====== Vinblastine 0.015μM R05 exp208 ======
==== Mechanism of Action ====
Inhibits microtubule polymerization and mitotic spindle formation, induces spindle assembly checkpoint (SAC)
* **Class / Subclass 1:** Cell Cycle / Microtubule Poison
* **Class / Subclass 2:** Organelle Function / Cytoskeletal Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%Vincaleukoblastine sulfate%%
* **Synonyms:** Vincaleukoblastine sulfate salt
* **CAS #:** 143-67-9
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/241902|241902]]
* **IUPAC:** %%methyl (1R,9R,10S,11R,12R,19R)-11-acetyloxy-12-ethyl-4-[(13S,15S,17S)-17-ethyl-17-hydroxy-13-methoxycarbonyl-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraen-13-yl]-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraene-10-carboxylate;sulfuric acid%%
* **INCHI Name:** InChI=1S/C46H58N4O9.H2O4S/c1-8-42(54)23-28-24-45(40(52)57-6,36-30(15-19-49(25-28)26-42)29-13-10-11-14-33(29)47-36)32-21-31-34(22-35(32)56-5)48(4)38-44(31)17-20-50-18-12-16-43(9-2,37(44)50)39(59-27(3)51)46(38,55)41(53)58-7;1-5(2,3)4/h10-14,16,21-22,28,37-39,47,54-55H,8-9,15,17-20,23-26H2,1-7H3;(H2,1,2,3,4)/t28-,37+,38-,39-,42+,43-,44-,45+,46+;/m1./s1
* **INCHI Key:** KDQAABAKXDWYSZ-JKDPCDLQSA-N
* **Molecular Weight:** 909.1
* **Canonical SMILES:** CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O
* **Isomeric SMILES:** CC[C@@]1(C[C@@H]2C[C@@](C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)[C@]78CCN9[C@H]7[C@@](C=CC9)([C@H]([C@@]([C@@H]8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O
* **Molecular Formula:** C46H60N4O13S
{{:chemogenomics:structures:chem-0040.svg?nolink}}
* **Supplier Name:** Sigma-Aldrich
* **Catalog #:** V1377
* **Lot #:** N/A
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C46H58N4O9 811.42766; found 811.42916
* **Platform ID:** Vinblastine
* **Min:** -7.8990; **Max:** 88.1311
{{:chemogenomics:dose_response:dr_250.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |0.0045 |
| IC30 |0.0051 |
| IC40 |0.0056 |
| IC50 |0.0056 |
| IC60 |N/A |
| IC70 |0.0079 |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 05
* **Dose**: 15nM
* **Days of incubation**: 8
* **Doublings**: -0.1
* **Numbers of reads**: 20529421
==== 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^
|0/70|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Vinblastine_0.015uM_Round-5_exp208.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp208.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:D:DONSON|DONSON]]|-2.57|0.68|
|[[:human_genes:A:ANKRD17|ANKRD17]]|-2.54|0.32|
|[[:human_genes:M:MTCH2|MTCH2]]|-2.46|0.37|
|[[:human_genes:A:ARCN1|ARCN1]]|-2.43|0.42|
|[[:human_genes:F:FAM200A|FAM200A]]|-2.43|0.37|
|[[:human_genes:C:C18orf32|C18orf32]]|-2.38|0.63|
|[[:human_genes:R:RPL36A-HNRNPH2|RPL36A-HNRNPH2]]|-2.37|0.75|
|[[:human_genes:A:AURKB|AURKB]]|-2.30|0.57|
|[[:human_genes:A:ATP6V1B2|ATP6V1B2]]|-2.30|0.42|
|[[:human_genes:M:MTA2|MTA2]]|-2.28|0.37|
|[[:human_genes:P:PLK4|PLK4]]|-2.27|0.42|
|[[:human_genes:P:PSMD14|PSMD14]]|-2.27|0.68|
|[[:human_genes:P:PSMA1|PSMA1]]|-2.26|0.42|
|[[:human_genes:L:LRMP|LRMP]]|-2.23|0.42|
|[[:human_genes:C:CADPS|CADPS]]|-2.19|0.42|
|[[:human_genes:C:CCDC27|CCDC27]]|-2.17|0.51|
|[[:human_genes:N:NSF|NSF]]|-2.16|0.57|
|[[:human_genes:S:SACS|SACS]]|-2.16|0.42|
|[[:human_genes:N:NHP2L1|NHP2L1]]|-2.15|0.51|
|[[:human_genes:H:HIVEP3|HIVEP3]]|-2.14|0.51|
|[[:human_genes:S:STAC2|STAC2]]|-2.12|0.42|
|[[:human_genes:M:MBTD1|MBTD1]]|-2.08|0.45|
|[[:human_genes:P:PLCG2|PLCG2]]|-2.07|0.42|
|[[:human_genes:N:NKIRAS2|NKIRAS2]]|-2.07|0.42|
|[[:human_genes:C:CEP290|CEP290]]|-2.04|0.42|
|[[:human_genes:Z:ZNF275|ZNF275]]|-2.03|0.42|
|[[:human_genes:A:ATP6V1A|ATP6V1A]]|-2.03|0.51|
|[[:human_genes:E:EIF6|EIF6]]|-2.02|0.63|
|[[:human_genes:F:FARP2|FARP2]]|-2.01|0.42|
|[[:human_genes:B:BCL2L1|BCL2L1]]|-2.01|0.42|
|[[:human_genes:C:CHST12|CHST12]]|2.91|<0.01|
|[[:human_genes:I:IQCE|IQCE]]|2.99|<0.01|
|[[:human_genes:W:WDR82|WDR82]]|3.02|<0.01|
|[[:human_genes:C:CDC20|CDC20]]|3.10|<0.01|
|[[:human_genes:K:KLHL7|KLHL7]]|3.13|<0.01|
|[[:human_genes:Z:ZPBP|ZPBP]]|3.16|<0.01|
|[[:human_genes:H:HOXA13|HOXA13]]|3.17|<0.01|
|[[:human_genes:S:SNX8|SNX8]]|3.18|<0.01|
|[[:human_genes:H:HOXA5|HOXA5]]|3.21|<0.01|
|[[:human_genes:R:RADIL|RADIL]]|3.26|<0.01|
|[[:human_genes:L:LRRC72|LRRC72]]|3.30|<0.01|
|[[:human_genes:S:SLC29A4|SLC29A4]]|3.34|<0.01|
|[[:human_genes:T:TNRC18|TNRC18]]|3.37|<0.01|
|[[:human_genes:C:CAMK2B|CAMK2B]]|3.38|<0.01|
|[[:human_genes:P:PELO|PELO]]|3.48|<0.01|
|[[:human_genes:B:BMPER|BMPER]]|3.51|<0.01|
|[[:human_genes:G:GNA12|GNA12]]|3.54|<0.01|
|[[:human_genes:P:PDE1C|PDE1C]]|3.64|<0.01|
|[[:human_genes:Z:ZWILCH|ZWILCH]]|3.93|<0.01|
|[[:human_genes:M:MAD2L1BP|MAD2L1BP]]|4.35|<0.01|
|[[:human_genes:A:AMZ1|AMZ1]]|4.40|<0.01|
|[[:human_genes:B:BUB1B|BUB1B]]|5.61|<0.01|
|[[:human_genes:M:MAD1L1|MAD1L1]]|5.67|<0.01|
|[[:human_genes:M:MAD2L1|MAD2L1]]|5.87|<0.01|
|[[:human_genes:R:RBM14-RBM4|RBM14-RBM4]]|5.92|<0.01|
|[[:human_genes:R:RBM14|RBM14]]|6.54|<0.01|
|[[:human_genes:B:BUB3|BUB3]]|6.86|<0.01|
|[[:human_genes:Z:ZW10|ZW10]]|7.42|<0.01|
|[[:human_genes:T:TRIP13|TRIP13]]|7.56|<0.01|
|[[:human_genes:K:KNTC1|KNTC1]]|8.10|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp108|Vinblastine 0.2μM R03 exp108]]|0.057||
|[[:results:exp244|SB743921 0.001μM R05 exp244]]|0.291||
|[[:results:exp24|Nocodazole 0.2μM R00 exp24]]|0.245||
|[[:results:exp94|Nocodazole 0.1μM R03 exp94]]|0.225||
|[[:results:exp33|Rotenone 2μM R00 exp33]]|0.225||
|[[:results:exp64|Nocodazole 0.2μM R02 exp64]]|0.19||
|[[:results:exp256|HMS-I1 10μM R06 exp256]]|0.189||
|[[:results:exp93|DABN racemic mixture R03 exp93]]|0.185||
|[[:results:exp111|R-DABN 8μM R03 exp111]]|0.169||
|[[:results:exp98|BI-6727 0.04μM R03 exp98]]|0.075||
|[[:results:exp17|DABN 20μM R00 exp17]]|0.074||
{{:chemogenomics:comparison_plots:exp108_vs_exp208.png?nolink |}}
{{:chemogenomics:comparison_plots:exp208_vs_exp244.png?nolink |}}
{{:chemogenomics:comparison_plots:exp208_vs_exp24.png?nolink |}}
{{:chemogenomics:comparison_plots:exp208_vs_exp94.png?nolink |}}
{{:chemogenomics:comparison_plots:exp208_vs_exp33.png?nolink |}}
{{:chemogenomics:comparison_plots:exp208_vs_exp64.png?nolink |}}
{{:chemogenomics:comparison_plots:exp208_vs_exp256.png?nolink |}}
{{:chemogenomics:comparison_plots:exp208_vs_exp93.png?nolink |}}
{{:chemogenomics:comparison_plots:exp111_vs_exp208.png?nolink |}}
{{:chemogenomics:comparison_plots:exp208_vs_exp98.png?nolink |}}
{{:chemogenomics:comparison_plots:exp17_vs_exp208.png?nolink |}}
No GO term hits below threshold. (FDR <0.05)
^GO Term^Fold Change^Genes^
|mitotic spindle assembly checkpoint signaling|177.54|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|mitotic spindle checkpoint signaling|177.54|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|spindle assembly checkpoint signaling|177.54|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|negative regulation of mitotic sister chromatid segregation|160.35|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|negative regulation of mitotic sister chromatid separation|160.35|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|spindle checkpoint signaling|152.37|KNTC1,TRIP13,ZW10,BUB3,MAD1L1,BUB1B,ZWILCH,CDC20|
|negative regulation of chromosome segregation|150.64|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|negative regulation of chromosome separation|150.64|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|negative regulation of metaphase/anaphase transition of cell cycle|150.64|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|negative regulation of mitotic metaphase/anaphase transition|142.54|KNTC1,TRIP13,ZW10,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|negative regulation of sister chromatid segregation|142.54|KNTC1,TRIP13,ZW10,BUB3,MAD1L1,BUB1B,ZWILCH,CDC20|
|negative regulation of nuclear division|108.07|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,ZWILCH,CDC20|
|regulation of mitotic sister chromatid segregation|93.79|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,MAD2L1BP,ZWILCH|
|regulation of mitotic sister chromatid separation|87.21|TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,MAD2L1BP,ZWILCH,CDC20|
|regulation of chromosome separation|76.71|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,MAD2L1BP,ZWILCH,CDC20|
|regulation of mitotic metaphase/anaphase transition|62.77|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,MAD2L1BP,ZWILCH,CDC20|
|regulation of metaphase/anaphase transition of cell cycle|60.70|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,MAD2L1BP,ZWILCH,CDC20|
|regulation of mitotic nuclear division|52.38|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,MAD2L1BP,ZWILCH,HOXA13,CDC20|
|regulation of nuclear division|42.49|KNTC1,TRIP13,ZW10,BUB3,MAD2L1,MAD1L1,BUB1B,MAD2L1BP,ZWILCH,HOXA13,CDC20|