====== Trametinib 10μM R02 exp83 ======
==== Mechanism of Action ====
Inhibits MEK1 and MEK2, reversible allosteric mechanism, used in combination with BRAF V600E inhibitors
* **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%Trametinib%%
* **Synonyms:** GSK1120212; JTP-74057
* **CAS #:** 871700-17-3
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/11707110|11707110]]
* **IUPAC:** %%N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide%%
* **INCHI Name:** 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)
* **INCHI Key:** LIRYPHYGHXZJBZ-UHFFFAOYSA-N
* **Molecular Weight:** 615.4
* **Canonical SMILES:** 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
* **Isomeric SMILES:** N/A
* **Molecular Formula:** C26H23FIN5O4
{{:chemogenomics:structures:chem-0059.svg?nolink}}
* **Supplier Name:** Selleck Chemicals
* **Catalog #:** S2673
* **Lot #:** S267306
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C26H23FIN5O4 616.08515; found 616.08594
* **Platform ID:** GSK1120212
* **Min:** -14.6969; **Max:** 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 |
\\
==== Screen Summary ====
* **Round**: 02
* **Dose**: 10µM
* **Days of incubation**: 8
* **Doublings**: 6.0
* **Numbers of reads**: 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|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Trametinib_10uM_Round-2_exp83.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp83.png?nolink}}
^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|
^Screen^Correlation^Plot^
|[[:results:exp457|Bisphenol F 50μM R08 exp457]]|0.078||
|[[:results:exp453|B02 10μM R08 exp453]]|0.071||
|[[:results:exp433|LJH685 50μM R08 exp433]]|0.069||
|[[:results:exp149|SB203580 25μM R03 exp149]]|0.062||
|[[:results:exp470|Chloroquine 32μM R08 exp470]]|0.052||
|[[:results:exp47|Lapatinib 5μM R01 exp47]]|0.051||
{{:chemogenomics:comparison_plots:exp457_vs_exp83.png?nolink |}}
{{:chemogenomics:comparison_plots:exp453_vs_exp83.png?nolink |}}
{{:chemogenomics:comparison_plots:exp433_vs_exp83.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp83.png?nolink |}}
{{:chemogenomics:comparison_plots:exp470_vs_exp83.png?nolink |}}
{{:chemogenomics:comparison_plots:exp47_vs_exp83.png?nolink |}}
^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|
No GO term hits below threshold. (FDR <0.05)