====== ETC-159 50μM R08 exp480 ====== ==== Mechanism of Action ==== Inhibits PORCN palmitoyl transferase that modifies WNT ligands * **Class / Subclass 1:** Signal Transduction / Other Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%Etc-159%% * **Synonyms:** ETC-1922159 * **CAS #:** 1638250-96-0 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/86280523|86280523]] * **IUPAC:** %%2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide%% * **INCHI Name:** InChI=1S/C19H17N7O3/c1-24-17-16(18(28)25(2)19(24)29)26(11-20-17)10-15(27)21-14-9-8-13(22-23-14)12-6-4-3-5-7-12/h3-9,11H,10H2,1-2H3,(H,21,23,27) * **INCHI Key:** QTRXIFVSTWXRJJ-UHFFFAOYSA-N * **Molecular Weight:** 391.4 * **Canonical SMILES:** CN1C2=C(C(=O)N(C1=O)C)N(C=N2)CC(=O)NC3=NN=C(C=C3)C4=CC=CC=C4 * **Isomeric SMILES:** N/A * **Molecular Formula:** C19H17N7O3 {{:chemogenomics:structures:chem-0289.svg?nolink}} * **Supplier Name:** Med Chem Express * **Catalog #:** HY-18988 * **Lot #:** 18685 * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C19H17N7O3 392.14656; found 392.14729 * **Platform ID:** ETC159 * **Min:** -27.6061; **Max:** 13.1023 {{:chemogenomics:dose_response:dr_533.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |N/A | | IC30 |N/A | | IC40 |N/A | | IC50 |N/A | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 08 * **Dose**: 50µM * **Days of incubation**: 8 * **Doublings**: 5.3 * **Numbers of reads**: 16937241 ==== 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^ |12/3|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/ETC-159_50uM_Round-8_exp480.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp480.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:L:LCMT1|LCMT1]]|-3.93|<0.01| |[[:human_genes:G:GPR107|GPR107]]|-3.92|<0.01| |[[:human_genes:A:ARL1|ARL1]]|-3.56|<0.01| |[[:human_genes:P:PPME1|PPME1]]|-3.55|<0.01| |[[:human_genes:P:PPP6C|PPP6C]]|-3.52|<0.01| |[[:human_genes:S:SLC39A9|SLC39A9]]|-3.29|<0.01| |[[:human_genes:T:TCF4|TCF4]]|-3.24|<0.01| |[[:human_genes:B:BACH2|BACH2]]|-2.90|0.01| |[[:human_genes:K:KCTD5|KCTD5]]|-2.88|<0.01| |[[:human_genes:P:PGGT1B|PGGT1B]]|-2.77|<0.01| |[[:human_genes:M:MSL1|MSL1]]|-2.59|0.05| |[[:human_genes:C:CSK|CSK]]|-2.51|0.03| |[[:human_genes:C:CNOT8|CNOT8]]|-2.41|0.05| |[[:human_genes:P:PPP2CA|PPP2CA]]|-2.33|0.14| |[[:human_genes:P:PDCD6IP|PDCD6IP]]|-2.28|0.10| |[[:human_genes:D:DARS2|DARS2]]|-2.22|0.46| |[[:human_genes:A:ATP2B1|ATP2B1]]|-2.20|0.24| |[[:human_genes:R:RAPGEF3|RAPGEF3]]|-2.19|0.14| |[[:human_genes:R:RFWD2|RFWD2]]|-2.16|0.16| |[[:human_genes:A:ACTB|ACTB]]|-2.13|0.18| |[[:human_genes:D:DLD|DLD]]|-2.12|0.30| |[[:human_genes:C:CTDSPL2|CTDSPL2]]|-2.10|0.30| |[[:human_genes:Z:ZNF445|ZNF445]]|-2.09|0.31| |[[:human_genes:K:KIAA1432|KIAA1432]]|-2.06|0.32| |[[:human_genes:S:SMG9|SMG9]]|-2.05|0.35| |[[:human_genes:F:FAM134A|FAM134A]]|-2.02|0.30| |[[:human_genes:S:SS18|SS18]]|-1.99|0.30| |[[:human_genes:L:LAMTOR4|LAMTOR4]]|-1.99|0.30| |[[:human_genes:X:XPR1|XPR1]]|-1.99|0.30| |[[:human_genes:S:SRRD|SRRD]]|-1.96|0.32| |[[:human_genes:S:SLCO1B3|SLCO1B3]]|1.97|0.39| |[[:human_genes:L:LSR|LSR]]|1.98|0.62| |[[:human_genes:Z:ZSCAN22|ZSCAN22]]|1.98|0.39| |[[:human_genes:U:U2AF2|U2AF2]]|1.99|0.62| |[[:human_genes:O:OR8U8|OR8U8]]|1.99|0.72| |[[:human_genes:T:TRIM37|TRIM37]]|2.00|0.36| |[[:human_genes:N:NAT10|NAT10]]|2.01|0.62| |[[:human_genes:M:MTRNR2L4|MTRNR2L4]]|2.03|0.79| |[[:human_genes:R:RTP2|RTP2]]|2.04|0.32| |[[:human_genes:N:NSMAF|NSMAF]]|2.06|0.30| |[[:human_genes:C:C21orf2|C21orf2]]|2.08|0.29| |[[:human_genes:G:GLE1|GLE1]]|2.11|0.64| |[[:human_genes:R:RRM2|RRM2]]|2.15|0.74| |[[:human_genes:M:MS4A13|MS4A13]]|2.17|0.73| |[[:human_genes:H:HNRNPAB|HNRNPAB]]|2.18|0.20| |[[:human_genes:S:SCEL|SCEL]]|2.21|0.18| |[[:human_genes:C:CUL1|CUL1]]|2.24|0.18| |[[:human_genes:B:BAZ2A|BAZ2A]]|2.25|0.26| |[[:human_genes:K:KMT2D|KMT2D]]|2.35|0.11| |[[:human_genes:U:USP37|USP37]]|2.35|0.18| |[[:human_genes:S:SLC1A6|SLC1A6]]|2.35|0.11| |[[:human_genes:A:ATP8B2|ATP8B2]]|2.39|0.26| |[[:human_genes:S:SLC7A1|SLC7A1]]|2.44|0.36| |[[:human_genes:E:ETFB|ETFB]]|2.47|0.07| |[[:human_genes:F:FDPS|FDPS]]|2.68|0.07| |[[:human_genes:N:NOP58|NOP58]]|2.71|0.10| |[[:human_genes:P:PSMB8|PSMB8]]|2.72|0.04| |[[:human_genes:S:SRM|SRM]]|2.83|0.03| |[[:human_genes:N:NUMA1|NUMA1]]|2.94|0.06| |[[:human_genes:P:PCGF1|PCGF1]]|3.10|<0.01| ^Screen^Correlation^Plot^ |[[:results:exp190|Vincristine 0.0005μM R04 exp190]]|0.057|| |[[:results:exp269|Bisphenol A 100μM R06 exp269]]|0.061|| |[[:results:exp233|EPZ-5676 30μM R05 exp233]]|0.055|| |[[:results:exp455|Benzoate 10000μM R08 exp455]]|0.051|| {{:chemogenomics:comparison_plots:exp190_vs_exp480.png?nolink |}} {{:chemogenomics:comparison_plots:exp269_vs_exp480.png?nolink |}} {{:chemogenomics:comparison_plots:exp233_vs_exp480.png?nolink |}} {{:chemogenomics:comparison_plots:exp455_vs_exp480.png?nolink |}} No GO term hits below threshold. (FDR <0.05) No GO term hits below threshold. (FDR <0.05)