Trametinib 10μM R02 exp83 [The Human Chemical-Genetic Interaction Map Project]

This page is read only. You can view the source, but not change it. Ask your administrator if you think this is wrong.
====== Trametinib 10μM R02 exp83 ======
==== Mechanism of Action ====
Inhibits MEK1 and MEK2, reversible allosteric mechanism, used in combination with BRAF V600E inhibitors
  * **<color #00a2e8>Class / Subclass 1:</color>** Signal Transduction / Kinase Inhibitor




==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Compound References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%Trametinib%%
    * **<color #00a2e8>Synonyms:</color>** GSK1120212; JTP-74057
    * **<color #00a2e8>CAS #:</color>** 871700-17-3
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/11707110|11707110]]
    * **<color #00a2e8>IUPAC:</color>** %%N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)
    * **<color #00a2e8>INCHI Key:</color>** LIRYPHYGHXZJBZ-UHFFFAOYSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 615.4
    * **<color #00a2e8>Canonical SMILES:</color>** CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC=CC(=C4)NC(=O)C)C5CC5
    * **<color #00a2e8>Isomeric SMILES:</color>** N/A
    * **<color #00a2e8>Molecular Formula:</color>** C26H23FIN5O4
{{:chemogenomics:structures:chem-0059.svg?nolink}}
</panel>


<panel title='Compound Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** Selleck Chemicals
    * **<color #00a2e8>Catalog #:</color>** S2673
    * **<color #00a2e8>Lot #:</color>** S267306
</panel>


<panel title='Compound Characterization' collapsed='true'>
    * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+H)+ Calcd for C26H23FIN5O4 616.08515; found 616.08594
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** GSK1120212
    * **<color #00a2e8>Min:</color>** -14.6969; **<color #00a2e8>Max:</color>** 3.8984
{{:chemogenomics:dose_response:dr_37.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>**: 02
    * **<color #00a2e8>Dose</color>**: 10µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 6.0
    * **<color #00a2e8>Numbers of reads</color>**: 12205762


==== 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^
|5/2|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Trametinib_10uM_Round-2_exp83.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="default" size="sm" modal="modal_go_resistant">View</button>|
<modal id='ScorePlot' size='lg' title='Trametinib 10μM R02 exp83'>
{{:chemogenomics:cranks_plots:exp83.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:G:GPR107|GPR107]]|-3.13|<0.01|
|[[:human_genes:D:DERL2|DERL2]]|-2.86|0.02|
|[[:human_genes:K:KDSR|KDSR]]|-2.84|0.02|
|[[:human_genes:D:DNAJC3|DNAJC3]]|-2.81|0.02|
|[[:human_genes:Z:ZBTB7A|ZBTB7A]]|-2.76|0.02|
|[[:human_genes:A:ALG6|ALG6]]|-2.64|0.07|
|[[:human_genes:T:TMEM64|TMEM64]]|-2.63|0.09|
|[[:human_genes:C:CEPT1|CEPT1]]|-2.58|0.07|
|[[:human_genes:F:FLVCR1|FLVCR1]]|-2.53|0.08|
|[[:human_genes:H:HIST1H4E|HIST1H4E]]|-2.44|0.07|
|[[:human_genes:S:SLC7A5|SLC7A5]]|-2.41|0.07|
|[[:human_genes:U:UHRF1|UHRF1]]|-2.36|0.12|
|[[:human_genes:C:CD72|CD72]]|-2.35|0.12|
|[[:human_genes:S:SAP130|SAP130]]|-2.33|0.12|
|[[:human_genes:U:UBE3A|UBE3A]]|-2.33|0.09|
|[[:human_genes:P:PRRC1|PRRC1]]|-2.32|0.20|
|[[:human_genes:A:ATXN7L3|ATXN7L3]]|-2.32|0.20|
|[[:human_genes:M:MPDU1|MPDU1]]|-2.29|0.10|
|[[:human_genes:H:HIF1AN|HIF1AN]]|-2.25|0.12|
|[[:human_genes:A:ARFRP1|ARFRP1]]|-2.21|0.12|
|[[:human_genes:D:DCAF15|DCAF15]]|-2.20|0.12|
|[[:human_genes:C:CCDC37|CCDC37]]|-2.18|0.26|
|[[:human_genes:D:DCAF8L1|DCAF8L1]]|-2.17|0.13|
|[[:human_genes:A:ALG12|ALG12]]|-2.15|0.21|
|[[:human_genes:P:PTPN6|PTPN6]]|-2.15|0.21|
|[[:human_genes:N:NBPF9|NBPF9]]|-2.14|0.15|
|[[:human_genes:A:ARL1|ARL1]]|-2.12|0.16|
|[[:human_genes:T:TOP1|TOP1]]|-2.11|0.22|
|[[:human_genes:S:SCAF8|SCAF8]]|-2.09|0.18|
|[[:human_genes:F:FDPS|FDPS]]|-2.07|0.29|
|[[:human_genes:J:JMY|JMY]]|1.98|0.69|
|[[:human_genes:A:ACCS|ACCS]]|2.02|0.62|
|[[:human_genes:S:STXBP6|STXBP6]]|2.03|0.41|
|[[:human_genes:M:MCUR1|MCUR1]]|2.07|0.66|
|[[:human_genes:D:DNM2|DNM2]]|2.07|0.80|
|[[:human_genes:K:KREMEN1|KREMEN1]]|2.08|0.66|
|[[:human_genes:C:CMYA5|CMYA5]]|2.10|0.50|
|[[:human_genes:H:HIST1H1E|HIST1H1E]]|2.11|0.35|
|[[:human_genes:C:CHAF1A|CHAF1A]]|2.15|0.67|
|[[:human_genes:R:RPRD1B|RPRD1B]]|2.16|0.29|
|[[:human_genes:P:PDHB|PDHB]]|2.16|0.41|
|[[:human_genes:E:EXO1|EXO1]]|2.17|0.41|
|[[:human_genes:R:RB1|RB1]]|2.21|0.37|
|[[:human_genes:H:HINFP|HINFP]]|2.22|0.69|
|[[:human_genes:P:PSMC2|PSMC2]]|2.23|0.71|
|[[:human_genes:C:CCDC18|CCDC18]]|2.25|0.77|
|[[:human_genes:N:NUP160|NUP160]]|2.25|0.69|
|[[:human_genes:A:ATP6AP1|ATP6AP1]]|2.26|0.69|
|[[:human_genes:C:CALR|CALR]]|2.26|0.20|
|[[:human_genes:F:FAM46C|FAM46C]]|2.27|0.20|
|[[:human_genes:S:S100A2|S100A2]]|2.35|0.57|
|[[:human_genes:Z:ZSCAN12|ZSCAN12]]|2.37|0.67|
|[[:human_genes:P:PRPF4|PRPF4]]|2.39|0.69|
|[[:human_genes:C:CDK8|CDK8]]|2.43|0.20|
|[[:human_genes:F:FAM122A|FAM122A]]|2.54|0.06|
|[[:human_genes:P:PHF6|PHF6]]|2.55|0.06|
|[[:human_genes:E:ETV3|ETV3]]|2.68|0.26|
|[[:human_genes:C:CDK10|CDK10]]|2.75|0.06|
|[[:human_genes:S:SCAP|SCAP]]|3.05|0.02|
|[[:human_genes:C:CDK2|CDK2]]|3.26|<0.01|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp457|Bisphenol F 50μM R08 exp457]]|0.078|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp453|B02 10μM R08 exp453]]|0.071|<button type="primary" size="small" modal="2">View</button>|
|[[:results:exp433|LJH685 50μM R08 exp433]]|0.069|<button type="primary" size="small" modal="3">View</button>|
|[[:results:exp149|SB203580 25μM R03 exp149]]|0.062|<button type="primary" size="small" modal="4">View</button>|
|[[:results:exp470|Chloroquine 32μM R08 exp470]]|0.052|<button type="primary" size="small" modal="5">View</button>|
|[[:results:exp47|Lapatinib 5μM R01 exp47]]|0.051|<button type="primary" size="small" modal="6">View</button>|
</modal>


<modal id="1" size="lg" title="Bisphenol F 50μM R08 exp457  vs  Trametinib 10μM R02 exp83">
{{:chemogenomics:comparison_plots:exp457_vs_exp83.png?nolink |}}
</modal>

<modal id="2" size="lg" title="B02 10μM R08 exp453  vs  Trametinib 10μM R02 exp83">
{{:chemogenomics:comparison_plots:exp453_vs_exp83.png?nolink |}}
</modal>

<modal id="3" size="lg" title="LJH685 50μM R08 exp433  vs  Trametinib 10μM R02 exp83">
{{:chemogenomics:comparison_plots:exp433_vs_exp83.png?nolink |}}
</modal>

<modal id="4" size="lg" title="SB203580 25μM R03 exp149  vs  Trametinib 10μM R02 exp83">
{{:chemogenomics:comparison_plots:exp149_vs_exp83.png?nolink |}}
</modal>

<modal id="5" size="lg" title="Chloroquine 32μM R08 exp470  vs  Trametinib 10μM R02 exp83">
{{:chemogenomics:comparison_plots:exp470_vs_exp83.png?nolink |}}
</modal>

<modal id="6" size="lg" title="Lapatinib 5μM R01 exp47  vs  Trametinib 10μM R02 exp83">
{{:chemogenomics:comparison_plots:exp47_vs_exp83.png?nolink |}}
</modal>



<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">
^GO Term^Fold Change^Genes^
|oligosaccharide-lipid intermediate biosynthetic process|92.13|ALG6,MPDU1,ALG12|
|dolichol metabolic process|87.75|ALG6,MPDU1,ALG12|
|polyprenol metabolic process|80.12|ALG6,MPDU1,ALG12|
</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">No GO term hits below threshold. (FDR <0.05)</modal>