====== Erlotinib 10μM R05 exp216 ======
==== Mechanism of Action ====
Inhibits EGFR, also cyclin G-associated kinase (GAK)
* **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%Erlotinib%%
* **Synonyms:** CP-358774; NSC 718781; OSI-774
* **CAS #:** 183321-74-6
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/176870|176870]]
* **IUPAC:** %%N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine%%
* **INCHI Name:** InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25)
* **INCHI Key:** AAKJLRGGTJKAMG-UHFFFAOYSA-N
* **Molecular Weight:** 393.4
* **Canonical SMILES:** COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC
* **Isomeric SMILES:** N/A
* **Molecular Formula:** C22H23N3O4
{{:chemogenomics:structures:chem-0114.svg?nolink}}
* **Supplier Name:** Cayman Chemical
* **Catalog #:** 10483
* **Lot #:** N/A
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C22H23N3O4 394.17613; found 394.17708
* **Platform ID:** Erlotinib
* **Min:** -14.1940; **Max:** 21.2326
{{:chemogenomics:dose_response:dr_221.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**: 10µM
* **Days of incubation**: 8
* **Doublings**: 4.1
* **Numbers of reads**: 19100357
==== 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^
|18/31|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Erlotinib_10uM_Round-5_exp216.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp216.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:R:RSRC2|RSRC2]]|-3.58|0.02|
|[[:human_genes:I:ITPA|ITPA]]|-3.04|<0.01|
|[[:human_genes:R:RHOA|RHOA]]|-3.01|<0.01|
|[[:human_genes:C:CMIP|CMIP]]|-2.88|0.02|
|[[:human_genes:P:PRR12|PRR12]]|-2.82|0.02|
|[[:human_genes:A:ATP6V0A2|ATP6V0A2]]|-2.81|0.04|
|[[:human_genes:P:PTEN|PTEN]]|-2.75|0.02|
|[[:human_genes:E:EIF2A|EIF2A]]|-2.70|0.02|
|[[:human_genes:T:TCF4|TCF4]]|-2.69|0.02|
|[[:human_genes:B:BACH2|BACH2]]|-2.64|0.04|
|[[:human_genes:T:TRIB3|TRIB3]]|-2.64|0.04|
|[[:human_genes:U:UBE2N|UBE2N]]|-2.62|0.04|
|[[:human_genes:P:PPHLN1|PPHLN1]]|-2.60|0.04|
|[[:human_genes:D:DDX6|DDX6]]|-2.58|0.06|
|[[:human_genes:D:DOT1L|DOT1L]]|-2.58|0.04|
|[[:human_genes:D:DRG2|DRG2]]|-2.49|0.04|
|[[:human_genes:U:UMPS|UMPS]]|-2.48|0.50|
|[[:human_genes:C:CCDC173|CCDC173]]|-2.44|0.06|
|[[:human_genes:C:CTU1|CTU1]]|-2.40|0.04|
|[[:human_genes:C:CNOT8|CNOT8]]|-2.38|0.05|
|[[:human_genes:C:CNOT2|CNOT2]]|-2.37|0.05|
|[[:human_genes:T:TRMT1|TRMT1]]|-2.32|0.06|
|[[:human_genes:R:RER1|RER1]]|-2.27|0.06|
|[[:human_genes:I:INTS12|INTS12]]|-2.27|0.06|
|[[:human_genes:P:PRKAR1A|PRKAR1A]]|-2.26|0.07|
|[[:human_genes:C:CCDC101|CCDC101]]|-2.25|0.11|
|[[:human_genes:M:MAPK14|MAPK14]]|-2.23|0.08|
|[[:human_genes:C:CCM2|CCM2]]|-2.22|0.08|
|[[:human_genes:F:FAM208A|FAM208A]]|-2.21|0.08|
|[[:human_genes:M:MOCS3|MOCS3]]|-2.20|0.12|
|[[:human_genes:F:FBXW11|FBXW11]]|2.39|0.15|
|[[:human_genes:P:PFKP|PFKP]]|2.42|0.05|
|[[:human_genes:R:RPS12|RPS12]]|2.43|0.08|
|[[:human_genes:N:NCLN|NCLN]]|2.45|0.04|
|[[:human_genes:E:EIF2B1|EIF2B1]]|2.49|0.02|
|[[:human_genes:H:HSPE1|HSPE1]]|2.64|0.38|
|[[:human_genes:P:PLN|PLN]]|2.64|0.24|
|[[:human_genes:P:PTPMT1|PTPMT1]]|2.68|0.03|
|[[:human_genes:A:ANP32A|ANP32A]]|2.70|0.01|
|[[:human_genes:N:NFATC3|NFATC3]]|2.70|0.01|
|[[:human_genes:M:MBTPS2|MBTPS2]]|2.74|<0.01|
|[[:human_genes:E:EIF3A|EIF3A]]|2.80|<0.01|
|[[:human_genes:T:TSC1|TSC1]]|2.87|<0.01|
|[[:human_genes:R:RPS10|RPS10]]|2.93|<0.01|
|[[:human_genes:N:NPRL3|NPRL3]]|3.01|<0.01|
|[[:human_genes:E:EIF4B|EIF4B]]|3.05|<0.01|
|[[:human_genes:N:NPRL2|NPRL2]]|3.13|<0.01|
|[[:human_genes:D:DDX3X|DDX3X]]|3.21|<0.01|
|[[:human_genes:A:ARID4B|ARID4B]]|3.21|<0.01|
|[[:human_genes:C:CEBPG|CEBPG]]|3.50|<0.01|
|[[:human_genes:D:DEPDC5|DEPDC5]]|3.56|<0.01|
|[[:human_genes:N:NANS|NANS]]|3.64|<0.01|
|[[:human_genes:E:EIF3G|EIF3G]]|3.76|<0.01|
|[[:human_genes:E:EIF4A1|EIF4A1]]|3.93|<0.01|
|[[:human_genes:C:CMAS|CMAS]]|4.25|<0.01|
|[[:human_genes:T:TSC2|TSC2]]|4.47|<0.01|
|[[:human_genes:S:SERBP1|SERBP1]]|4.99|<0.01|
|[[:human_genes:A:ATF4|ATF4]]|5.36|<0.01|
|[[:human_genes:G:GCN1L1|GCN1L1]]|7.43|<0.01|
|[[:human_genes:E:EIF2AK4|EIF2AK4]]|8.48|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp189|Temozolomide 200μM R04 exp189]]|0.098||
|[[:results:exp242|Radicicol 0.16μM R05 exp242]]|0.079||
|[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.074||
|[[:results:exp210|LB-100 2μM R05 exp210]]|0.071||
|[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.067||
|[[:results:exp502|Milciclib 2μM R08 exp502]]|0.063||
|[[:results:exp234|Ethanol 0.01 R05 exp234]]|0.062||
|[[:results:exp485|GSK626616 14μM R08 exp485]]|0.062||
|[[:results:exp524|Staurosporine 0.02μM R08 exp524]]|0.061||
|[[:results:exp504|MK2206 4μM R08 exp504]]|0.057||
|[[:results:exp75|MK-1775 0.32μM R02 exp75]]|0.056||
|[[:results:exp30|Rapamycin 10μM R00 exp30]]|0.055||
|[[:results:exp82|Torin1 0.08μM R02 exp82]]|0.054||
|[[:results:exp299|Talazoparib 0.006μM R06 exp299]]|0.053||
|[[:results:exp535|Trimetrexate 0.03μM R08 exp535]]|0.053||
|[[:results:exp497|Lead acetate 2000μM R08 exp497]]|0.051||
|[[:results:exp72|LB-100 4.1μM R02 exp72]]|0.051||
|[[:results:exp330|5-Azacytidine 2μM R07 exp330]]|0.075||
|[[:results:exp233|EPZ-5676 30μM R05 exp233]]|0.066||
|[[:results:exp352|Dexamethasone 0.006 to 0.015μM on day4 R07 exp352]]|0.06||
|[[:results:exp229|Dimethyloxaloylglycine 100μM R05 exp229]]|0.053||
{{:chemogenomics:comparison_plots:exp189_vs_exp216.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp242.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp488.png?nolink |}}
{{:chemogenomics:comparison_plots:exp210_vs_exp216.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp489.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp502.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp234.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp485.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp524.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp75.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp30.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp82.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp299.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp535.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp497.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp72.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp330.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp233.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp352.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp229.png?nolink |}}
^GO Term^Fold Change^Genes^
|protein localization to heterochromatin|613.70|PPHLN1,TASOR|
^GO Term^Fold Change^Genes^
|cellular response to amino acid starvation|70.51|EIF2AK4,GCN1,ATF4,DEPDC5,NPRL2,NPRL3|
|negative regulation of TORC1 signaling|67.36|TSC2,DEPDC5,NPRL2,NPRL3,TSC1|
|response to amino acid starvation|66.28|EIF2AK4,GCN1,ATF4,DEPDC5,NPRL2,NPRL3|
|translation initiation factor activity|58.76|EIF4A1,EIF3G,EIF4B,EIF3A,EIF2B1|
|translational initiation|52.60|EIF4A1,EIF3G,DDX3X,EIF4B,EIF3A,EIF2B1|
|negative regulation of TOR signaling|41.84|TSC2,DEPDC5,NPRL2,NPRL3,TSC1|
|translation factor activity, RNA binding|41.43|GCN1,EIF4A1,EIF3G,EIF4B,EIF3A,EIF2B1|
|translation regulator activity, nucleic acid binding|31.87|GCN1,EIF4A1,EIF3G,EIF4B,EIF3A,EIF2B1|
|translation regulator activity|29.29|GCN1,SERBP1,EIF4A1,EIF3G,EIF4B,EIF3A,EIF2B1|
|cellular response to starvation|26.15|EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1|
|response to starvation|21.24|EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1|
|cellular response to nutrient levels|19.13|EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1|
|cellular response to extracellular stimulus|16.99|EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1|
|translation|13.96|GCN1,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12|
|cellular response to external stimulus|13.60|EIF2AK4,GCN1,ATF4,TSC2,DEPDC5,NPRL2,NPRL3,TSC1|
|peptide biosynthetic process|13.05|GCN1,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12|
|peptide metabolic process|10.51|GCN1,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12|
|amide biosynthetic process|9.90|GCN1,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12|
|amide metabolic process|8.04|GCN1,ATF4,CMAS,EIF4A1,EIF3G,DDX3X,EIF4B,RPS10,EIF3A,EIF2B1,RPS12|