====== GSK2606414 1μM R05 exp236 ======
==== Mechanism of Action ====
Inhibits PERK, also KIT receptor
* **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%CID 53469448%%
* **Synonyms:** N/A
* **CAS #:** 1337531-36-8
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/53469448|53469448]]
* **IUPAC:** %%1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone%%
* **INCHI Name:** InChI=1S/C24H20F3N5O/c1-31-12-18(21-22(28)29-13-30-23(21)31)15-5-6-19-16(11-15)7-8-32(19)20(33)10-14-3-2-4-17(9-14)24(25,26)27/h2-6,9,11-13H,7-8,10H2,1H3,(H2,28,29,30)
* **INCHI Key:** SIXVRXARNAVBTC-UHFFFAOYSA-N
* **Molecular Weight:** 451.4
* **Canonical SMILES:** CN1C=C(C2=C(N=CN=C21)N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F
* **Isomeric SMILES:** N/A
* **Molecular Formula:** C24H20F3N5O
{{:chemogenomics:structures:chem-0141.svg?nolink}}
* **Supplier Name:** N/A
* **Catalog #:** N/A
* **Lot #:** N/A
* **HRMS (ESI-TOF) m/z:** [M+H]+ Calcd for C21H21F3N5O 452.1693; found 452.1682
* **Platform ID:** GSK2606414
* **Min:** -5.0193; **Max:** 14.8932
{{:chemogenomics:dose_response:dr_224.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**: 05
* **Dose**: 1µM
* **Days of incubation**: 8
* **Doublings**: 6.8
* **Numbers of reads**: 13642122
==== 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^
|1/1|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/GSK2606414_1uM_Round-5_exp236.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp236.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:T:TTC37|TTC37]]|-3.12|0.03|
|[[:human_genes:A:ASB3|ASB3]]|-2.63|0.07|
|[[:human_genes:M:MBTPS2|MBTPS2]]|-2.61|0.07|
|[[:human_genes:D:DEXI|DEXI]]|-2.50|0.08|
|[[:human_genes:F:FRRS1|FRRS1]]|-2.49|0.15|
|[[:human_genes:R:RHOA|RHOA]]|-2.48|0.08|
|[[:human_genes:M:MCM9|MCM9]]|-2.37|0.23|
|[[:human_genes:S:SREK1|SREK1]]|-2.21|0.23|
|[[:human_genes:P:PCYT1A|PCYT1A]]|-2.20|0.23|
|[[:human_genes:M:MBTPS1|MBTPS1]]|-2.19|0.36|
|[[:human_genes:H:HAUS8|HAUS8]]|-2.19|0.23|
|[[:human_genes:C:CDIPT|CDIPT]]|-2.17|0.36|
|[[:human_genes:C:C20orf96|C20orf96]]|-2.17|0.23|
|[[:human_genes:C:CTU1|CTU1]]|-2.16|0.23|
|[[:human_genes:F:FOXJ3|FOXJ3]]|-2.15|0.23|
|[[:human_genes:A:AGMAT|AGMAT]]|-2.13|0.23|
|[[:human_genes:H:HMBS|HMBS]]|-2.12|0.32|
|[[:human_genes:P:PPHLN1|PPHLN1]]|-2.12|0.32|
|[[:human_genes:P:PMM2|PMM2]]|-2.07|0.31|
|[[:human_genes:E:EPT1|EPT1]]|-2.06|0.31|
|[[:human_genes:D:DNAJC5G|DNAJC5G]]|-2.05|0.31|
|[[:human_genes:E:EEF2|EEF2]]|-2.04|0.72|
|[[:human_genes:F:FBXW7|FBXW7]]|-2.04|0.31|
|[[:human_genes:L:LEO1|LEO1]]|-2.03|0.36|
|[[:human_genes:F:FTSJ1|FTSJ1]]|-2.03|0.31|
|[[:human_genes:S:SOD1|SOD1]]|-2.01|0.57|
|[[:human_genes:A:ARMS2|ARMS2]]|-2.01|0.32|
|[[:human_genes:E:EIF2A|EIF2A]]|-1.97|0.36|
|[[:human_genes:F:FAM219A|FAM219A]]|-1.95|0.36|
|[[:human_genes:S:SCN10A|SCN10A]]|-1.95|0.36|
|[[:human_genes:D:DDTL|DDTL]]|1.98|0.48|
|[[:human_genes:C:C4orf33|C4orf33]]|1.98|0.48|
|[[:human_genes:A:AUP1|AUP1]]|2.00|0.58|
|[[:human_genes:C:C21orf91|C21orf91]]|2.02|0.49|
|[[:human_genes:A:ARCN1|ARCN1]]|2.02|0.58|
|[[:human_genes:S:STX8|STX8]]|2.04|0.58|
|[[:human_genes:A:ATXN2|ATXN2]]|2.05|0.48|
|[[:human_genes:P:PLK2|PLK2]]|2.06|0.47|
|[[:human_genes:C:CCDC58|CCDC58]]|2.06|0.48|
|[[:human_genes:P:PLSCR2|PLSCR2]]|2.07|0.47|
|[[:human_genes:F:FAM13A|FAM13A]]|2.10|0.47|
|[[:human_genes:P:PAN2|PAN2]]|2.10|0.47|
|[[:human_genes:G:GLTSCR2|GLTSCR2]]|2.11|0.58|
|[[:human_genes:R:RPS2|RPS2]]|2.12|0.47|
|[[:human_genes:R:RPS14|RPS14]]|2.15|0.58|
|[[:human_genes:N:NFATC3|NFATC3]]|2.16|0.48|
|[[:human_genes:S:SNRNP70|SNRNP70]]|2.17|0.58|
|[[:human_genes:F:FAM231B|FAM231B]]|2.21|0.47|
|[[:human_genes:M:MARVELD1|MARVELD1]]|2.24|0.69|
|[[:human_genes:R:RBM39|RBM39]]|2.25|0.67|
|[[:human_genes:T:TSPY8|TSPY8]]|2.26|0.69|
|[[:human_genes:O:OR4A16|OR4A16]]|2.30|0.47|
|[[:human_genes:U:UGGT1|UGGT1]]|2.35|0.47|
|[[:human_genes:L:LLGL1|LLGL1]]|2.39|0.47|
|[[:human_genes:C:CDC73|CDC73]]|2.41|0.48|
|[[:human_genes:X:XAB2|XAB2]]|2.43|0.69|
|[[:human_genes:C:CKAP5|CKAP5]]|2.44|0.58|
|[[:human_genes:C:COPB1|COPB1]]|2.57|0.48|
|[[:human_genes:U:UTP6|UTP6]]|2.82|0.47|
|[[:human_genes:D:DNAJC30|DNAJC30]]|3.04|0.04|
No correlation data above threshold. (correlation > 0.05)
^GO Term^Fold Change^Genes^
|regulation of cholesterol biosynthetic process|115.07|MBTPS2,MBTPS1,SOD1|
|regulation of sterol biosynthetic process|115.07|MBTPS2,MBTPS1,SOD1|
|ER-nucleus signaling pathway|73.97|MBTPS2,MBTPS1,EIF2A|
No GO term hits below threshold. (FDR <0.05)