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Ask your administrator if you think this is wrong. ====== Erlotinib 10μM R05 exp216 ====== ==== Mechanism of Action ==== Inhibits EGFR, also cyclin G-associated kinase (GAK) * **<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>** %%Erlotinib%% * **<color #00a2e8>Synonyms:</color>** CP-358774; NSC 718781; OSI-774 * **<color #00a2e8>CAS #:</color>** 183321-74-6 * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/176870|176870]] * **<color #00a2e8>IUPAC:</color>** %%N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine%% * **<color #00a2e8>INCHI Name:</color>** 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) * **<color #00a2e8>INCHI Key:</color>** AAKJLRGGTJKAMG-UHFFFAOYSA-N * **<color #00a2e8>Molecular Weight:</color>** 393.4 * **<color #00a2e8>Canonical SMILES:</color>** COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC * **<color #00a2e8>Isomeric SMILES:</color>** N/A * **<color #00a2e8>Molecular Formula:</color>** C22H23N3O4 {{:chemogenomics:structures:chem-0114.svg?nolink}} </panel> <panel title='Compound Supplier' collapsed='true'> * **<color #00a2e8>Supplier Name:</color>** Cayman Chemical * **<color #00a2e8>Catalog #:</color>** 10483 * **<color #00a2e8>Lot #:</color>** N/A </panel> <panel title='Compound Characterization' collapsed='true'> * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+H)+ Calcd for C22H23N3O4 394.17613; found 394.17708 </panel> <panel title='Dose Response Curve' collapsed='true'> * **<color #00a2e8>Platform ID:</color>** Erlotinib * **<color #00a2e8>Min:</color>** -14.1940; **<color #00a2e8>Max:</color>** 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 | \\ </panel> </accordion> ==== Screen Summary ==== * **<color #00a2e8>Round</color>**: 05 * **<color #00a2e8>Dose</color>**: 10µM * **<color #00a2e8>Days of incubation</color>**: 8 * **<color #00a2e8>Doublings</color>**: 4.1 * **<color #00a2e8>Numbers of reads</color>**: 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|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Erlotinib_10uM_Round-5_exp216.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='Erlotinib 10μM R05 exp216'> {{:chemogenomics:cranks_plots:exp216.png?nolink}} </modal> <modal id="modal_hits" size="sm" title="Top 30 S/R Genes"> ^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| </modal> <modal id="modal_screen_similarity" size="lg" title="Correlated Screens"> ^Screen^Correlation^Plot^ |[[:results:exp189|Temozolomide 200μM R04 exp189]]|0.098|<button type="primary" size="small" modal="1">View</button>| |[[:results:exp242|Radicicol 0.16μM R05 exp242]]|0.079|<button type="primary" size="small" modal="2">View</button>| |[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.074|<button type="primary" size="small" modal="3">View</button>| |[[:results:exp210|LB-100 2μM R05 exp210]]|0.071|<button type="primary" size="small" modal="4">View</button>| |[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.067|<button type="primary" size="small" modal="5">View</button>| |[[:results:exp502|Milciclib 2μM R08 exp502]]|0.063|<button type="primary" size="small" modal="6">View</button>| |[[:results:exp234|Ethanol 0.01 R05 exp234]]|0.062|<button type="primary" size="small" modal="7">View</button>| |[[:results:exp485|GSK626616 14μM R08 exp485]]|0.062|<button type="primary" size="small" modal="8">View</button>| |[[:results:exp524|Staurosporine 0.02μM R08 exp524]]|0.061|<button type="primary" size="small" modal="9">View</button>| |[[:results:exp504|MK2206 4μM R08 exp504]]|0.057|<button type="primary" size="small" modal="10">View</button>| |[[:results:exp75|MK-1775 0.32μM R02 exp75]]|0.056|<button type="primary" size="small" modal="11">View</button>| |[[:results:exp30|Rapamycin 10μM R00 exp30]]|0.055|<button type="primary" size="small" modal="12">View</button>| |[[:results:exp82|Torin1 0.08μM R02 exp82]]|0.054|<button type="primary" size="small" modal="13">View</button>| |[[:results:exp299|Talazoparib 0.006μM R06 exp299]]|0.053|<button type="primary" size="small" modal="14">View</button>| |[[:results:exp535|Trimetrexate 0.03μM R08 exp535]]|0.053|<button type="primary" size="small" modal="15">View</button>| |[[:results:exp497|Lead acetate 2000μM R08 exp497]]|0.051|<button type="primary" size="small" modal="16">View</button>| |[[:results:exp72|LB-100 4.1μM R02 exp72]]|0.051|<button type="primary" size="small" modal="17">View</button>| |[[:results:exp330|5-Azacytidine 2μM R07 exp330]]|0.075|<button type="primary" size="small" modal="18">View</button>| |[[:results:exp233|EPZ-5676 30μM R05 exp233]]|0.066|<button type="primary" size="small" modal="19">View</button>| |[[:results:exp352|Dexamethasone 0.006 to 0.015μM on day4 R07 exp352]]|0.06|<button type="primary" size="small" modal="20">View</button>| |[[:results:exp229|Dimethyloxaloylglycine 100μM R05 exp229]]|0.053|<button type="primary" size="small" modal="21">View</button>| </modal> <modal id="1" size="lg" title="Erlotinib 10μM R05 exp216 vs Temozolomide 200μM R04 exp189"> {{:chemogenomics:comparison_plots:exp189_vs_exp216.png?nolink |}} </modal> <modal id="2" size="lg" title="Erlotinib 10μM R05 exp216 vs Radicicol 0.16μM R05 exp242"> {{:chemogenomics:comparison_plots:exp216_vs_exp242.png?nolink |}} </modal> <modal id="3" size="lg" title="Erlotinib 10μM R05 exp216 vs Hippuristanol 0.12μM R08 exp488"> {{:chemogenomics:comparison_plots:exp216_vs_exp488.png?nolink |}} </modal> <modal id="4" size="lg" title="Erlotinib 10μM R05 exp216 vs LB-100 2μM R05 exp210"> {{:chemogenomics:comparison_plots:exp210_vs_exp216.png?nolink |}} </modal> <modal id="5" size="lg" title="Erlotinib 10μM R05 exp216 vs Hippuristanol 0.12μM R08 exp489 no dilution day6"> {{:chemogenomics:comparison_plots:exp216_vs_exp489.png?nolink |}} </modal> <modal id="6" size="lg" title="Erlotinib 10μM R05 exp216 vs Milciclib 2μM R08 exp502"> {{:chemogenomics:comparison_plots:exp216_vs_exp502.png?nolink |}} </modal> <modal id="7" size="lg" title="Erlotinib 10μM R05 exp216 vs Ethanol 0.01 R05 exp234"> {{:chemogenomics:comparison_plots:exp216_vs_exp234.png?nolink |}} </modal> <modal id="8" size="lg" title="Erlotinib 10μM R05 exp216 vs GSK626616 14μM R08 exp485"> {{:chemogenomics:comparison_plots:exp216_vs_exp485.png?nolink |}} </modal> <modal id="9" size="lg" title="Erlotinib 10μM R05 exp216 vs Staurosporine 0.02μM R08 exp524"> {{:chemogenomics:comparison_plots:exp216_vs_exp524.png?nolink |}} </modal> <modal id="10" size="lg" title="Erlotinib 10μM R05 exp216 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp216_vs_exp504.png?nolink |}} </modal> <modal id="11" size="lg" title="Erlotinib 10μM R05 exp216 vs MK-1775 0.32μM R02 exp75"> {{:chemogenomics:comparison_plots:exp216_vs_exp75.png?nolink |}} </modal> <modal id="12" size="lg" title="Erlotinib 10μM R05 exp216 vs Rapamycin 10μM R00 exp30"> {{:chemogenomics:comparison_plots:exp216_vs_exp30.png?nolink |}} </modal> <modal id="13" size="lg" title="Erlotinib 10μM R05 exp216 vs Torin1 0.08μM R02 exp82"> {{:chemogenomics:comparison_plots:exp216_vs_exp82.png?nolink |}} </modal> <modal id="14" size="lg" title="Erlotinib 10μM R05 exp216 vs Talazoparib 0.006μM R06 exp299"> {{:chemogenomics:comparison_plots:exp216_vs_exp299.png?nolink |}} </modal> <modal id="15" size="lg" title="Erlotinib 10μM R05 exp216 vs Trimetrexate 0.03μM R08 exp535"> {{:chemogenomics:comparison_plots:exp216_vs_exp535.png?nolink |}} </modal> <modal id="16" size="lg" title="Erlotinib 10μM R05 exp216 vs Lead acetate 2000μM R08 exp497"> {{:chemogenomics:comparison_plots:exp216_vs_exp497.png?nolink |}} </modal> <modal id="17" size="lg" title="Erlotinib 10μM R05 exp216 vs LB-100 4.1μM R02 exp72"> {{:chemogenomics:comparison_plots:exp216_vs_exp72.png?nolink |}} </modal> <modal id="18" size="lg" title="5-Azacytidine 2μM R07 exp330 vs Erlotinib 10μM R05 exp216"> {{:chemogenomics:comparison_plots:exp216_vs_exp330.png?nolink |}} </modal> <modal id="19" size="lg" title="EPZ-5676 30μM R05 exp233 vs Erlotinib 10μM R05 exp216"> {{:chemogenomics:comparison_plots:exp216_vs_exp233.png?nolink |}} </modal> <modal id="20" size="lg" title="Dexamethasone 0.006 to 0.015μM on day4 R07 exp352 vs Erlotinib 10μM R05 exp216"> {{:chemogenomics:comparison_plots:exp216_vs_exp352.png?nolink |}} </modal> <modal id="21" size="lg" title="Dimethyloxaloylglycine 100μM R05 exp229 vs Erlotinib 10μM R05 exp216"> {{:chemogenomics:comparison_plots:exp216_vs_exp229.png?nolink |}} </modal> <modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms"> ^GO Term^Fold Change^Genes^ |protein localization to heterochromatin|613.70|PPHLN1,TASOR| </modal> <modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms"> ^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| </modal> Last modified: 2026/01/15 21:36by 127.0.0.1