====== Hydroxychloroquine 30μM R08 exp490 ====== ==== Mechanism of Action ==== Lysosomotropic agent, prevents sequestration of heme into hemozoin, forms toxic complex with heme, also inhibits TLR 7/9 * **Class / Subclass 1:** Infectious Disease / Antimalarial * **Class / Subclass 2:** DNA Damage, Repair and Replication / Intercalating Agent * **Class / Subclass 3:** Proteostasis / Autophagy Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%Hydroxychloroquine sulfate%% * **Synonyms:** HCQ sulfate * **CAS #:** 747-36-4 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/12947|12947]] * **IUPAC:** %%2-[4-[(7-chloroquinolin-4-yl)amino]pentyl-ethylamino]ethanol;sulfuric acid%% * **INCHI Name:** InChI=1S/C18H26ClN3O.H2O4S/c1-3-22(11-12-23)10-4-5-14(2)21-17-8-9-20-18-13-15(19)6-7-16(17)18;1-5(2,3)4/h6-9,13-14,23H,3-5,10-12H2,1-2H3,(H,20,21);(H2,1,2,3,4) * **INCHI Key:** JCBIVZZPXRZKTI-UHFFFAOYSA-N * **Molecular Weight:** 434 * **Canonical SMILES:** CCN(CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl)CCO.OS(=O)(=O)O * **Isomeric SMILES:** N/A * **Molecular Formula:** C18H28ClN3O5S {{:chemogenomics:structures:chem-0298.svg?nolink}} * **Supplier Name:** Combi-Blocks * **Catalog #:** QA-8047 * **Lot #:** B11244 Characterization data not available. * **Platform ID:** Hydroxychloroquine * **Min:** -11.2129; **Max:** 98.9777 {{:chemogenomics:dose_response:dr_545.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |18.4900 | | IC20 |24.0900 | | IC30 |28.7200 | | IC40 |33.1700 | | IC50 |37.8700 | | IC60 |43.2200 | | IC70 |49.9200 | | IC80 |59.5200 | | IC90 |77.5500 | \\ ==== Screen Summary ==== * **Round**: 08 * **Dose**: 30µM * **Days of incubation**: 8 * **Doublings**: 6.2 * **Numbers of reads**: 16492093 ==== 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^ |9/0|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Hydroxychloroquine_30uM_Round-8_exp490.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp490.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:O:ODC1|ODC1]]|-4.41|<0.01| |[[:human_genes:F:FLVCR1|FLVCR1]]|-3.20|<0.01| |[[:human_genes:K:KAT7|KAT7]]|-3.02|<0.01| |[[:human_genes:W:WDR81|WDR81]]|-2.94|0.01| |[[:human_genes:R:RAB7A|RAB7A]]|-2.88|<0.01| |[[:human_genes:S:SLC5A3|SLC5A3]]|-2.61|0.03| |[[:human_genes:U:UBA3|UBA3]]|-2.59|0.09| |[[:human_genes:A:ARL1|ARL1]]|-2.51|0.05| |[[:human_genes:S:SLC25A1|SLC25A1]]|-2.49|0.05| |[[:human_genes:C:CDIPT|CDIPT]]|-2.47|0.21| |[[:human_genes:A:ADIPOR2|ADIPOR2]]|-2.46|0.05| |[[:human_genes:S:SLC39A9|SLC39A9]]|-2.43|0.05| |[[:human_genes:M:MARCKSL1|MARCKSL1]]|-2.43|0.05| |[[:human_genes:F:FIGNL2|FIGNL2]]|-2.38|0.06| |[[:human_genes:C:COMMD10|COMMD10]]|-2.38|0.06| |[[:human_genes:U:UHRF1|UHRF1]]|-2.38|0.17| |[[:human_genes:C:CCDC22|CCDC22]]|-2.28|0.09| |[[:human_genes:M:MGA|MGA]]|-2.28|0.09| |[[:human_genes:D:DOT1L|DOT1L]]|-2.26|0.09| |[[:human_genes:C:CNOT4|CNOT4]]|-2.25|0.09| |[[:human_genes:C:COMMD5|COMMD5]]|-2.23|0.10| |[[:human_genes:B:BTN2A1|BTN2A1]]|-2.20|0.26| |[[:human_genes:P:PEX7|PEX7]]|-2.18|0.12| |[[:human_genes:A:ANO4|ANO4]]|-2.17|0.21| |[[:human_genes:C:C6orf118|C6orf118]]|-2.17|0.26| |[[:human_genes:T:TAAR5|TAAR5]]|-2.16|0.13| |[[:human_genes:F:FDPS|FDPS]]|-2.13|0.23| |[[:human_genes:A:ATP2A2|ATP2A2]]|-2.11|0.73| |[[:human_genes:T:TMEM189|TMEM189]]|-2.11|0.17| |[[:human_genes:P:PROL1|PROL1]]|-2.07|0.19| |[[:human_genes:C:CDC40|CDC40]]|1.91|0.55| |[[:human_genes:A:ANKK1|ANKK1]]|1.92|0.55| |[[:human_genes:R:RCC1|RCC1]]|1.93|0.79| |[[:human_genes:M:MTHFD2|MTHFD2]]|1.94|0.55| |[[:human_genes:T:TAC4|TAC4]]|1.95|0.55| |[[:human_genes:U:USP39|USP39]]|1.95|0.79| |[[:human_genes:S:SURF1|SURF1]]|1.96|0.55| |[[:human_genes:D:DAGLA|DAGLA]]|1.96|0.55| |[[:human_genes:F:FRS2|FRS2]]|1.96|0.55| |[[:human_genes:T:TRIM44|TRIM44]]|1.99|0.55| |[[:human_genes:C:CCDC9|CCDC9]]|2.00|0.55| |[[:human_genes:T:TCEAL5|TCEAL5]]|2.01|0.55| |[[:human_genes:E:EXTL1|EXTL1]]|2.03|0.55| |[[:human_genes:F:FAM9B|FAM9B]]|2.04|0.55| |[[:human_genes:S:SREBF2|SREBF2]]|2.05|0.69| |[[:human_genes:N:NPRL2|NPRL2]]|2.06|0.55| |[[:human_genes:S:SHMT2|SHMT2]]|2.07|0.55| |[[:human_genes:I:ISY1|ISY1]]|2.10|0.71| |[[:human_genes:T:TMEM63C|TMEM63C]]|2.12|0.43| |[[:human_genes:N:NID1|NID1]]|2.14|0.43| |[[:human_genes:C:CPA2|CPA2]]|2.15|0.43| |[[:human_genes:N:NDUFA13|NDUFA13]]|2.17|0.55| |[[:human_genes:N:NEK3|NEK3]]|2.17|0.43| |[[:human_genes:S:SEC13|SEC13]]|2.18|0.69| |[[:human_genes:C:CSNK2A1|CSNK2A1]]|2.22|0.43| |[[:human_genes:P:PTGIS|PTGIS]]|2.24|0.43| |[[:human_genes:Z:ZNF91|ZNF91]]|2.27|0.43| |[[:human_genes:E:EIF2S1|EIF2S1]]|2.52|0.77| |[[:human_genes:G:GTPBP4|GTPBP4]]|2.57|0.43| |[[:human_genes:M:MAT2B|MAT2B]]|2.60|0.22| ^Screen^Correlation^Plot^ |[[:results:exp530|Thioridazine 5μM R08 exp530]]|0.096|| |[[:results:exp508|NN-Dimethylsphingosine 2.5μM R08 exp508]]|0.095|| |[[:results:exp77|Prochlorperazine 5.2μM R02 exp77]]|0.069|| |[[:results:exp470|Chloroquine 32μM R08 exp470]]|0.098|| |[[:results:exp483|FTY720 3μM R08 exp483]]|0.082|| |[[:results:exp453|B02 10μM R08 exp453]]|0.063|| |[[:results:exp465|Cannabidiol 13μM R08 exp465]]|0.061|| |[[:results:exp457|Bisphenol F 50μM R08 exp457]]|0.059|| |[[:results:exp454|Bafilomycin-A1 0.009μM R08 exp454]]|0.053|| |[[:results:exp452|Azithromycin 100μM R08 exp452]]|0.052|| {{:chemogenomics:comparison_plots:exp490_vs_exp530.png?nolink |}} {{:chemogenomics:comparison_plots:exp490_vs_exp508.png?nolink |}} {{:chemogenomics:comparison_plots:exp490_vs_exp77.png?nolink |}} {{:chemogenomics:comparison_plots:exp470_vs_exp490.png?nolink |}} {{:chemogenomics:comparison_plots:exp483_vs_exp490.png?nolink |}} {{:chemogenomics:comparison_plots:exp453_vs_exp490.png?nolink |}} {{:chemogenomics:comparison_plots:exp465_vs_exp490.png?nolink |}} {{:chemogenomics:comparison_plots:exp457_vs_exp490.png?nolink |}} {{:chemogenomics:comparison_plots:exp454_vs_exp490.png?nolink |}} {{:chemogenomics:comparison_plots:exp452_vs_exp490.png?nolink |}} No GO term hits below threshold. (FDR <0.05) No GO term hits below threshold. (FDR <0.05)