====== Colchicine 0.009μM R05 exp215 ======
==== Mechanism of Action ====
Inhibits microtubule polymerization
* **Class / Subclass 1:** Cell Cycle / Microtubule Poison
* **Class / Subclass 2:** Organelle Function / Cytoskeletal Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%Colchicine%%
* **Synonyms:** N/A
* **CAS #:** 64-86-8
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/6167|6167]]
* **IUPAC:** %%N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl]acetamide%%
* **INCHI Name:** InChI=1S/C22H25NO6/c1-12(24)23-16-8-6-13-10-19(27-3)21(28-4)22(29-5)20(13)14-7-9-18(26-2)17(25)11-15(14)16/h7,9-11,16H,6,8H2,1-5H3,(H,23,24)/t16-/m0/s1
* **INCHI Key:** IAKHMKGGTNLKSZ-INIZCTEOSA-N
* **Molecular Weight:** 399.4
* **Canonical SMILES:** CC(=O)NC1CCC2=CC(=C(C(=C2C3=CC=C(C(=O)C=C13)OC)OC)OC)OC
* **Isomeric SMILES:** CC(=O)N[C@H]1CCC2=CC(=C(C(=C2C3=CC=C(C(=O)C=C13)OC)OC)OC)OC
* **Molecular Formula:** C22H25NO6
{{:chemogenomics:structures:chem-0111.svg?nolink}}
* **Supplier Name:** Sigma-Aldrich
* **Catalog #:** C9754
* **Lot #:** N/A
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C22H25NO6 400.17546; found 400.17564
* **Platform ID:** Colchicine
* **Min:** -2.2590; **Max:** 86.4027
{{:chemogenomics:dose_response:dr_198.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |0.0071 |
| IC30 |0.0091 |
| IC40 |0.0111 |
| IC50 |0.0133 |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 05
* **Dose**: 9nM
* **Days of incubation**: 8
* **Doublings**: 5.5
* **Numbers of reads**: 19549288
==== 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^
|58/26|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Colchicine_0.009uM_Round-5_exp215.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp215.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:K:KIF15|KIF15]]|-5.11|<0.01|
|[[:human_genes:S:STMN1|STMN1]]|-4.93|<0.01|
|[[:human_genes:K:KNTC1|KNTC1]]|-4.42|<0.01|
|[[:human_genes:D:DLGAP5|DLGAP5]]|-4.35|<0.01|
|[[:human_genes:L:LRRC8A|LRRC8A]]|-3.91|<0.01|
|[[:human_genes:S:SEPHS1|SEPHS1]]|-3.91|<0.01|
|[[:human_genes:A:ABCC1|ABCC1]]|-3.85|<0.01|
|[[:human_genes:D:DPH1|DPH1]]|-3.82|<0.01|
|[[:human_genes:T:TCF4|TCF4]]|-3.78|<0.01|
|[[:human_genes:V:VBP1|VBP1]]|-3.68|<0.01|
|[[:human_genes:M:MAPRE1|MAPRE1]]|-3.61|<0.01|
|[[:human_genes:G:GCLM|GCLM]]|-3.53|<0.01|
|[[:human_genes:T:TACC3|TACC3]]|-3.40|<0.01|
|[[:human_genes:X:XRN2|XRN2]]|-3.39|0.01|
|[[:human_genes:A:ASPM|ASPM]]|-3.27|<0.01|
|[[:human_genes:T:TUBB4B|TUBB4B]]|-3.13|<0.01|
|[[:human_genes:T:TMEM30A|TMEM30A]]|-3.12|<0.01|
|[[:human_genes:A:ATP8B2|ATP8B2]]|-3.10|<0.01|
|[[:human_genes:G:GTSE1|GTSE1]]|-3.07|<0.01|
|[[:human_genes:U:UFSP2|UFSP2]]|-3.07|<0.01|
|[[:human_genes:Q:QRICH1|QRICH1]]|-3.03|<0.01|
|[[:human_genes:M:MBNL1|MBNL1]]|-2.98|<0.01|
|[[:human_genes:R:RHOA|RHOA]]|-2.90|<0.01|
|[[:human_genes:Z:ZNF367|ZNF367]]|-2.80|<0.01|
|[[:human_genes:L:LUC7L2|LUC7L2]]|-2.79|<0.01|
|[[:human_genes:N:NAA60|NAA60]]|-2.74|<0.01|
|[[:human_genes:C:CNOT8|CNOT8]]|-2.71|<0.01|
|[[:human_genes:S:SKA1|SKA1]]|-2.69|<0.01|
|[[:human_genes:B:BICD2|BICD2]]|-2.68|0.01|
|[[:human_genes:S:SOX4|SOX4]]|-2.67|0.02|
|[[:human_genes:N:NUP107|NUP107]]|2.34|0.07|
|[[:human_genes:P:PRKAR1A|PRKAR1A]]|2.45|0.02|
|[[:human_genes:M:MCL1|MCL1]]|2.46|0.04|
|[[:human_genes:T:TIPRL|TIPRL]]|2.50|0.02|
|[[:human_genes:K:KIF4A|KIF4A]]|2.51|0.02|
|[[:human_genes:E:EPT1|EPT1]]|2.52|0.02|
|[[:human_genes:D:DNTTIP2|DNTTIP2]]|2.53|0.06|
|[[:human_genes:P:PEX12|PEX12]]|2.56|0.02|
|[[:human_genes:P:PIGF|PIGF]]|2.57|0.02|
|[[:human_genes:M:MED26|MED26]]|2.57|0.03|
|[[:human_genes:N:NDE1|NDE1]]|2.62|0.02|
|[[:human_genes:E:EIF3A|EIF3A]]|2.62|0.02|
|[[:human_genes:R:RFC1|RFC1]]|2.63|0.14|
|[[:human_genes:A:AHCYL1|AHCYL1]]|2.66|0.02|
|[[:human_genes:H:HSPE1|HSPE1]]|2.71|0.31|
|[[:human_genes:N:NUP133|NUP133]]|2.72|0.06|
|[[:human_genes:T:TMEM189-UBE2V1|TMEM189-UBE2V1]]|2.75|<0.01|
|[[:human_genes:D:DYNC1H1|DYNC1H1]]|2.79|0.31|
|[[:human_genes:P:PIP4K2A|PIP4K2A]]|2.91|0.02|
|[[:human_genes:P:PPP1CA|PPP1CA]]|2.92|<0.01|
|[[:human_genes:P:PSMC2|PSMC2]]|3.01|0.02|
|[[:human_genes:P:PPP1CC|PPP1CC]]|3.02|<0.01|
|[[:human_genes:P:PPP3CA|PPP3CA]]|3.09|<0.01|
|[[:human_genes:A:ATP1B3|ATP1B3]]|3.12|<0.01|
|[[:human_genes:T:TMEM189|TMEM189]]|3.28|<0.01|
|[[:human_genes:P:PPP3R1|PPP3R1]]|3.47|<0.01|
|[[:human_genes:A:ATP1A1|ATP1A1]]|4.19|<0.01|
|[[:human_genes:T:TMEM161B|TMEM161B]]|4.41|<0.01|
|[[:human_genes:A:ATAT1|ATAT1]]|4.70|<0.01|
|[[:human_genes:N:NUMA1|NUMA1]]|4.98|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp228|Demecolcine 0.03μM R05 exp228]]|0.189||
|[[:results:exp179|Combretastatin A4 0.002 to 0.003μM day4 R04 exp179]]|0.136||
|[[:results:exp190|Vincristine 0.0005μM R04 exp190]]|0.112||
|[[:results:exp217|Mdivi-1 15μM R05 exp217]]|0.098||
|[[:results:exp59|UMK57 1μM R01 exp59]]|0.085||
|[[:results:exp243|S-trityl-L-cysteine 0.5μM R05 exp243]]|0.083||
|[[:results:exp517|Quercetin 20μM R08 exp517]]|0.07||
|[[:results:exp184|Ixabepilone 0.004 to 0.005μM on day4 R04 exp184]]|0.066||
|[[:results:exp60|Vinblastine 0.002μM R01 exp60]]|0.065||
|[[:results:exp106|UM131593 0.2μM R03 exp106]]|0.063||
|[[:results:exp103|Taxol 0.004μM R03 exp103]]|0.06||
|[[:results:exp231|Epothilone-B 0.0015μM R05 exp231]]|0.056||
|[[:results:exp460|BML-284 0.09μM R08 exp460]]|0.136||
|[[:results:exp312|2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312]]|0.076||
|[[:results:exp311|2-Methoxyestradiol 0.55 to 0.75μM on day4 R07 exp311]]|0.072||
|[[:results:exp97|BI-6727 0.0125μM R03 exp97]]|0.061||
|[[:results:exp310|2-Methoxyestradiol 0.55μM R07 exp310]]|0.054||
{{:chemogenomics:comparison_plots:exp215_vs_exp228.png?nolink |}}
{{:chemogenomics:comparison_plots:exp179_vs_exp215.png?nolink |}}
{{:chemogenomics:comparison_plots:exp190_vs_exp215.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp217.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp59.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp243.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp517.png?nolink |}}
{{:chemogenomics:comparison_plots:exp184_vs_exp215.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp60.png?nolink |}}
{{:chemogenomics:comparison_plots:exp106_vs_exp215.png?nolink |}}
{{:chemogenomics:comparison_plots:exp103_vs_exp215.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp231.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp460.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp312.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp311.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp97.png?nolink |}}
{{:chemogenomics:comparison_plots:exp215_vs_exp310.png?nolink |}}
^GO Term^Fold Change^Genes^
|centrosome localization|61.22|DLGAP5,ASPM,BICD2|
|microtubule organizing center localization|61.22|DLGAP5,ASPM,BICD2|
|mitotic spindle organization|24.92|STMN1,DLGAP5,TACC3,RHOA|
|microtubule cytoskeleton organization involved in mitosis|22.94|STMN1,DLGAP5,MAPRE1,TACC3,RHOA|
|regulation of microtubule cytoskeleton organization|22.33|STMN1,MAPRE1,TACC3,RHOA,SKA1,BICD2|
|spindle organization|20.64|STMN1,DLGAP5,MAPRE1,TACC3,ASPM,RHOA|
|mitotic spindle|20.06|DLGAP5,MAPRE1,TACC3,ASPM,TUBB4B,SKA1|
|spindle pole|17.41|KNTC1,DLGAP5,MAPRE1,TACC3,ASPM|
|regulation of microtubule-based process|14.49|STMN1,MAPRE1,TACC3,RHOA,SKA1,BICD2|
|chromosome segregation|12.67|KNTC1,DLGAP5,MAPRE1,ASPM,RHOA,NAA60,SKA1|
|spindle|11.44|KIF15,KNTC1,DLGAP5,MAPRE1,TACC3,ASPM,TUBB4B,SKA1|
|tubulin binding|11.32|KIF15,STMN1,DLGAP5,VBP1,MAPRE1,GTSE1,SKA1|
|microtubule|10.91|KIF15,STMN1,KNTC1,MAPRE1,ASPM,TUBB4B,GTSE1,SKA1|
|mitotic cell cycle|9.83|KIF15,STMN1,KNTC1,DLGAP5,MAPRE1,TACC3,TUBB4B,GTSE1,RHOA,SKA1|
|microtubule cytoskeleton organization|8.78|STMN1,DLGAP5,MAPRE1,TACC3,ASPM,TUBB4B,RHOA,BICD2|
|microtubule-based process|8.35|KIF15,STMN1,DLGAP5,VBP1,MAPRE1,TACC3,ASPM,TUBB4B,GTSE1,RHOA,BICD2|
|cell division|8.19|STMN1,KNTC1,MAPRE1,TACC3,ASPM,RHOA,SKA1|
|mitotic cell cycle process|8.00|STMN1,KNTC1,DLGAP5,MAPRE1,TACC3,GTSE1,RHOA|
|cell cycle process|6.77|STMN1,KNTC1,DLGAP5,MAPRE1,TACC3,ASPM,GTSE1,RHOA,NAA60,SKA1|
^GO Term^Fold Change^Genes^
|ethanolaminephosphotransferase activity|552.33|PIGF,SELENOI|
|protein serine/threonine phosphatase complex|45.09|PPP3R1,PPP3CA,PPP1CC,PPP1CA|
|phosphatase complex|43.32|PPP3R1,PPP3CA,PPP1CC,PPP1CA|