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Ask your administrator if you think this is wrong. ====== L-74142 5μM R03 exp131 ====== ==== Mechanism of Action ==== DRD4 receptor antagonist * **<color #00a2e8>Class / Subclass 1:</color>** Signal Transduction / GPCR antagonist ==== Technical Notes ==== <accordion collapsed='true'> <panel title='Compound References' collapsed='true'> * **<color #00a2e8>PubChem Name:</color>** %%5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-YL)isoxazole hydrochloride%% * **<color #00a2e8>Synonyms:</color>** N/A * **<color #00a2e8>CAS #:</color>** 874882-93-6 * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/24744861|24744861]] * **<color #00a2e8>IUPAC:</color>** %%5-(4-chlorophenyl)-4-methyl-3-[1-(2-phenylethyl)piperidin-4-yl]-1,2-oxazole;hydrochloride%% * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C23H25ClN2O.ClH/c1-17-22(25-27-23(17)20-7-9-21(24)10-8-20)19-12-15-26(16-13-19)14-11-18-5-3-2-4-6-18;/h2-10,19H,11-16H2,1H3;1H * **<color #00a2e8>INCHI Key:</color>** HZRPUQURUAXOHB-UHFFFAOYSA-N * **<color #00a2e8>Molecular Weight:</color>** 417.4 * **<color #00a2e8>Canonical SMILES:</color>** CC1=C(ON=C1C2CCN(CC2)CCC3=CC=CC=C3)C4=CC=C(C=C4)Cl.Cl * **<color #00a2e8>Isomeric SMILES:</color>** N/A * **<color #00a2e8>Molecular Formula:</color>** C23H26Cl2N2O {{:chemogenomics:structures:chem-0083.svg?nolink}} </panel> <panel title='Compound Supplier' collapsed='true'> * **<color #00a2e8>Supplier Name:</color>** Tocris Bioscience * **<color #00a2e8>Catalog #:</color>** 1004 * **<color #00a2e8>Lot #:</color>** 2A/171873 </panel> <panel title='Compound Characterization' collapsed='true'> * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+H)+ Calcd for C23H25ClN2O 381.17282; found 381.17493 </panel> <panel title='Dose Response Curve' collapsed='true'> * **<color #00a2e8>Platform ID:</color>** L741742 * **<color #00a2e8>Min:</color>** -5.7324; **<color #00a2e8>Max:</color>** 58.2869 {{:chemogenomics:dose_response:dr_88.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |4.3609 | | IC30 |5.6579 | | IC40 |7.0041 | | IC50 |8.5196 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ </panel> </accordion> ==== Screen Summary ==== * **<color #00a2e8>Round</color>**: 03 * **<color #00a2e8>Dose</color>**: 5µM * **<color #00a2e8>Days of incubation</color>**: 8 * **<color #00a2e8>Doublings</color>**: 7.1 * **<color #00a2e8>Numbers of reads</color>**: 12019422 ==== 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^ |6/0|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/L-74142_5uM_Round-3_exp131.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="default" size="sm" modal="modal_go_resistant">View</button>| <modal id='ScorePlot' size='lg' title='L-74142 5μM R03 exp131'> {{:chemogenomics:cranks_plots:exp131.png?nolink}} </modal> <modal id="modal_hits" size="sm" title="Top 30 S/R Genes"> ^Gene^CRANKS Score^FDR^ |[[:human_genes:S:SLC5A3|SLC5A3]]|-3.25|<0.01| |[[:human_genes:K:KDSR|KDSR]]|-3.17|<0.01| |[[:human_genes:V:VAC14|VAC14]]|-3.00|0.02| |[[:human_genes:O:ODC1|ODC1]]|-2.77|0.02| |[[:human_genes:C:C7orf55-LUC7L2|C7orf55-LUC7L2]]|-2.62|0.06| |[[:human_genes:K:KIAA1432|KIAA1432]]|-2.61|0.04| |[[:human_genes:T:TRIP4|TRIP4]]|-2.56|0.05| |[[:human_genes:F:FIG4|FIG4]]|-2.49|0.05| |[[:human_genes:A:ATP6V1A|ATP6V1A]]|-2.49|0.32| |[[:human_genes:F:FLVCR1|FLVCR1]]|-2.43|0.06| |[[:human_genes:S:SCAP|SCAP]]|-2.42|0.06| |[[:human_genes:C:CENPA|CENPA]]|-2.41|0.12| |[[:human_genes:C:COG7|COG7]]|-2.29|0.12| |[[:human_genes:U:UNC50|UNC50]]|-2.22|0.15| |[[:human_genes:T:TRIP12|TRIP12]]|-2.20|0.16| |[[:human_genes:C:CNTNAP5|CNTNAP5]]|-2.16|0.18| |[[:human_genes:A:AVPI1|AVPI1]]|-2.15|0.18| |[[:human_genes:R:RAB1B|RAB1B]]|-2.14|0.18| |[[:human_genes:Z:ZC3H18|ZC3H18]]|-2.14|0.32| |[[:human_genes:T:TBC1D7|TBC1D7]]|-2.13|0.18| |[[:human_genes:K:KIAA1549L|KIAA1549L]]|-2.12|0.26| |[[:human_genes:P:PITPNB|PITPNB]]|-2.12|0.18| |[[:human_genes:D:DOLK|DOLK]]|-2.11|0.26| |[[:human_genes:M:MBTPS1|MBTPS1]]|-2.10|0.33| |[[:human_genes:G:GCLC|GCLC]]|-2.09|0.26| |[[:human_genes:K:KIR3DL2|KIR3DL2]]|-2.07|0.22| |[[:human_genes:M:MAP3K1|MAP3K1]]|-2.07|0.27| |[[:human_genes:S:SPTSSA|SPTSSA]]|-2.07|0.22| |[[:human_genes:S:SPTLC1|SPTLC1]]|-2.06|0.23| |[[:human_genes:S:SLC25A1|SLC25A1]]|-2.05|0.23| |[[:human_genes:T:TMSB15B|TMSB15B]]|1.93|0.86| |[[:human_genes:A:APOBEC3D|APOBEC3D]]|1.94|0.62| |[[:human_genes:N:NKAIN2|NKAIN2]]|1.94|0.50| |[[:human_genes:S:SLC1A3|SLC1A3]]|1.94|0.50| |[[:human_genes:C:CRIP1|CRIP1]]|1.95|0.50| |[[:human_genes:O:OR10X1|OR10X1]]|1.96|0.62| |[[:human_genes:T:TSNARE1|TSNARE1]]|1.97|0.50| |[[:human_genes:C:CXCL12|CXCL12]]|1.97|0.50| |[[:human_genes:R:RAB44|RAB44]]|1.98|0.50| |[[:human_genes:E:EIF3D|EIF3D]]|1.99|0.60| |[[:human_genes:G:GNL2|GNL2]]|1.99|0.60| |[[:human_genes:E:EIF5|EIF5]]|2.00|0.80| |[[:human_genes:U:USP11|USP11]]|2.01|0.50| |[[:human_genes:R:RPL36AL|RPL36AL]]|2.01|0.69| |[[:human_genes:N:NDC80|NDC80]]|2.02|0.86| |[[:human_genes:A:AGBL1|AGBL1]]|2.06|0.50| |[[:human_genes:C:CCDC73|CCDC73]]|2.11|0.47| |[[:human_genes:M:MYH7B|MYH7B]]|2.17|0.50| |[[:human_genes:N:NAA16|NAA16]]|2.19|0.44| |[[:human_genes:M:MPV17L2|MPV17L2]]|2.20|0.44| |[[:human_genes:H:HCFC1R1|HCFC1R1]]|2.20|0.47| |[[:human_genes:D:DCAF8L1|DCAF8L1]]|2.21|0.47| |[[:human_genes:V:VWA8|VWA8]]|2.22|0.44| |[[:human_genes:M:MPRIP|MPRIP]]|2.24|0.50| |[[:human_genes:C:CDC20|CDC20]]|2.31|0.69| |[[:human_genes:G:GJD4|GJD4]]|2.33|0.44| |[[:human_genes:B:BECN1|BECN1]]|2.39|0.44| |[[:human_genes:R:RPS6KA5|RPS6KA5]]|2.41|0.47| |[[:human_genes:O:OR51Q1|OR51Q1]]|2.47|0.44| |[[:human_genes:R:RARS|RARS]]|2.57|0.81| </modal> <modal id="modal_screen_similarity" size="lg" title="Correlated Screens"> ^Screen^Correlation^Plot^ |[[:results:exp538|ZLN024 50μM R08 exp538]]|0.07|<button type="primary" size="small" modal="1">View</button>| |[[:results:exp152|SGC2043 10μM R03 exp152]]|0.064|<button type="primary" size="small" modal="2">View</button>| |[[:results:exp164|Q15 1 to 2μM on day4 R04 exp164]]|0.061|<button type="primary" size="small" modal="3">View</button>| |[[:results:exp149|SB203580 25μM R03 exp149]]|0.054|<button type="primary" size="small" modal="4">View</button>| |[[:results:exp169|BH1 1μM R04 exp169]]|0.075|<button type="primary" size="small" modal="5">View</button>| |[[:results:exp461|BS-181 20μM R08 exp461]]|0.069|<button type="primary" size="small" modal="6">View</button>| |[[:results:exp182|IU1-47 25μM R04 exp182]]|0.054|<button type="primary" size="small" modal="7">View</button>| |[[:results:exp442|Ibrutinib 10μM R08 exp442]]|0.051|<button type="primary" size="small" modal="8">View</button>| |[[:results:exp344|Chlorpromazine 10μM R07 exp344]]|0.051|<button type="primary" size="small" modal="9">View</button>| </modal> <modal id="1" size="lg" title="L-74142 5μM R03 exp131 vs ZLN024 50μM R08 exp538"> {{:chemogenomics:comparison_plots:exp131_vs_exp538.png?nolink |}} </modal> <modal id="2" size="lg" title="L-74142 5μM R03 exp131 vs SGC2043 10μM R03 exp152"> {{:chemogenomics:comparison_plots:exp131_vs_exp152.png?nolink |}} </modal> <modal id="3" size="lg" title="L-74142 5μM R03 exp131 vs Q15 1 to 2μM on day4 R04 exp164"> {{:chemogenomics:comparison_plots:exp131_vs_exp164.png?nolink |}} </modal> <modal id="4" size="lg" title="L-74142 5μM R03 exp131 vs SB203580 25μM R03 exp149"> {{:chemogenomics:comparison_plots:exp131_vs_exp149.png?nolink |}} </modal> <modal id="5" size="lg" title="BH1 1μM R04 exp169 vs L-74142 5μM R03 exp131"> {{:chemogenomics:comparison_plots:exp131_vs_exp169.png?nolink |}} </modal> <modal id="6" size="lg" title="BS-181 20μM R08 exp461 vs L-74142 5μM R03 exp131"> {{:chemogenomics:comparison_plots:exp131_vs_exp461.png?nolink |}} </modal> <modal id="7" size="lg" title="IU1-47 25μM R04 exp182 vs L-74142 5μM R03 exp131"> {{:chemogenomics:comparison_plots:exp131_vs_exp182.png?nolink |}} </modal> <modal id="8" size="lg" title="Ibrutinib 10μM R08 exp442 vs L-74142 5μM R03 exp131"> {{:chemogenomics:comparison_plots:exp131_vs_exp442.png?nolink |}} </modal> <modal id="9" size="lg" title="Chlorpromazine 10μM R07 exp344 vs L-74142 5μM R03 exp131"> {{:chemogenomics:comparison_plots:exp131_vs_exp344.png?nolink |}} </modal> <modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms"> ^GO Term^Fold Change^Genes^ |sphingoid metabolic process|92.11|KDSR,SPTSSA,SPTLC1| |Golgi membrane|9.36|VAC14,RIC1,FIG4,ATP6V1A,SCAP,COG7,UNC50,RAB1B,PITPNB,MBTPS1| </modal> <modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">No GO term hits below threshold. (FDR <0.05)</modal> Last modified: 2026/01/15 21:36by 127.0.0.1