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Ask your administrator if you think this is wrong. ====== Campthothecin 0.001μM R06 exp270 ====== ==== Mechanism of Action ==== Inhibits topoisomerase I, stabilizes TopoI-DNA complex, causes DNA strand breaks * **<color #00a2e8>Class / Subclass 1:</color>** DNA Damage, Repair and Replication / Clastogen ==== Technical Notes ==== <accordion collapsed='true'> <panel title='Compound References' collapsed='true'> * **<color #00a2e8>PubChem Name:</color>** %%Camptothecin%% * **<color #00a2e8>Synonyms:</color>** Camptothecin; (S)-(+)-Camptothecin; CPT * **<color #00a2e8>CAS #:</color>** 7689-03-4 * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/24360|24360]] * **<color #00a2e8>IUPAC:</color>** %%(19S)-19-ethyl-19-hydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione%% * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C20H16N2O4/c1-2-20(25)14-8-16-17-12(7-11-5-3-4-6-15(11)21-17)9-22(16)18(23)13(14)10-26-19(20)24/h3-8,25H,2,9-10H2,1H3/t20-/m0/s1 * **<color #00a2e8>INCHI Key:</color>** VSJKWCGYPAHWDS-FQEVSTJZSA-N * **<color #00a2e8>Molecular Weight:</color>** 348.4 * **<color #00a2e8>Canonical SMILES:</color>** CCC1(C2=C(COC1=O)C(=O)N3CC4=CC5=CC=CC=C5N=C4C3=C2)O * **<color #00a2e8>Isomeric SMILES:</color>** CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=CC5=CC=CC=C5N=C4C3=C2)O * **<color #00a2e8>Molecular Formula:</color>** C20H16N2O4 {{:chemogenomics:structures:chem-0162.svg?nolink}} </panel> <panel title='Compound Supplier' collapsed='true'> * **<color #00a2e8>Supplier Name:</color>** Sigma-Aldrich * **<color #00a2e8>Catalog #:</color>** C9911 * **<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 C20H16N2O4 349.11828; found 349.11567 </panel> <panel title='Dose Response Curve' collapsed='true'> * **<color #00a2e8>Platform ID:</color>** Camptothecin * **<color #00a2e8>Min:</color>** 25.8061; **<color #00a2e8>Max:</color>** 99.6985 {{:chemogenomics:dose_response:dr_315.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |N/A | | IC30 |0.0006 | | IC40 |N/A | | IC50 |0.0010 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ </panel> </accordion> ==== Screen Summary ==== * **<color #00a2e8>Round</color>**: 06 * **<color #00a2e8>Dose</color>**: 1nM * **<color #00a2e8>Days of incubation</color>**: 8 * **<color #00a2e8>Doublings</color>**: 5.8 * **<color #00a2e8>Numbers of reads</color>**: 8689434 ==== 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^ |7/0|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Campthothecin_0.001uM_Round-6_exp270.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='Campthothecin 0.001μM R06 exp270'> {{:chemogenomics:cranks_plots:exp270.png?nolink}} </modal> <modal id="modal_hits" size="sm" title="Top 30 S/R Genes"> ^Gene^CRANKS Score^FDR^ |[[:human_genes:M:MCM9|MCM9]]|-3.84|<0.01| |[[:human_genes:M:MCM8|MCM8]]|-3.30|<0.01| |[[:human_genes:S:STRA13|STRA13]]|-3.29|<0.01| |[[:human_genes:A:ATM|ATM]]|-3.09|<0.01| |[[:human_genes:S:SWI5|SWI5]]|-2.72|0.04| |[[:human_genes:S:SWSAP1|SWSAP1]]|-2.70|0.02| |[[:human_genes:N:NBN|NBN]]|-2.65|0.03| |[[:human_genes:A:ANKRD32|ANKRD32]]|-2.48|0.18| |[[:human_genes:P:PARP1|PARP1]]|-2.44|0.07| |[[:human_genes:K:KPNA4|KPNA4]]|-2.39|0.08| |[[:human_genes:U:UIMC1|UIMC1]]|-2.35|0.27| |[[:human_genes:A:APITD1-CORT|APITD1-CORT]]|-2.34|0.10| |[[:human_genes:R:RNF8|RNF8]]|-2.31|0.10| |[[:human_genes:C:CDIPT|CDIPT]]|-2.28|0.62| |[[:human_genes:R:RNASEH2A|RNASEH2A]]|-2.26|0.30| |[[:human_genes:M:MDM2|MDM2]]|-2.25|0.44| |[[:human_genes:S:SAFB|SAFB]]|-2.22|0.17| |[[:human_genes:P:PPP1R15A|PPP1R15A]]|-2.19|0.27| |[[:human_genes:A:ANAPC15|ANAPC15]]|-2.16|0.28| |[[:human_genes:C:C19orf40|C19orf40]]|-2.14|0.22| |[[:human_genes:T:TCF4|TCF4]]|-2.08|0.27| |[[:human_genes:E:ERCC2|ERCC2]]|-2.08|0.49| |[[:human_genes:K:KRT222|KRT222]]|-2.07|0.27| |[[:human_genes:M:METTL14|METTL14]]|-2.06|0.44| |[[:human_genes:C:CHGB|CHGB]]|-2.05|0.33| |[[:human_genes:U:UBE2J1|UBE2J1]]|-2.05|0.28| |[[:human_genes:C:C1orf112|C1orf112]]|-2.04|0.33| |[[:human_genes:E:EIF1|EIF1]]|-2.03|0.44| |[[:human_genes:S:SPIDR|SPIDR]]|-2.02|0.29| |[[:human_genes:D:DNAJB9|DNAJB9]]|-1.99|0.30| |[[:human_genes:N:NOL12|NOL12]]|1.95|0.65| |[[:human_genes:N:NPIPA5|NPIPA5]]|1.96|0.70| |[[:human_genes:N:NCSTN|NCSTN]]|1.96|0.57| |[[:human_genes:T:TMEM134|TMEM134]]|1.97|0.57| |[[:human_genes:S:SMG5|SMG5]]|1.98|0.75| |[[:human_genes:S:SRPK3|SRPK3]]|1.99|0.57| |[[:human_genes:M:MED14|MED14]]|1.99|0.57| |[[:human_genes:P:PPP1R8|PPP1R8]]|2.00|0.57| |[[:human_genes:C:COPB1|COPB1]]|2.01|0.70| |[[:human_genes:D:DNM2|DNM2]]|2.03|0.78| |[[:human_genes:C:CPEB2|CPEB2]]|2.04|0.70| |[[:human_genes:P:POLDIP2|POLDIP2]]|2.05|0.57| |[[:human_genes:N:NDUFB7|NDUFB7]]|2.06|0.58| |[[:human_genes:L:LYG2|LYG2]]|2.07|0.57| |[[:human_genes:R:RPL11|RPL11]]|2.09|0.78| |[[:human_genes:M:MT1X|MT1X]]|2.09|0.57| |[[:human_genes:C:C19orf59|C19orf59]]|2.11|0.57| |[[:human_genes:H:HMHA1|HMHA1]]|2.11|0.57| |[[:human_genes:T:TOP1MT|TOP1MT]]|2.13|0.57| |[[:human_genes:E:EIF4A3|EIF4A3]]|2.15|0.64| |[[:human_genes:R:RPS5|RPS5]]|2.18|0.57| |[[:human_genes:K:KDR|KDR]]|2.28|0.57| |[[:human_genes:P:PSMC3|PSMC3]]|2.28|0.65| |[[:human_genes:S:SLC2A1|SLC2A1]]|2.28|0.57| |[[:human_genes:S:SLC10A7|SLC10A7]]|2.31|0.30| |[[:human_genes:T:TCN2|TCN2]]|2.35|0.42| |[[:human_genes:C:CERKL|CERKL]]|2.39|0.26| |[[:human_genes:P:PIK3CD|PIK3CD]]|2.43|0.26| |[[:human_genes:F:FAM72C|FAM72C]]|2.50|0.70| |[[:human_genes:S:SOWAHA|SOWAHA]]|2.56|0.26| </modal> <modal id="modal_screen_similarity" size="lg" title="Correlated Screens"> ^Screen^Correlation^Plot^ |[[:results:exp520|Rucaparib 6.5μM R08 exp520]]|0.081|<button type="primary" size="small" modal="1">View</button>| |[[:results:exp512|Olaparib 4μM R08 exp512]]|0.056|<button type="primary" size="small" modal="2">View</button>| |[[:results:exp299|Talazoparib 0.006μM R06 exp299]]|0.052|<button type="primary" size="small" modal="3">View</button>| </modal> <modal id="1" size="lg" title="Campthothecin 0.001μM R06 exp270 vs Rucaparib 6.5μM R08 exp520"> {{:chemogenomics:comparison_plots:exp270_vs_exp520.png?nolink |}} </modal> <modal id="2" size="lg" title="Campthothecin 0.001μM R06 exp270 vs Olaparib 4μM R08 exp512"> {{:chemogenomics:comparison_plots:exp270_vs_exp512.png?nolink |}} </modal> <modal id="3" size="lg" title="Campthothecin 0.001μM R06 exp270 vs Talazoparib 0.006μM R06 exp299"> {{:chemogenomics:comparison_plots:exp270_vs_exp299.png?nolink |}} </modal> <modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms"> ^GO Term^Fold Change^Genes^ |interstrand cross-link repair|74.99|MCM9,MCM8,CENPX,RNF8| |DNA-templated DNA replication maintenance of fidelity|60.13|MCM9,MCM8,CENPX,NBN,PARP1| |recombinational repair|42.85|MCM9,MCM8,ATM,SWI5,SWSAP1,NBN,SLF1,SPIDR| |site of double-strand break|39.34|NBN,SLF1,PARP1,UIMC1,RNF8| |double-strand break repair via homologous recombination|38.46|MCM9,MCM8,ATM,SWI5,NBN,SLF1,SPIDR| |double-strand break repair|34.88|MCM9,MCM8,ATM,SWI5,SWSAP1,NBN,SLF1,PARP1,UIMC1,RNF8,SPIDR| |response to ionizing radiation|33.55|ATM,SWI5,PARP1,UIMC1,RNF8,MDM2,SPIDR| |site of DNA damage|29.51|NBN,SLF1,PARP1,UIMC1,RNF8| |DNA recombination|28.33|MCM9,MCM8,CENPX,ATM,SWI5,SWSAP1,NBN,SLF1,RNF8,SPIDR| |positive regulation of DNA repair|26.12|SLF1,PARP1,UIMC1,RNF8,SPIDR| |DNA-templated DNA replication|24.33|MCM9,MCM8,CENPX,NBN,PARP1| |signal transduction in response to DNA damage|22.93|ATM,NBN,UIMC1,RNF8,MDM2| |DNA replication|19.71|MCM9,MCM8,CENPX,NBN,PARP1,RNASEH2A| |DNA repair|18.95|MCM9,MCM8,CENPX,ATM,SWI5,SWSAP1,NBN,SLF1,PARP1,UIMC1,RNF8,RNASEH2A,ERCC2,SPIDR| |positive regulation of DNA metabolic process|17.77|ATM,NBN,SLF1,PARP1,UIMC1,RNF8,ERCC2,SPIDR| |DNA damage response|14.26|MCM9,MCM8,CENPX,ATM,SWI5,SWSAP1,NBN,SLF1,PARP1,UIMC1,RNF8,RNASEH2A,MDM2,PPP1R15A,ERCC2,SPIDR| |DNA metabolic process|12.46|MCM9,MCM8,CENPX,ATM,SWI5,SWSAP1,NBN,SLF1,PARP1,UIMC1,RNF8,RNASEH2A,ERCC2,SPIDR| |response to radiation|12.44|ATM,SWI5,PARP1,UIMC1,RNF8,MDM2,ERCC2,SPIDR| |regulation of DNA metabolic process|10.06|ATM,NBN,SLF1,PARP1,UIMC1,RNF8,ERCC2,SPIDR| </modal> <modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">No GO term hits below threshold. (FDR <0.05)</modal> Last modified: 2026/01/15 21:36by 127.0.0.1