Rapamycin 1μM R00 exp29 [The Human Chemical-Genetic Interaction Map Project]

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====== Rapamycin 1μM R00 exp29 ======
==== Mechanism of Action ====
Allosteric mTORC1 inhibitor, forms ternary complex with FKBP12 and mTOR, attenuates protein synthesis and metabolism
  * **<color #00a2e8>Class / Subclass 1:</color>** Signal Transduction / Kinase Inhibitor
  * **<color #00a2e8>Class / Subclass 2:</color>** Proteostasis / mTOR inhibitor



==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Compound References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%Sirolimus%%
    * **<color #00a2e8>Synonyms:</color>** Sirolimus; AY 22989
    * **<color #00a2e8>CAS #:</color>** 53123-88-9
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/5284616|5284616]]
    * **<color #00a2e8>IUPAC:</color>** %%(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11+,16-12+,31-17+,35-25+/t30-,32-,33-,34-,36-,37+,38+,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1
    * **<color #00a2e8>INCHI Key:</color>** QFJCIRLUMZQUOT-HPLJOQBZSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 914.2
    * **<color #00a2e8>Canonical SMILES:</color>** CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)O)C)C)O)OC)C)C)C)OC
    * **<color #00a2e8>Isomeric SMILES:</color>** C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)O)C)/C)O)OC)C)C)/C)OC
    * **<color #00a2e8>Molecular Formula:</color>** C51H79NO13
{{:chemogenomics:structures:chem-0016.svg?nolink}}
</panel>


<panel title='Compound Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** LC Laboratories
    * **<color #00a2e8>Catalog #:</color>** R-5000
    * **<color #00a2e8>Lot #:</color>** ASW-130
</panel>


<panel title='Compound Characterization' collapsed='true'>
    * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+Na)+ Calcd for C51H79NO13 936.54436; found 936.54366
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** Rapamycin
    * **<color #00a2e8>Min:</color>** 29.4254; **<color #00a2e8>Max:</color>** 49.7567
{{:chemogenomics:dose_response:dr_273.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>**: 00
    * **<color #00a2e8>Dose</color>**: 1µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 5.2
    * **<color #00a2e8>Numbers of reads</color>**: 10402895


==== 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^
|7/45|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Rapamycin_1uM_Round-0_exp29.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='Rapamycin 1μM R00 exp29'>
{{:chemogenomics:cranks_plots:exp29.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:U:UXS1|UXS1]]|-3.75|<0.01|
|[[:human_genes:O:ORC3|ORC3]]|-3.44|<0.01|
|[[:human_genes:A:ASB3|ASB3]]|-3.42|<0.01|
|[[:human_genes:L:LMO2|LMO2]]|-3.00|<0.01|
|[[:human_genes:L:LAMTOR4|LAMTOR4]]|-2.96|0.01|
|[[:human_genes:S:SOX7|SOX7]]|-2.86|0.02|
|[[:human_genes:D:DHX29|DHX29]]|-2.69|0.02|
|[[:human_genes:M:MNS1|MNS1]]|-2.58|0.06|
|[[:human_genes:R:RRAGA|RRAGA]]|-2.55|0.06|
|[[:human_genes:C:COX7A2L|COX7A2L]]|-2.46|0.06|
|[[:human_genes:G:GNA13|GNA13]]|-2.44|0.06|
|[[:human_genes:M:MEF2C|MEF2C]]|-2.42|0.06|
|[[:human_genes:X:XPOT|XPOT]]|-2.41|0.09|
|[[:human_genes:E:ERG|ERG]]|-2.40|0.09|
|[[:human_genes:G:GPR75-ASB3|GPR75-ASB3]]|-2.37|0.07|
|[[:human_genes:T:TRIP12|TRIP12]]|-2.35|0.07|
|[[:human_genes:X:XPO5|XPO5]]|-2.33|0.21|
|[[:human_genes:D:DCAF15|DCAF15]]|-2.27|0.10|
|[[:human_genes:P:PHF15|PHF15]]|-2.26|0.09|
|[[:human_genes:C:CAMK2G|CAMK2G]]|-2.26|0.09|
|[[:human_genes:F:FAF2|FAF2]]|-2.24|0.12|
|[[:human_genes:I:ID3|ID3]]|-2.24|0.09|
|[[:human_genes:D:DCAF5|DCAF5]]|-2.24|0.09|
|[[:human_genes:S:SETD1B|SETD1B]]|-2.23|0.20|
|[[:human_genes:E:EIF4E|EIF4E]]|-2.23|0.09|
|[[:human_genes:A:ATF7IP|ATF7IP]]|-2.23|0.09|
|[[:human_genes:Z:ZBTB7A|ZBTB7A]]|-2.22|0.09|
|[[:human_genes:T:TRIM33|TRIM33]]|-2.20|0.09|
|[[:human_genes:L:LAMTOR2|LAMTOR2]]|-2.19|0.09|
|[[:human_genes:C:CALCB|CALCB]]|-2.19|0.15|
|[[:human_genes:G:GID8|GID8]]|2.61|<0.01|
|[[:human_genes:N:NME9|NME9]]|2.71|<0.01|
|[[:human_genes:N:NCK1|NCK1]]|2.71|<0.01|
|[[:human_genes:Z:ZFR|ZFR]]|2.72|0.09|
|[[:human_genes:C:C19orf53|C19orf53]]|2.73|0.02|
|[[:human_genes:R:RPS28|RPS28]]|2.73|0.16|
|[[:human_genes:S:SLC25A1|SLC25A1]]|2.75|<0.01|
|[[:human_genes:W:WEE1|WEE1]]|2.79|0.07|
|[[:human_genes:S:SCAP|SCAP]]|2.81|<0.01|
|[[:human_genes:B:BTK|BTK]]|2.84|<0.01|
|[[:human_genes:C:CNOT7|CNOT7]]|2.96|<0.01|
|[[:human_genes:P:PSMD11|PSMD11]]|3.01|<0.01|
|[[:human_genes:A:ANP32E|ANP32E]]|3.02|<0.01|
|[[:human_genes:G:GSK3B|GSK3B]]|3.04|<0.01|
|[[:human_genes:M:MAEA|MAEA]]|3.07|<0.01|
|[[:human_genes:W:WDR26|WDR26]]|3.08|<0.01|
|[[:human_genes:P:PDS5B|PDS5B]]|3.16|<0.01|
|[[:human_genes:P:PPP3CA|PPP3CA]]|3.20|<0.01|
|[[:human_genes:O:OTUB1|OTUB1]]|3.34|<0.01|
|[[:human_genes:C:CNOT2|CNOT2]]|3.46|<0.01|
|[[:human_genes:K:KMT2E|KMT2E]]|3.59|<0.01|
|[[:human_genes:C:CXorf56|CXorf56]]|3.68|<0.01|
|[[:human_genes:F:FAM122A|FAM122A]]|3.85|<0.01|
|[[:human_genes:M:MEMO1|MEMO1]]|3.88|<0.01|
|[[:human_genes:C:CDK8|CDK8]]|4.00|<0.01|
|[[:human_genes:P:PPP3R1|PPP3R1]]|4.37|<0.01|
|[[:human_genes:U:UBE2H|UBE2H]]|4.64|<0.01|
|[[:human_genes:C:CNOT8|CNOT8]]|5.66|<0.01|
|[[:human_genes:Y:YPEL5|YPEL5]]|5.81|<0.01|
|[[:human_genes:F:FKBP1A|FKBP1A]]|7.84|<0.01|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp306|Rapamycin 2μM R07 exp306]]|0.14|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp308|Rapamycin 2μM plus FK-506 5μM R07 exp308]]|0.102|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp307|Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307]]|0.079|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp82|Torin1 0.08μM R02 exp82]]|0.055|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp37|Wortmannin 0.5μM R00 exp37]]|0.051|<button type="primary" size="small" modal="5">View</button>|
|[[:results:exp30|Rapamycin 10μM R00 exp30]]|0.185|<button type="primary" size="small" modal="6">View</button>|
|[[:results:exp429|Rapamycin 0.001μM R08 exp429]]|0.164|<button type="primary" size="small" modal="7">View</button>|
|[[:results:exp352|Dexamethasone 0.006 to 0.015μM on day4 R07 exp352]]|0.06|<button type="primary" size="small" modal="8">View</button>|
|[[:results:exp351|Dexamethasone 0.006μM R07 exp351]]|0.059|<button type="primary" size="small" modal="9">View</button>|
|[[:results:exp15|Cycloheximide 0.2μM R00 exp15]]|0.058|<button type="primary" size="small" modal="10">View</button>|
|[[:results:exp70|INK128 0.2μM R02 exp70]]|0.057|<button type="primary" size="small" modal="11">View</button>|
|[[:results:exp71|KU-0063794 3.8μM R02 exp71]]|0.054|<button type="primary" size="small" modal="12">View</button>|
|[[:results:exp25|Oligomycin-A 2μM R00 exp25]]|0.054|<button type="primary" size="small" modal="13">View</button>|
|[[:results:exp504|MK2206 4μM R08 exp504]]|0.052|<button type="primary" size="small" modal="14">View</button>|
|[[:results:exp16|DABN 2μM R00 exp16]]|0.052|<button type="primary" size="small" modal="15">View</button>|
|[[:results:exp13|Chloramphenicol 20μM R00 exp13]]|0.052|<button type="primary" size="small" modal="16">View</button>|
</modal>


<modal id="1" size="lg" title="Rapamycin 1μM R00 exp29  vs  Rapamycin 2μM R07 exp306">
{{:chemogenomics:comparison_plots:exp29_vs_exp306.png?nolink |}}
</modal>

<modal id="2" size="lg" title="Rapamycin 1μM R00 exp29  vs  Rapamycin 2μM plus FK-506 5μM R07 exp308">
{{:chemogenomics:comparison_plots:exp29_vs_exp308.png?nolink |}}
</modal>

<modal id="3" size="lg" title="Rapamycin 1μM R00 exp29  vs  Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307">
{{:chemogenomics:comparison_plots:exp29_vs_exp307.png?nolink |}}
</modal>

<modal id="4" size="lg" title="Rapamycin 1μM R00 exp29  vs  Torin1 0.08μM R02 exp82">
{{:chemogenomics:comparison_plots:exp29_vs_exp82.png?nolink |}}
</modal>

<modal id="5" size="lg" title="Rapamycin 1μM R00 exp29  vs  Wortmannin 0.5μM R00 exp37">
{{:chemogenomics:comparison_plots:exp29_vs_exp37.png?nolink |}}
</modal>

<modal id="6" size="lg" title="Rapamycin 10μM R00 exp30  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp29_vs_exp30.png?nolink |}}
</modal>

<modal id="7" size="lg" title="Rapamycin 0.001μM R08 exp429  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp29_vs_exp429.png?nolink |}}
</modal>

<modal id="8" size="lg" title="Dexamethasone 0.006 to 0.015μM on day4 R07 exp352  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp29_vs_exp352.png?nolink |}}
</modal>

<modal id="9" size="lg" title="Dexamethasone 0.006μM R07 exp351  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp29_vs_exp351.png?nolink |}}
</modal>

<modal id="10" size="lg" title="Cycloheximide 0.2μM R00 exp15  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp15_vs_exp29.png?nolink |}}
</modal>

<modal id="11" size="lg" title="INK128 0.2μM R02 exp70  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp29_vs_exp70.png?nolink |}}
</modal>

<modal id="12" size="lg" title="KU-0063794 3.8μM R02 exp71  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp29_vs_exp71.png?nolink |}}
</modal>

<modal id="13" size="lg" title="Oligomycin-A 2μM R00 exp25  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp25_vs_exp29.png?nolink |}}
</modal>

<modal id="14" size="lg" title="MK2206 4μM R08 exp504  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp29_vs_exp504.png?nolink |}}
</modal>

<modal id="15" size="lg" title="DABN 2μM R00 exp16  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp16_vs_exp29.png?nolink |}}
</modal>

<modal id="16" size="lg" title="Chloramphenicol 20μM R00 exp13  vs  Rapamycin 1μM R00 exp29">
{{:chemogenomics:comparison_plots:exp13_vs_exp29.png?nolink |}}
</modal>



<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">
^GO Term^Fold Change^Genes^
|GTPase activator complex|177.65|LAMTOR4,RRAGA,LAMTOR2|
|enzyme activator complex|118.44|LAMTOR4,RRAGA,LAMTOR2|
</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">
^GO Term^Fold Change^Genes^
|negative regulation of calcium ion import across plasma membrane|276.35|PPP3R1,PPP3CA|
|GID complex|276.35|WDR26,MAEA|
|CCR4-NOT core complex|221.08|CNOT2,CNOT7|
|cellular response to interleukin-3|221.08|GSK3B,GSK3A|
|negative regulation of glycogen biosynthetic process|221.08|GSK3B,GSK3A|
|poly(A)-specific ribonuclease activity|138.18|CNOT8,CNOT2,CNOT7|
|3-5-RNA exonuclease activity|47.37|CNOT8,CNOT2,CNOT7|
|RNA exonuclease activity, producing 5-phosphomonoesters|43.63|CNOT8,CNOT2,CNOT7|
|regulation of calcineurin-NFAT signaling cascade|43.63|PPP3R1,PPP3CA,GSK3B|
|regulation of calcineurin-mediated signaling|42.52|PPP3R1,PPP3CA,GSK3B|
|proteasome-mediated ubiquitin-dependent protein catabolic process|11.25|UBE2H,WDR26,MAEA,GSK3B,PSMD11,GID8,GSK3A|
|proteasomal protein catabolic process|10.21|UBE2H,WDR26,MAEA,GSK3B,PSMD11,GID8,GSK3A|
|proteolysis involved in protein catabolic process|7.60|UBE2H,WDR26,MAEA,GSK3B,PSMD11,CLPP,GID8,GSK3A|
|ubiquitin-dependent protein catabolic process|7.59|UBE2H,WDR26,MAEA,GSK3B,PSMD11,GID8,GSK3A|
|intracellular protein-containing complex|7.57|YPEL5,CNOT8,PPP3R1,CNOT2,PPP3CA,WDR26,MAEA,GSK3B,PSMD11,CNOT7,GID8,GSK3A|
|modification-dependent protein catabolic process|7.44|UBE2H,WDR26,MAEA,GSK3B,PSMD11,GID8,GSK3A|
|modification-dependent macromolecule catabolic process|7.29|UBE2H,WDR26,MAEA,GSK3B,PSMD11,GID8,GSK3A|
|macromolecule catabolic process|7.20|CNOT8,UBE2H,CNOT2,WDR26,MAEA,GSK3B,PSMD11,CNOT7,BTK,CLPP,GID8,GSK3A|
|protein catabolic process|7.17|UBE2H,WDR26,MAEA,GSK3B,PSMD11,BTK,CLPP,GID8,GSK3A|
</modal>