====== Vinblastine 0.2μM R03 exp108 ======
==== 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:** -0.8093; **Max:** 78.3626
{{:chemogenomics:dose_response:dr_162.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |0.0461 |
| IC30 |0.1198 |
| IC40 |0.2622 |
| IC50 |0.5380 |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 03
* **Dose**: 200nM
* **Days of incubation**: 8
* **Doublings**: -0.6
* **Numbers of reads**: 10228528
==== 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^
|0/13|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Vinblastine_0.2uM_Round-3_exp108.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp108.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:S:SART1|SART1]]|-2.76|0.74|
|[[:human_genes:U:UNC50|UNC50]]|-2.57|0.26|
|[[:human_genes:N:NMRAL1|NMRAL1]]|-2.56|0.35|
|[[:human_genes:Y:YTHDC1|YTHDC1]]|-2.34|0.74|
|[[:human_genes:P:PTCH1|PTCH1]]|-2.22|0.63|
|[[:human_genes:L:LMLN|LMLN]]|-2.19|0.58|
|[[:human_genes:C:C10orf111|C10orf111]]|-2.17|0.58|
|[[:human_genes:S:SEPHS2|SEPHS2]]|-2.16|0.58|
|[[:human_genes:A:ANAPC2|ANAPC2]]|-2.11|0.63|
|[[:human_genes:V:VPS52|VPS52]]|-2.10|0.74|
|[[:human_genes:T:TEX13B|TEX13B]]|-2.07|0.63|
|[[:human_genes:T:TBL1XR1|TBL1XR1]]|-2.06|0.63|
|[[:human_genes:O:OLFML2B|OLFML2B]]|-2.05|0.63|
|[[:human_genes:M:MGA|MGA]]|-2.04|0.63|
|[[:human_genes:V:VPS28|VPS28]]|-2.02|0.63|
|[[:human_genes:M:MAEA|MAEA]]|-2.00|0.63|
|[[:human_genes:A:ATP6V0C|ATP6V0C]]|-1.98|0.65|
|[[:human_genes:R:RACGAP1|RACGAP1]]|-1.97|0.63|
|[[:human_genes:C:CCNB1|CCNB1]]|-1.96|0.63|
|[[:human_genes:H:H2BFWT|H2BFWT]]|-1.94|0.63|
|[[:human_genes:L:L3MBTL2|L3MBTL2]]|-1.94|0.63|
|[[:human_genes:F:FCRL2|FCRL2]]|-1.90|0.63|
|[[:human_genes:E:EBP|EBP]]|-1.89|0.63|
|[[:human_genes:Z:ZNF839|ZNF839]]|-1.89|0.63|
|[[:human_genes:T:TBC1D7|TBC1D7]]|-1.88|0.63|
|[[:human_genes:T:TIMM17B|TIMM17B]]|-1.88|0.63|
|[[:human_genes:Z:ZNF335|ZNF335]]|-1.88|0.74|
|[[:human_genes:T:TSPAN14|TSPAN14]]|-1.88|0.63|
|[[:human_genes:T:TSG101|TSG101]]|-1.87|0.63|
|[[:human_genes:S:SRCAP|SRCAP]]|-1.87|0.63|
|[[:human_genes:P:PP2D1|PP2D1]]|2.11|0.16|
|[[:human_genes:U:UBE2G2|UBE2G2]]|2.13|0.16|
|[[:human_genes:P:PAM16|PAM16]]|2.18|0.17|
|[[:human_genes:A:ATP5O|ATP5O]]|2.20|0.12|
|[[:human_genes:T:TRIAP1|TRIAP1]]|2.23|0.16|
|[[:human_genes:M:MED13L|MED13L]]|2.25|0.16|
|[[:human_genes:T:TTI1|TTI1]]|2.25|0.20|
|[[:human_genes:P:PDSS1|PDSS1]]|2.30|0.19|
|[[:human_genes:M:MOCS3|MOCS3]]|2.32|0.18|
|[[:human_genes:R:ROMO1|ROMO1]]|2.32|0.13|
|[[:human_genes:P:PELO|PELO]]|2.33|0.17|
|[[:human_genes:P:PPP6C|PPP6C]]|2.43|0.08|
|[[:human_genes:R:RPTOR|RPTOR]]|2.48|0.03|
|[[:human_genes:M:MS4A13|MS4A13]]|2.54|0.48|
|[[:human_genes:D:DOHH|DOHH]]|2.55|0.05|
|[[:human_genes:R:RTCB|RTCB]]|2.56|0.16|
|[[:human_genes:C:CYCS|CYCS]]|2.57|0.03|
|[[:human_genes:T:TRMT10A|TRMT10A]]|2.60|0.04|
|[[:human_genes:Q:QSER1|QSER1]]|2.67|0.03|
|[[:human_genes:G:GFPT1|GFPT1]]|2.92|0.03|
|[[:human_genes:B:BUB3|BUB3]]|3.04|0.08|
|[[:human_genes:D:DPAGT1|DPAGT1]]|3.28|0.02|
|[[:human_genes:P:PYROXD1|PYROXD1]]|3.35|0.08|
|[[:human_genes:M:MAD2L1BP|MAD2L1BP]]|3.40|<0.01|
|[[:human_genes:Z:ZW10|ZW10]]|3.65|<0.01|
|[[:human_genes:M:MAD1L1|MAD1L1]]|4.41|<0.01|
|[[:human_genes:B:BUB1B|BUB1B]]|5.74|<0.01|
|[[:human_genes:K:KNTC1|KNTC1]]|5.88|<0.01|
|[[:human_genes:M:MAD2L1|MAD2L1]]|6.82|<0.01|
|[[:human_genes:T:TRIP13|TRIP13]]|7.82|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp126|GSK461364A 0.1μM R03 exp126]]|0.141||
|[[:results:exp98|BI-6727 0.04μM R03 exp98]]|0.128||
|[[:results:exp96|BI-2536 0.02μM R03 exp96]]|0.119||
|[[:results:exp111|R-DABN 8μM R03 exp111]]|0.106||
|[[:results:exp448|Ammonium tetrathiomolybdate 10μM R08 exp448]]|0.091||
|[[:results:exp64|Nocodazole 0.2μM R02 exp64]]|0.077||
|[[:results:exp93|DABN racemic mixture R03 exp93]]|0.076||
|[[:results:exp17|DABN 20μM R00 exp17]]|0.071||
|[[:results:exp456|Benzoate 20000μM R08 exp456]]|0.068||
|[[:results:exp539|42°C R08 exp539]]|0.065||
|[[:results:exp256|HMS-I1 10μM R06 exp256]]|0.065||
|[[:results:exp487|Hinokiflavone 12μM R08 exp487]]|0.065||
|[[:results:exp199|Etoposide 0.3μM R05 exp199]]|0.065||
|[[:results:exp443|SNS-032 15μM R08 exp443]]|0.064||
|[[:results:exp472|CI-1040 9.5μM R08 exp472]]|0.063||
|[[:results:exp259|6-Thio-2-deoxyguanosine 2μM R06 exp259]]|0.062||
|[[:results:exp24|Nocodazole 0.2μM R00 exp24]]|0.06||
|[[:results:exp208|Vinblastine 0.015μM R05 exp208]]|0.057||
|[[:results:exp94|Nocodazole 0.1μM R03 exp94]]|0.056||
|[[:results:exp459|Bleomycin 5μM R08 exp459]]|0.055||
|[[:results:exp22|MLN-4924 2μM R00 exp22]]|0.054||
|[[:results:exp478|Doxorubicin 0.02μM R08 exp478]]|0.053||
|[[:results:exp33|Rotenone 2μM R00 exp33]]|0.052||
|[[:results:exp106|UM131593 0.2μM R03 exp106]]|0.051||
|[[:results:exp532|TIC10 10μM R08 exp532]]|0.051||
|[[:results:exp515|PU-H71 1μM R08 exp515]]|0.051||
|[[:results:exp135|MS023 7μM R03 exp135]]|0.051||
{{:chemogenomics:comparison_plots:exp108_vs_exp126.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp98.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp96.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp111.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp448.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp64.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp93.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp17.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp456.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp539.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp256.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp487.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp199.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp443.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp472.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp259.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp24.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp208.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp94.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp459.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp22.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp478.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp33.png?nolink |}}
{{:chemogenomics:comparison_plots:exp106_vs_exp108.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp532.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp515.png?nolink |}}
{{:chemogenomics:comparison_plots:exp108_vs_exp135.png?nolink |}}
No GO term hits below threshold. (FDR <0.05)
^GO Term^Fold Change^Genes^
|spindle assembly checkpoint signaling|138.16|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|mitotic spindle assembly checkpoint signaling|138.16|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|mitotic spindle checkpoint signaling|138.16|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|negative regulation of mitotic sister chromatid separation|124.79|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|negative regulation of mitotic sister chromatid segregation|124.79|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|negative regulation of metaphase/anaphase transition of cell cycle|117.23|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|negative regulation of chromosome segregation|117.23|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|negative regulation of chromosome separation|117.23|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|spindle checkpoint signaling|114.34|TRIP13,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|negative regulation of mitotic metaphase/anaphase transition|106.96|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10|
|negative regulation of sister chromatid segregation|106.96|TRIP13,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|negative regulation of nuclear division|84.10|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,BUB3|
|regulation of mitotic sister chromatid segregation|83.42|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,MAD2L1BP,BUB3|
|regulation of mitotic sister chromatid separation|66.70|TRIP13,MAD2L1,BUB1B,MAD1L1,ZW10,MAD2L1BP,BUB3|
|regulation of chromosome separation|60.56|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,MAD2L1BP,BUB3|
|regulation of mitotic metaphase/anaphase transition|49.67|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,MAD2L1BP,BUB3|
|regulation of metaphase/anaphase transition of cell cycle|48.06|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,MAD2L1BP,BUB3|
|regulation of sister chromatid segregation|42.92|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,MAD2L1BP,BUB3|
|regulation of mitotic nuclear division|37.79|TRIP13,MAD2L1,KNTC1,BUB1B,MAD1L1,ZW10,MAD2L1BP,BUB3|