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Ask your administrator if you think this is wrong. ====== SB743921 0.001μM R05 exp244 ====== ==== Mechanism of Action ==== Inhibits Eg5 kinesin, derivative of S-trityl-L-cysteine * **<color #00a2e8>Class / Subclass 1:</color>** Cell Cycle / Mitotic Inhibitor ==== Technical Notes ==== <accordion collapsed='true'> <panel title='Compound References' collapsed='true'> * **<color #00a2e8>PubChem Name:</color>** %%N-(3-Aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxochromen-2-yl)-2-methylpropyl]-4-methylbenzamide;hydrochloride%% * **<color #00a2e8>Synonyms:</color>** N/A * **<color #00a2e8>CAS #:</color>** 940929-33-9 * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/49867937|49867937]] * **<color #00a2e8>IUPAC:</color>** %%N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxochromen-2-yl)-2-methylpropyl]-4-methylbenzamide;hydrochloride%% * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C31H33ClN2O3.ClH/c1-20(2)28(34(17-7-16-33)31(36)23-12-10-21(3)11-13-23)30-26(18-22-8-5-4-6-9-22)29(35)25-15-14-24(32)19-27(25)37-30;/h4-6,8-15,19-20,28H,7,16-18,33H2,1-3H3;1H/t28-;/m1./s1 * **<color #00a2e8>INCHI Key:</color>** MLMZVWABFOLFGV-LNLSOMNWSA-N * **<color #00a2e8>Molecular Weight:</color>** 553.5 * **<color #00a2e8>Canonical SMILES:</color>** CC1=CC=C(C=C1)C(=O)N(CCCN)C(C2=C(C(=O)C3=C(O2)C=C(C=C3)Cl)CC4=CC=CC=C4)C(C)C.Cl * **<color #00a2e8>Isomeric SMILES:</color>** CC1=CC=C(C=C1)C(=O)N(CCCN)[C@@H](C2=C(C(=O)C3=C(O2)C=C(C=C3)Cl)CC4=CC=CC=C4)C(C)C.Cl * **<color #00a2e8>Molecular Formula:</color>** C31H34Cl2N2O3 {{:chemogenomics:structures:chem-0149.svg?nolink}} </panel> <panel title='Compound Supplier' collapsed='true'> * **<color #00a2e8>Supplier Name:</color>** N/A * **<color #00a2e8>Catalog #:</color>** N/A * **<color #00a2e8>Lot #:</color>** N/A </panel> <panel title='Compound Characterization' collapsed='true'> Characterization data not available. </panel> <panel title='Dose Response Curve' collapsed='true'> * **<color #00a2e8>Platform ID:</color>** SB743921 * **<color #00a2e8>Min:</color>** -3.7906; **<color #00a2e8>Max:</color>** 93.6518 {{:chemogenomics:dose_response:dr_276.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |0.0006 | | IC30 |0.0007 | | IC40 |0.0007 | | IC50 |0.0008 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ </panel> </accordion> ==== Screen Summary ==== * **<color #00a2e8>Round</color>**: 05 * **<color #00a2e8>Dose</color>**: 1nM * **<color #00a2e8>Days of incubation</color>**: 8 * **<color #00a2e8>Doublings</color>**: -0.0 * **<color #00a2e8>Numbers of reads</color>**: 22832707 ==== 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^ |0/155|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/SB743921_0.001uM_Round-5_exp244.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="default" size="sm" modal="modal_go_sensitive">View</button>|<button type="primary" size="sm" modal="modal_go_resistant">View</button>| <modal id='ScorePlot' size='lg' title='SB743921 0.001μM R05 exp244'> {{:chemogenomics:cranks_plots:exp244.png?nolink}} </modal> <modal id="modal_hits" size="sm" title="Top 30 S/R Genes"> ^Gene^CRANKS Score^FDR^ |[[:human_genes:C:COPA|COPA]]|-2.95|0.31| |[[:human_genes:A:AURKB|AURKB]]|-2.87|0.31| |[[:human_genes:T:TPX2|TPX2]]|-2.82|0.24| |[[:human_genes:P:PSMC5|PSMC5]]|-2.81|0.31| |[[:human_genes:S:SMC2|SMC2]]|-2.69|0.31| |[[:human_genes:U:UBE2Z|UBE2Z]]|-2.61|0.21| |[[:human_genes:T:TCERG1L|TCERG1L]]|-2.50|0.24| |[[:human_genes:T:TSC2|TSC2]]|-2.47|0.22| |[[:human_genes:S:SKIV2L2|SKIV2L2]]|-2.40|0.57| |[[:human_genes:O:OR2A14|OR2A14]]|-2.36|0.24| |[[:human_genes:T:TBCC|TBCC]]|-2.34|0.38| |[[:human_genes:C:CDC73|CDC73]]|-2.32|0.33| |[[:human_genes:P:PPP1R13L|PPP1R13L]]|-2.31|0.31| |[[:human_genes:P:PSMC6|PSMC6]]|-2.28|0.54| |[[:human_genes:Z:ZNF202|ZNF202]]|-2.26|0.31| |[[:human_genes:K:KRTAP4-8|KRTAP4-8]]|-2.19|0.38| |[[:human_genes:C:CTR9|CTR9]]|-2.18|0.38| |[[:human_genes:G:GSN|GSN]]|-2.17|0.31| |[[:human_genes:P:PTPRJ|PTPRJ]]|-2.17|0.31| |[[:human_genes:C:C1orf173|C1orf173]]|-2.11|0.31| |[[:human_genes:R:RBKS|RBKS]]|-2.09|0.31| |[[:human_genes:D:DNAJC21|DNAJC21]]|-2.09|0.31| |[[:human_genes:C:C1orf131|C1orf131]]|-2.07|0.38| |[[:human_genes:C:CEP250|CEP250]]|-2.07|0.31| |[[:human_genes:A:ASH2L|ASH2L]]|-2.07|0.31| |[[:human_genes:D:DONSON|DONSON]]|-2.07|0.69| |[[:human_genes:C:COG3|COG3]]|-2.07|0.38| |[[:human_genes:A:ANKRD12|ANKRD12]]|-2.07|0.31| |[[:human_genes:C:CHMP6|CHMP6]]|-2.06|0.31| |[[:human_genes:A:ANKRD34A|ANKRD34A]]|-2.05|0.31| |[[:human_genes:P:PDE1C|PDE1C]]|3.47|<0.01| |[[:human_genes:I:IGF2BP3|IGF2BP3]]|3.47|<0.01| |[[:human_genes:R:RADIL|RADIL]]|3.47|<0.01| |[[:human_genes:H:HOXA1|HOXA1]]|3.49|<0.01| |[[:human_genes:H:HDAC9|HDAC9]]|3.51|<0.01| |[[:human_genes:N:NT5C3A|NT5C3A]]|3.53|<0.01| |[[:human_genes:D:DCTN5|DCTN5]]|3.69|<0.01| |[[:human_genes:I:INMT|INMT]]|3.76|<0.01| |[[:human_genes:B:BZW2|BZW2]]|4.09|<0.01| |[[:human_genes:R:RAC1|RAC1]]|4.13|<0.01| |[[:human_genes:T:TNRC18|TNRC18]]|4.15|<0.01| |[[:human_genes:M:MAD2L1BP|MAD2L1BP]]|4.16|<0.01| |[[:human_genes:U:USP42|USP42]]|4.31|<0.01| |[[:human_genes:R:RBM14-RBM4|RBM14-RBM4]]|4.41|<0.01| |[[:human_genes:C:CYTH3|CYTH3]]|4.43|<0.01| |[[:human_genes:R:RBM14|RBM14]]|4.56|<0.01| |[[:human_genes:I:ITGB8|ITGB8]]|4.67|<0.01| |[[:human_genes:A:AMZ1|AMZ1]]|4.69|<0.01| |[[:human_genes:B:BMPER|BMPER]]|4.74|<0.01| |[[:human_genes:Z:ZWILCH|ZWILCH]]|4.93|<0.01| |[[:human_genes:P:PAFAH1B1|PAFAH1B1]]|5.04|<0.01| |[[:human_genes:M:MAD1L1|MAD1L1]]|5.20|<0.01| |[[:human_genes:D:DYNLRB1|DYNLRB1]]|5.54|<0.01| |[[:human_genes:D:DYNC1H1|DYNC1H1]]|5.70|<0.01| |[[:human_genes:B:BUB3|BUB3]]|5.75|<0.01| |[[:human_genes:B:BUB1B|BUB1B]]|5.87|<0.01| |[[:human_genes:M:MAD2L1|MAD2L1]]|6.04|<0.01| |[[:human_genes:Z:ZW10|ZW10]]|6.17|<0.01| |[[:human_genes:K:KNTC1|KNTC1]]|6.56|<0.01| |[[:human_genes:T:TRIP13|TRIP13]]|7.14|<0.01| </modal> <modal id="modal_screen_similarity" size="lg" title="Correlated Screens"> ^Screen^Correlation^Plot^ |[[:results:exp208|Vinblastine 0.015μM R05 exp208]]|0.291|<button type="primary" size="small" modal="1">View</button>| |[[:results:exp94|Nocodazole 0.1μM R03 exp94]]|0.341|<button type="primary" size="small" modal="2">View</button>| |[[:results:exp33|Rotenone 2μM R00 exp33]]|0.338|<button type="primary" size="small" modal="3">View</button>| |[[:results:exp24|Nocodazole 0.2μM R00 exp24]]|0.311|<button type="primary" size="small" modal="4">View</button>| |[[:results:exp93|DABN racemic mixture R03 exp93]]|0.273|<button type="primary" size="small" modal="5">View</button>| |[[:results:exp111|R-DABN 8μM R03 exp111]]|0.227|<button type="primary" size="small" modal="6">View</button>| |[[:results:exp64|Nocodazole 0.2μM R02 exp64]]|0.221|<button type="primary" size="small" modal="7">View</button>| |[[:results:exp256|HMS-I1 10μM R06 exp256]]|0.216|<button type="primary" size="small" modal="8">View</button>| |[[:results:exp98|BI-6727 0.04μM R03 exp98]]|0.091|<button type="primary" size="small" modal="9">View</button>| </modal> <modal id="1" size="lg" title="SB743921 0.001μM R05 exp244 vs Vinblastine 0.015μM R05 exp208"> {{:chemogenomics:comparison_plots:exp208_vs_exp244.png?nolink |}} </modal> <modal id="2" size="lg" title="Nocodazole 0.1μM R03 exp94 vs SB743921 0.001μM R05 exp244"> {{:chemogenomics:comparison_plots:exp244_vs_exp94.png?nolink |}} </modal> <modal id="3" size="lg" title="Rotenone 2μM R00 exp33 vs SB743921 0.001μM R05 exp244"> {{:chemogenomics:comparison_plots:exp244_vs_exp33.png?nolink |}} </modal> <modal id="4" size="lg" title="Nocodazole 0.2μM R00 exp24 vs SB743921 0.001μM R05 exp244"> {{:chemogenomics:comparison_plots:exp24_vs_exp244.png?nolink |}} </modal> <modal id="5" size="lg" title="DABN racemic mixture R03 exp93 vs SB743921 0.001μM R05 exp244"> {{:chemogenomics:comparison_plots:exp244_vs_exp93.png?nolink |}} </modal> <modal id="6" size="lg" title="R-DABN 8μM R03 exp111 vs SB743921 0.001μM R05 exp244"> {{:chemogenomics:comparison_plots:exp111_vs_exp244.png?nolink |}} </modal> <modal id="7" size="lg" title="Nocodazole 0.2μM R02 exp64 vs SB743921 0.001μM R05 exp244"> {{:chemogenomics:comparison_plots:exp244_vs_exp64.png?nolink |}} </modal> <modal id="8" size="lg" title="HMS-I1 10μM R06 exp256 vs SB743921 0.001μM R05 exp244"> {{:chemogenomics:comparison_plots:exp244_vs_exp256.png?nolink |}} </modal> <modal id="9" size="lg" title="BI-6727 0.04μM R03 exp98 vs SB743921 0.001μM R05 exp244"> {{:chemogenomics:comparison_plots:exp244_vs_exp98.png?nolink |}} </modal> <modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">No GO term hits below threshold. (FDR <0.05)</modal> <modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms"> ^GO Term^Fold Change^Genes^ |mitotic spindle checkpoint signaling|157.81|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH| |spindle assembly checkpoint signaling|157.81|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH| |mitotic spindle assembly checkpoint signaling|157.81|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH| |negative regulation of mitotic sister chromatid segregation|142.54|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH| |negative regulation of mitotic sister chromatid separation|142.54|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH| |negative regulation of metaphase/anaphase transition of cell cycle|133.90|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH| |negative regulation of chromosome separation|133.90|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH| |negative regulation of chromosome segregation|133.90|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH| |spindle checkpoint signaling|133.32|TRIP13,KNTC1,ZW10,BUB1B,BUB3,MAD1L1,ZWILCH| |negative regulation of mitotic metaphase/anaphase transition|124.72|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,MAD1L1,ZWILCH| |negative regulation of sister chromatid segregation|124.72|TRIP13,KNTC1,ZW10,BUB1B,BUB3,MAD1L1,ZWILCH| |negative regulation of nuclear division|96.06|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH| |regulation of mitotic sister chromatid segregation|93.79|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH,MAD2L1BP| |regulation of mitotic sister chromatid separation|77.52|TRIP13,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH,MAD2L1BP| |regulation of chromosome separation|69.04|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH,MAD2L1BP| |regulation of mitotic metaphase/anaphase transition|56.49|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH,MAD2L1BP| |regulation of metaphase/anaphase transition of cell cycle|54.63|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH,MAD2L1BP| |regulation of sister chromatid segregation|48.74|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH,MAD2L1BP| |regulation of mitotic nuclear division|42.85|TRIP13,KNTC1,ZW10,MAD2L1,BUB1B,BUB3,MAD1L1,ZWILCH,MAD2L1BP| </modal> Last modified: 2026/01/15 21:36by 127.0.0.1