====== Combretastatin A4 0.002 to 0.003μM day4 R04 exp179 ======
==== Mechanism of Action ====
Inhibits microtubule polymerization
* **Class / Subclass 1:** Cell Cycle / Microtubule Poison
* **Class / Subclass 2:** Organelle Function / Cytoskeletal Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%Combretastatin A4%%
* **Synonyms:** CRC 87-09
* **CAS #:** 117048-59-6
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/5351344|5351344]]
* **IUPAC:** %%2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol%%
* **INCHI Name:** InChI=1S/C18H20O5/c1-20-15-8-7-12(9-14(15)19)5-6-13-10-16(21-2)18(23-4)17(11-13)22-3/h5-11,19H,1-4H3/b6-5-
* **INCHI Key:** HVXBOLULGPECHP-WAYWQWQTSA-N
* **Molecular Weight:** 316.3
* **Canonical SMILES:** COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)O
* **Isomeric SMILES:** COC1=C(C=C(C=C1)/C=C\\C2=CC(=C(C(=C2)OC)OC)OC)O
* **Molecular Formula:** C18H20O5
{{:chemogenomics:structures:chem-0112.svg?nolink}}
* **Supplier Name:** Abcam
* **Catalog #:** AB120925
* **Lot #:** N/A
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C18H20O5 317.13835; found 317.13863
* **Platform ID:** Combretastatin_A4
* **Min:** -2.6499; **Max:** 88.5172
{{:chemogenomics:dose_response:dr_199.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |0.0017 |
| IC30 |0.0019 |
| IC40 |0.0022 |
| IC50 |0.0024 |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 04
* **Dose**: 0.002-0.003µM
* **Days of incubation**: 8
* **Doublings**: 5.7
* **Numbers of reads**: 23260964
==== 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^
|23/5|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Combretastatin_A4_0.002-0.003day4uM_Round-4_exp179.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp179.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:S:STMN1|STMN1]]|-4.39|<0.01|
|[[:human_genes:Q:QRICH1|QRICH1]]|-3.84|<0.01|
|[[:human_genes:B:BRD1|BRD1]]|-3.61|<0.01|
|[[:human_genes:T:TACC3|TACC3]]|-3.48|<0.01|
|[[:human_genes:D:DLGAP5|DLGAP5]]|-3.24|<0.01|
|[[:human_genes:G:GAK|GAK]]|-3.17|<0.01|
|[[:human_genes:K:KIF15|KIF15]]|-3.16|<0.01|
|[[:human_genes:U:URI1|URI1]]|-3.13|<0.01|
|[[:human_genes:M:MSI2|MSI2]]|-2.97|<0.01|
|[[:human_genes:T:TCF4|TCF4]]|-2.90|<0.01|
|[[:human_genes:S:SEPHS1|SEPHS1]]|-2.89|<0.01|
|[[:human_genes:M:MAPRE1|MAPRE1]]|-2.75|0.02|
|[[:human_genes:L:LRRC8A|LRRC8A]]|-2.74|<0.01|
|[[:human_genes:A:ASPM|ASPM]]|-2.71|0.02|
|[[:human_genes:R:RSRC2|RSRC2]]|-2.63|0.09|
|[[:human_genes:I:IPO9|IPO9]]|-2.62|0.05|
|[[:human_genes:K:KNTC1|KNTC1]]|-2.61|0.01|
|[[:human_genes:V:VBP1|VBP1]]|-2.61|0.01|
|[[:human_genes:N:NEMF|NEMF]]|-2.61|0.03|
|[[:human_genes:C:CCDC153|CCDC153]]|-2.59|0.06|
|[[:human_genes:G:GTSE1|GTSE1]]|-2.53|0.04|
|[[:human_genes:K:KLF16|KLF16]]|-2.49|0.04|
|[[:human_genes:N:NPRL3|NPRL3]]|-2.48|0.08|
|[[:human_genes:F:FBXW7|FBXW7]]|-2.45|0.03|
|[[:human_genes:D:DPH1|DPH1]]|-2.40|0.04|
|[[:human_genes:C:CALM2|CALM2]]|-2.38|0.07|
|[[:human_genes:B:BICD2|BICD2]]|-2.35|0.07|
|[[:human_genes:S:SKA1|SKA1]]|-2.33|0.05|
|[[:human_genes:A:ANP32A|ANP32A]]|-2.32|0.08|
|[[:human_genes:P:PRKAG1|PRKAG1]]|-2.24|0.11|
|[[:human_genes:A:ATP6AP1|ATP6AP1]]|1.99|0.51|
|[[:human_genes:P:PDCD10|PDCD10]]|2.01|0.27|
|[[:human_genes:A:ADIPOR1|ADIPOR1]]|2.02|0.27|
|[[:human_genes:V:VCP|VCP]]|2.03|0.49|
|[[:human_genes:P:PDE8A|PDE8A]]|2.06|0.41|
|[[:human_genes:A:AGPAT9|AGPAT9]]|2.08|0.24|
|[[:human_genes:G:GRPEL1|GRPEL1]]|2.09|0.47|
|[[:human_genes:P:PDE7A|PDE7A]]|2.10|0.23|
|[[:human_genes:P:PCDH11X|PCDH11X]]|2.11|0.23|
|[[:human_genes:C:CEP290|CEP290]]|2.12|0.23|
|[[:human_genes:N:NUDCD2|NUDCD2]]|2.14|0.22|
|[[:human_genes:P:PRSS58|PRSS58]]|2.15|0.22|
|[[:human_genes:D:DCUN1D1|DCUN1D1]]|2.16|0.22|
|[[:human_genes:M:MCL1|MCL1]]|2.17|0.25|
|[[:human_genes:U:UBALD2|UBALD2]]|2.17|0.25|
|[[:human_genes:N:NR1D2|NR1D2]]|2.24|0.17|
|[[:human_genes:D:DNAJA1|DNAJA1]]|2.30|0.26|
|[[:human_genes:R:RUFY3|RUFY3]]|2.38|0.09|
|[[:human_genes:E:EIF2S1|EIF2S1]]|2.43|0.57|
|[[:human_genes:C:C5orf22|C5orf22]]|2.45|0.07|
|[[:human_genes:S:SLC25A51|SLC25A51]]|2.47|0.07|
|[[:human_genes:C:C14orf182|C14orf182]]|2.52|0.09|
|[[:human_genes:T:TP53|TP53]]|2.52|0.09|
|[[:human_genes:Z:ZC3H18|ZC3H18]]|2.64|0.22|
|[[:human_genes:P:PPP3R1|PPP3R1]]|2.76|0.02|
|[[:human_genes:A:ATP1B3|ATP1B3]]|2.79|0.02|
|[[:human_genes:A:ATAT1|ATAT1]]|2.99|<0.01|
|[[:human_genes:P:PSMD7|PSMD7]]|3.05|0.24|
|[[:human_genes:T:TMEM161B|TMEM161B]]|3.80|<0.01|
|[[:human_genes:A:ATP1A1|ATP1A1]]|4.77|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp228|Demecolcine 0.03μM R05 exp228]]|0.182||
|[[:results:exp243|S-trityl-L-cysteine 0.5μM R05 exp243]]|0.121||
|[[:results:exp190|Vincristine 0.0005μM R04 exp190]]|0.12||
|[[:results:exp184|Ixabepilone 0.004 to 0.005μM on day4 R04 exp184]]|0.11||
|[[:results:exp217|Mdivi-1 15μM R05 exp217]]|0.097||
|[[:results:exp59|UMK57 1μM R01 exp59]]|0.096||
|[[:results:exp517|Quercetin 20μM R08 exp517]]|0.09||
|[[:results:exp107|UMK57 0.6μM R03 exp107]]|0.085||
|[[:results:exp60|Vinblastine 0.002μM R01 exp60]]|0.077||
|[[:results:exp103|Taxol 0.004μM R03 exp103]]|0.076||
|[[:results:exp46|HMS-I1 1μM R01 exp46]]|0.069||
|[[:results:exp526|Sulforaphane 9μM R08 exp526 no dilution day6]]|0.064||
|[[:results:exp525|Sulforaphane 9μM R08 exp525]]|0.062||
|[[:results:exp231|Epothilone-B 0.0015μM R05 exp231]]|0.061||
|[[:results:exp500|LY2090314 0.003μM R08 exp500 no dilution day6]]|0.056||
|[[:results:exp125|GSK461364A 0.005μM R03 exp125]]|0.056||
|[[:results:exp106|UM131593 0.2μM R03 exp106]]|0.055||
|[[:results:exp356|Docosahexaenoic-acid 50μM R07 exp356]]|0.055||
|[[:results:exp32|Rifampicin 10μM R00 exp32]]|0.051||
|[[:results:exp485|GSK626616 14μM R08 exp485]]|0.051||
|[[:results:exp360|Genistein 15μM R07 exp360]]|0.051||
|[[:results:exp215|Colchicine 0.009μM R05 exp215]]|0.136||
|[[:results:exp460|BML-284 0.09μM R08 exp460]]|0.121||
|[[:results:exp312|2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312]]|0.108||
|[[:results:exp311|2-Methoxyestradiol 0.55 to 0.75μM on day4 R07 exp311]]|0.097||
|[[:results:exp310|2-Methoxyestradiol 0.55μM R07 exp310]]|0.087||
|[[:results:exp162|BI-D1870 2μM R04 exp162]]|0.059||
|[[:results:exp223|Cabazitaxel 0.001μM R05 exp223]]|0.058||
|[[:results:exp97|BI-6727 0.0125μM R03 exp97]]|0.056||
{{:chemogenomics:comparison_plots:exp179_vs_exp228.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp243.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp190.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp184.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp217.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp59.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp517.png?nolink |}}
{{:chemogenomics:comparison_plots:exp107_vs_exp179.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp60.png?nolink |}}
{{:chemogenomics:comparison_plots:exp103_vs_exp179.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp46.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp526.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp525.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp231.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp500.png?nolink |}}
{{:chemogenomics:comparison_plots:exp125_vs_exp179.png?nolink |}}
{{:chemogenomics:comparison_plots:exp106_vs_exp179.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp356.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp32.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp485.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp360.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp215.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp460.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp312.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp311.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp310.png?nolink |}}
{{:chemogenomics:comparison_plots:exp162_vs_exp179.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp223.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp97.png?nolink |}}
^GO Term^Fold Change^Genes^
|microtubule organizing center localization|63.50|DLGAP5,ASPM,BICD2|
|centrosome localization|63.50|DLGAP5,ASPM,BICD2|
|spindle microtubule|31.48|MAPRE1,KNTC1,CALM2,SKA1|
|spindle pole|21.67|TACC3,DLGAP5,MAPRE1,ASPM,KNTC1,CALM2|
|regulation of microtubule cytoskeleton organization|19.30|STMN1,TACC3,MAPRE1,BICD2,SKA1|
|spindle organization|17.74|STMN1,TACC3,DLGAP5,MAPRE1,ASPM|
|mitotic spindle|17.24|TACC3,DLGAP5,MAPRE1,ASPM,SKA1|
|regulation of microtubule-based process|12.58|STMN1,TACC3,MAPRE1,BICD2,SKA1|
|spindle|11.83|TACC3,DLGAP5,KIF15,MAPRE1,ASPM,KNTC1,CALM2,SKA1|
|tubulin binding|11.77|STMN1,DLGAP5,KIF15,MAPRE1,VBP1,GTSE1,SKA1|
|microtubule|11.32|STMN1,KIF15,MAPRE1,ASPM,KNTC1,GTSE1,CALM2,SKA1|
|mitotic cell cycle|9.19|STMN1,TACC3,DLGAP5,KIF15,MAPRE1,KNTC1,GTSE1,CALM2,SKA1|
|mitotic cell cycle process|8.31|STMN1,TACC3,DLGAP5,MAPRE1,KNTC1,GTSE1,CALM2|
|centrosome|7.97|TACC3,DLGAP5,KIF15,MAPRE1,ASPM,CALM2,BICD2,SKA1|
|microtubule-based process|7.07|STMN1,TACC3,DLGAP5,KIF15,MAPRE1,ASPM,VBP1,GTSE1,BICD2|
|cell cycle process|7.03|STMN1,TACC3,DLGAP5,MAPRE1,ASPM,KNTC1,GTSE1,FBXW7,CALM2,SKA1|
|polymeric cytoskeletal fiber|6.61|STMN1,KIF15,MAPRE1,ASPM,KNTC1,GTSE1,CALM2,SKA1|
|microtubule organizing center|6.09|TACC3,DLGAP5,KIF15,MAPRE1,ASPM,CALM2,BICD2,SKA1|
|cytoskeletal protein binding|5.69|STMN1,DLGAP5,KIF15,MAPRE1,VBP1,GTSE1,CALM2,BICD2,SKA1|
^GO Term^Fold Change^Genes^
|ATPase regulator activity|47.02|ATP1B3,DNAJA1,GRPEL1,ATP6AP1|