|
|[[:human_genes:H:HMGCL|HMGCL]]|4.13|0.00|
|[[:human_genes:E:EIF4A1|EIF4A1]]|4.60|0.00|
|[[:human_genes:F:FAF2|FAF2]]|4.98|0.00|
|[[:human_genes:L:LDLR|LDLR]]|5.11|0.00|
|[[:human_genes:A:ABCD3|ABCD3]]|6.02|0.00|
|[[:human_genes:L:LDLRAP1|LDLRAP1]]|7.00|0.00|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp226|Cerivastatin 0.15μM R05 exp226]]|0.287|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp67|BVD-523 15μM R02 exp67]]|0.057|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp452|Azithromycin 100μM R08 exp452]]|0.054|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp68|Clomiphene 4.4μM R02 exp68]]|0.053|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp454|Bafilomycin-A1 0.009μM R08 exp454]]|0.051|<button type="primary" size="small" modal="5">View</button>|
</modal>


<modal id="1" size="lg" title="Cerivastatin 0.15μM R05 exp226  vs  Fluvastatin 2.2μM R06 exp282">
{{:chemogenomics:comparison_plots:exp226_vs_exp282.png?nolink |}}
</modal>

<modal id="2" size="lg" title="BVD-523 15μM R02 exp67  vs  Fluvastatin 2.2μM R06 exp282">
{{:chemogenomics:comparison_plots:exp282_vs_exp67.png?nolink |}}
</modal>

<modal id="3" size="lg" title="Azithromycin 100μM R08 exp452  vs  Fluvastatin 2.2μM R06 exp282">
{{:chemogenomics:comparison_plots:exp282_vs_exp452.png?nolink |}}
</modal>

<modal id="4" size="lg" title="Clomiphene 4.4μM R02 exp68  vs  Fluvastatin 2.2μM R06 exp282">
{{:chemogenomics:comparison_plots:exp282_vs_exp68.png?nolink |}}
</modal>

<modal id="5" size="lg" title="Bafilomycin-A1 0.009μM R08 exp454  vs  Fluvastatin 2.2μM R06 exp282">
{{:chemogenomics:comparison_plots:exp282_vs_exp454.png?nolink |}}
</modal>



<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">
^GO Term^Fold Change^Genes^
|COPII-coated vesicle cargo loading|126.84|SCAP,SEC31A,RAB1A|
|regulation of cholesterol biosynthetic process|98.65|SREBF2,MBTPS2,MBTPS1|
|regulation of sterol biosynthetic process|98.65|SCAP,MBTPS2,MBTPS1|
|ER-nucleus signaling pathway|98.65|SCAP,SREBF2,MBTPS2,MBTPS1,GSK3B|
|positive regulation of glycoprotein metabolic process|73.99|RAB1B,RAB1A,GOLGA2|
|regulation of cholesterol metabolic process|69.64|SCAP,SREBF2,MBTPS2,MBTPS1|
|regulation of alcohol biosynthetic process|49.33|SCAP,SREBF2,MBTPS2,MBTPS1|
|ER to Golgi transport vesicle membrane|40.13|SCAP,SREBF2,USO1,SEC31A|
|COPII-coated ER to Golgi transport vesicle|33.25|SCAP,SREBF2,USO1,SEC31A,GOLGA2|
|regulation of steroid biosynthetic process|32.43|SCAP,SREBF2,MBTPS2,MBTPS1|
|cholesterol metabolic process|30.88|SCAP,SREBF2,MBTPS2,SQLE,MBTPS1,HMGCR|
|endoplasmic reticulum to Golgi vesicle-mediated transport|28.41|SCAP,RAB1B,USO1,SEC31A,RAB1A,GOLGA2|
|secondary alcohol metabolic process|28.41|SCAP,SREBF2,MBTPS2,SQLE,MBTPS1,HMGCR|
|sterol metabolic process|27.75|SCAP,SREBF2,MBTPS2,SQLE,MBTPS1,HMGCR|
|Golgi organization|26.70|RAB1B,USO1,ARL1,COG7,RAB1A,GOLGA2|
|Golgi vesicle transport|19.37|SCAP,RAB1B,USO1,SLC10A7,COG7,PITPNB,SEC31A,RAB1A,GOLGA2|
|steroid metabolic process|14.09|SCAP,SREBF2,MBTPS2,SQLE,MBTPS1,HMGCR|
|Golgi membrane|12.63|UNC50,SCAP,ENTPD4,SREBF2,RAB1B,USO1,ARL1,MBTPS2,SLC10A7,COG7,PITPNB,MBTPS1,RAB1A,GOLGA2|
|Golgi apparatus subcompartment|11.38|SLC39A9,USO1,ARL1,SLC10A7,COG7,MBTPS1,GOLGA2|
</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">
^GO Term^Fold Change^Genes^
|GID complex|414.35|ARMC8,MAEA,RMND5A|
|protein import into peroxisome matrix, receptor recycling|276.23|PEX2,PEX1,PEX12|
|peroxisomal membrane transport|131.54|ABCD3,PEX2,PEX3,PEX1,PEX12|
|peroxisomal transport|120.10|ABCD3,PEX2,PEX3,PEX1,PEX12|
|protein targeting to peroxisome|116.31|PEX2,PEX3,PEX1,PEX12|
|retrograde protein transport, ER to cytosol|97.49|FAF2,HSP90B1,AUP1|
|endoplasmic reticulum to cytosol transport|97.49|FAF2,HSP90B1,AUP1|
|establishment of protein localization to peroxisome|87.23|PEX2,PEX1,PEX12|
|peroxisome organization|83.71|ABCD3,PEX2,PEX3,PEX1,PEX12|
|microbody membrane|51.79|ABCD3,ACSL3,PEX2,PEX3,PEX1,PEX12|
|peroxisomal membrane|51.79|ABCD3,ACSL3,PEX2,PEX3,PEX1,PEX12|
|microbody|27.04|ABCD3,HMGCL,ACSL3,PEX2,PEX3,PEX1,PEX12|
|peroxisome|27.04|ABCD3,HMGCL,ACSL3,PEX2,PEX3,PEX1,PEX12|
|proteasome-mediated ubiquitin-dependent protein catabolic process|12.81|FAF2,ARMC8,HSP90B1,MAEA,UBE2H,RMND5A,PEX12,AUP1|
|proteasomal protein catabolic process|11.63|FAF2,ARMC8,HSP90B1,MAEA,UBE2H,RMND5A,PEX12,AUP1|
|ubiquitin-dependent protein catabolic process|8.65|FAF2,ARMC8,HSP90B1,MAEA,UBE2H,RMND5A,PEX12,AUP1|
|modification-dependent protein catabolic process|8.48|FAF2,ARMC8,HSP90B1,MAEA,UBE2H,RMND5A,PEX12,AUP1|
|modification-dependent macromolecule catabolic process|8.31|FAF2,ARMC8,HSP90B1,MAEA,UBE2H,RMND5A,PEX12,AUP1|
|protein catabolic process|7.15|LDLR,FAF2,ARMC8,HSP90B1,MAEA,UBE2H,RMND5A,PEX12,AUP1|
</modal>