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Ask your administrator if you think this is wrong. ====== Golgicide-A 4μM R03 exp122 ====== ==== Mechanism of Action ==== Inhibits cis-Golgi ArfGEF, blocks secretion at ER-Golgi * **<color #00a2e8>Class / Subclass 1:</color>** Organelle Function / Vesicule Trafficking Inhibitor ==== Technical Notes ==== <accordion collapsed='true'> <panel title='Compound References' collapsed='true'> * **<color #00a2e8>PubChem Name:</color>** %%6,8-Difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline%% * **<color #00a2e8>Synonyms:</color>** N/A * **<color #00a2e8>CAS #:</color>** 1005036-73-6 * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/3154410|3154410]] * **<color #00a2e8>IUPAC:</color>** %%6,8-difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline%% * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C17H14F2N2/c18-11-7-14-12-4-1-5-13(12)16(10-3-2-6-20-9-10)21-17(14)15(19)8-11/h1-4,6-9,12-13,16,21H,5H2 * **<color #00a2e8>INCHI Key:</color>** NJZHEQOUHLZCOX-UHFFFAOYSA-N * **<color #00a2e8>Molecular Weight:</color>** 284.3 * **<color #00a2e8>Canonical SMILES:</color>** C1C=CC2C1C(NC3=C2C=C(C=C3F)F)C4=CN=CC=C4 * **<color #00a2e8>Isomeric SMILES:</color>** N/A * **<color #00a2e8>Molecular Formula:</color>** C17H14F2N2 {{:chemogenomics:structures:chem-0075.svg?nolink}} </panel> <panel title='Compound Supplier' collapsed='true'> * **<color #00a2e8>Supplier Name:</color>** Sigma-Aldrich * **<color #00a2e8>Catalog #:</color>** G0923 * **<color #00a2e8>Lot #:</color>** 105M4619V </panel> <panel title='Compound Characterization' collapsed='true'> * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+H)+ Calcd for C17H14F2N2 285.11978; found 285.11995 </panel> <panel title='Dose Response Curve'> Dose response curve not available. </panel> </accordion> ==== Screen Summary ==== * **<color #00a2e8>Round</color>**: 03 * **<color #00a2e8>Dose</color>**: 4µM * **<color #00a2e8>Days of incubation</color>**: 8 * **<color #00a2e8>Doublings</color>**: 7.0 * **<color #00a2e8>Numbers of reads</color>**: 15252670 ==== 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^ |66/23|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Golgicide_A_4uM_Round-3_exp122.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="primary" 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='Golgicide-A 4μM R03 exp122'> {{:chemogenomics:cranks_plots:exp122.png?nolink}} </modal> <modal id="modal_hits" size="sm" title="Top 30 S/R Genes"> ^Gene^CRANKS Score^FDR^ |[[:human_genes:A:ARF1|ARF1]]|-4.82|<0.01| |[[:human_genes:S:SLC35E1|SLC35E1]]|-4.26|<0.01| |[[:human_genes:R:RAB3GAP2|RAB3GAP2]]|-4.12|<0.01| |[[:human_genes:P:PDIA6|PDIA6]]|-3.97|<0.01| |[[:human_genes:D:DRG2|DRG2]]|-3.77|<0.01| |[[:human_genes:Y:YIPF5|YIPF5]]|-3.75|<0.01| |[[:human_genes:N:NPRL3|NPRL3]]|-3.71|<0.01| |[[:human_genes:D:DNAJC3|DNAJC3]]|-3.64|<0.01| |[[:human_genes:S:SZT2|SZT2]]|-3.39|<0.01| |[[:human_genes:A:ATP2B1|ATP2B1]]|-3.33|<0.01| |[[:human_genes:C:CSK|CSK]]|-3.21|<0.01| |[[:human_genes:R:RBM26|RBM26]]|-3.15|<0.01| |[[:human_genes:A:ATG9A|ATG9A]]|-3.08|<0.01| |[[:human_genes:D:DERL2|DERL2]]|-3.08|<0.01| |[[:human_genes:T:TMED10|TMED10]]|-3.00|<0.01| |[[:human_genes:K:KIAA0922|KIAA0922]]|-2.97|<0.01| |[[:human_genes:C:C1orf27|C1orf27]]|-2.97|<0.01| |[[:human_genes:P:PRKAA1|PRKAA1]]|-2.87|<0.01| |[[:human_genes:U:UBA6|UBA6]]|-2.87|<0.01| |[[:human_genes:M:MANF|MANF]]|-2.84|<0.01| |[[:human_genes:R:RBM14|RBM14]]|-2.83|0.01| |[[:human_genes:I:ITFG2|ITFG2]]|-2.78|<0.01| |[[:human_genes:P:PLAA|PLAA]]|-2.76|<0.01| |[[:human_genes:V:VKORC1L1|VKORC1L1]]|-2.75|<0.01| |[[:human_genes:R:RBM14-RBM4|RBM14-RBM4]]|-2.74|0.02| |[[:human_genes:P:PTPN6|PTPN6]]|-2.71|<0.01| |[[:human_genes:U:UFC1|UFC1]]|-2.70|<0.01| |[[:human_genes:X:XPOT|XPOT]]|-2.66|<0.01| |[[:human_genes:S:SMPD4|SMPD4]]|-2.65|<0.01| |[[:human_genes:D:DNAJB11|DNAJB11]]|-2.64|0.01| |[[:human_genes:D:DNAJB2|DNAJB2]]|2.27|0.36| |[[:human_genes:M:MTMR9|MTMR9]]|2.27|0.11| |[[:human_genes:R:RELB|RELB]]|2.31|0.10| |[[:human_genes:I:ITSN1|ITSN1]]|2.32|0.05| |[[:human_genes:X:XBP1|XBP1]]|2.35|0.04| |[[:human_genes:R:RBBP5|RBBP5]]|2.41|0.03| |[[:human_genes:S:SLC30A7|SLC30A7]]|2.42|0.06| |[[:human_genes:G:GAGE2A|GAGE2A]]|2.44|0.52| |[[:human_genes:S:SF3B3|SF3B3]]|2.45|0.19| |[[:human_genes:U:UBE3D|UBE3D]]|2.46|0.03| |[[:human_genes:S:SLC30A5|SLC30A5]]|2.53|0.02| |[[:human_genes:H:HNRNPU|HNRNPU]]|2.53|0.02| |[[:human_genes:E:EIF2AK3|EIF2AK3]]|2.57|0.02| |[[:human_genes:A:ANKHD1-EIF4EBP3|ANKHD1-EIF4EBP3]]|2.60|0.03| |[[:human_genes:R:RAB2A|RAB2A]]|2.61|0.03| |[[:human_genes:A:ANKRD17|ANKRD17]]|2.63|0.03| |[[:human_genes:P:PRPF18|PRPF18]]|2.66|0.19| |[[:human_genes:M:MTMR6|MTMR6]]|2.79|0.03| |[[:human_genes:A:AHCYL1|AHCYL1]]|2.80|0.02| |[[:human_genes:K:KDELR2|KDELR2]]|3.19|<0.01| |[[:human_genes:G:GALNT2|GALNT2]]|3.84|<0.01| |[[:human_genes:E:ERP44|ERP44]]|3.87|<0.01| |[[:human_genes:E:ERGIC1|ERGIC1]]|4.03|<0.01| |[[:human_genes:S:SEC31A|SEC31A]]|4.24|<0.01| |[[:human_genes:S:SAR1A|SAR1A]]|4.26|<0.01| |[[:human_genes:A:ARFGAP1|ARFGAP1]]|4.34|<0.01| |[[:human_genes:A:ARF5|ARF5]]|4.48|<0.01| |[[:human_genes:S:SEC23B|SEC23B]]|4.55|<0.01| |[[:human_genes:S:SLC30A6|SLC30A6]]|4.66|<0.01| |[[:human_genes:A:ARF4|ARF4]]|5.33|<0.01| </modal> <modal id="modal_screen_similarity" size="lg" title="Correlated Screens"> ^Screen^Correlation^Plot^ |[[:results:exp6|Bortezomib 0.005μM R00 exp6]]|0.058|<button type="primary" size="small" modal="1">View</button>| |[[:results:exp180|Dynasore 10μM R04 exp180]]|0.057|<button type="primary" size="small" modal="2">View</button>| </modal> <modal id="1" size="lg" title="Bortezomib 0.005μM R00 exp6 vs Golgicide-A 4μM R03 exp122"> {{:chemogenomics:comparison_plots:exp122_vs_exp6.png?nolink |}} </modal> <modal id="2" size="lg" title="Dynasore 10μM R04 exp180 vs Golgicide-A 4μM R03 exp122"> {{:chemogenomics:comparison_plots:exp122_vs_exp180.png?nolink |}} </modal> <modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms"> ^GO Term^Fold Change^Genes^ |negative regulation of TORC1 signaling|59.91|NPRL3,SZT2,PRKAA1,ITFG2| |negative regulation of TOR signaling|37.21|NPRL3,SZT2,PRKAA1,ITFG2| </modal> <modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms"> ^GO Term^Fold Change^Genes^ |zinc ion import into Golgi lumen|552.63|SLC30A5,SLC30A7| |cytosol to Golgi apparatus transport|368.42|SLC30A5,SLC30A7| |zinc ion import into organelle|207.24|SLC30A6,SLC30A5,SLC30A7| |COPII-coated vesicle cargo loading|118.42|SEC23B,SAR1A,SEC31A| |zinc ion transmembrane transporter activity|72.08|SLC30A6,SLC30A5,SLC30A7| |zinc ion transmembrane transport|63.77|SLC30A6,SLC30A5,SLC30A7| |zinc ion transport|61.40|SLC30A6,SLC30A5,SLC30A7| |vesicle cargo loading|53.48|SEC23B,SAR1A,SEC31A| |endoplasmic reticulum exit site|53.48|SEC23B,SAR1A,SEC31A| |retrograde vesicle-mediated transport, Golgi to endoplasmic reticulum|46.05|ARF4,ARF5,ERGIC1,KDELR2| |ER to Golgi transport vesicle membrane|37.47|SEC23B,SAR1A,SEC31A,SLC30A5| |COPII-coated ER to Golgi transport vesicle|37.26|SEC23B,SAR1A,SEC31A,ERGIC1,SLC30A5,CNIH4| |endoplasmic reticulum to Golgi vesicle-mediated transport|35.37|ARF4,SEC23B,SAR1A,SEC31A,ERGIC1,KDELR2,RAB2A,CNIH4| |endoplasmic reticulum-Golgi intermediate compartment|21.59|ERGIC1,ERP44,MTMR6,RAB2A,CNIH4| |Golgi vesicle transport|18.09|ARF4,SEC23B,ARF5,SAR1A,SEC31A,ERGIC1,KDELR2,RAB2A,CNIH4| |coated vesicle membrane|14.32|SEC23B,SAR1A,SEC31A,KDELR2,SLC30A5| |coated vesicle|12.77|SEC23B,SAR1A,SEC31A,ERGIC1,KDELR2,SLC30A5,CNIH4| |Golgi membrane|6.74|ARF4,ARFGAP1,ERGIC1,GALNT2,KDELR2,RAB2A,SLC30A5,SLC30A7| |perinuclear region of cytoplasm|6.17|SEC23B,ARF5,SEC31A,GALNT2,MTMR6,EIF2AK3,SLC30A7,MTMR9| </modal> Last modified: 2026/01/15 21:36by 127.0.0.1