====== Amiloride 100μM R08 exp447 ====== ==== Mechanism of Action ==== Inhibits epithelial sodium channel (ENaC) and other Na+/H+ channels, also inhibits urokinase-type plasminogen activator (uPA) * **Class / Subclass 1:** Signal Transduction / Ion Channel Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%Amiloride hydrochloride%% * **Synonyms:** MK-870 hydrochloride * **CAS #:** 2016-88-8 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/16230|16230]] * **IUPAC:** %%3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide;hydrochloride%% * **INCHI Name:** InChI=1S/C6H8ClN7O.ClH/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11;/h(H4,8,9,13)(H4,10,11,14,15);1H * **INCHI Key:** ACHKKGDWZVCSNH-UHFFFAOYSA-N * **Molecular Weight:** 266.09 * **Canonical SMILES:** C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.Cl * **Isomeric SMILES:** N/A * **Molecular Formula:** C6H9Cl2N7O {{:chemogenomics:structures:chem-0258.svg?nolink}} * **Supplier Name:** Med Chem Express * **Catalog #:** HY-B0285A * **Lot #:** 14566 * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C6H8ClN7O 230.05516; found 230.05522 * **Platform ID:** Amiloride * **Min:** -0.7865; **Max:** 67.7240 {{:chemogenomics:dose_response:dr_496.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |3.7720 | | IC20 |16.2300 | | IC30 |42.8000 | | IC40 |94.7900 | | IC50 |196.6000 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 08 * **Dose**: 100µM * **Days of incubation**: 8 * **Doublings**: 2.5 * **Numbers of reads**: 18416066 ==== 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^ |10/36|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Amiloride_100uM_Round-8_exp447.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp447.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:A:ABCC4|ABCC4]]|-5.44|<0.01| |[[:human_genes:V:VPS25|VPS25]]|-3.16|0.17| |[[:human_genes:T:TSSC1|TSSC1]]|-3.11|<0.01| |[[:human_genes:P:PRKAA1|PRKAA1]]|-3.08|<0.01| |[[:human_genes:M:MTF2|MTF2]]|-3.05|<0.01| |[[:human_genes:G:GOT1|GOT1]]|-2.83|<0.01| |[[:human_genes:R:RIC8A|RIC8A]]|-2.76|0.01| |[[:human_genes:Q:QRICH1|QRICH1]]|-2.72|0.01| |[[:human_genes:T:TCF4|TCF4]]|-2.70|0.01| |[[:human_genes:P:PIK3CA|PIK3CA]]|-2.55|0.03| |[[:human_genes:F:FDPS|FDPS]]|-2.51|0.07| |[[:human_genes:S:SEPHS1|SEPHS1]]|-2.47|0.04| |[[:human_genes:Z:ZSCAN12|ZSCAN12]]|-2.38|0.32| |[[:human_genes:M:MSI2|MSI2]]|-2.38|0.07| |[[:human_genes:G:GPR101|GPR101]]|-2.32|0.09| |[[:human_genes:E:ESPL1|ESPL1]]|-2.31|0.30| |[[:human_genes:P:PRKAG1|PRKAG1]]|-2.30|0.16| |[[:human_genes:O:OR10G3|OR10G3]]|-2.27|0.22| |[[:human_genes:D:DCUN1D1|DCUN1D1]]|-2.24|0.13| |[[:human_genes:L:LACC1|LACC1]]|-2.21|0.14| |[[:human_genes:P:PTPN6|PTPN6]]|-2.21|0.14| |[[:human_genes:N:NNT|NNT]]|-2.17|0.22| |[[:human_genes:G:GOLGA8H|GOLGA8H]]|-2.16|0.49| |[[:human_genes:P:PRAMEF6|PRAMEF6]]|-2.16|0.16| |[[:human_genes:U:UROD|UROD]]|-2.15|0.33| |[[:human_genes:S:SIK2|SIK2]]|-2.15|0.22| |[[:human_genes:T:TNIK|TNIK]]|-2.14|0.22| |[[:human_genes:A:ACACA|ACACA]]|-2.14|0.22| |[[:human_genes:N:NLRX1|NLRX1]]|-2.13|0.22| |[[:human_genes:U:UBR4|UBR4]]|-2.13|0.30| |[[:human_genes:P:PPP3CA|PPP3CA]]|2.41|0.03| |[[:human_genes:P:PPA1|PPA1]]|2.43|0.04| |[[:human_genes:N:NARS2|NARS2]]|2.45|0.02| |[[:human_genes:P:PTAR1|PTAR1]]|2.46|0.04| |[[:human_genes:M:MBNL1|MBNL1]]|2.46|0.02| |[[:human_genes:U:UBE2G2|UBE2G2]]|2.48|0.04| |[[:human_genes:A:AGPAT1|AGPAT1]]|2.48|0.06| |[[:human_genes:C:CHKA|CHKA]]|2.49|0.02| |[[:human_genes:Z:ZBTB18|ZBTB18]]|2.54|0.02| |[[:human_genes:S:SHMT2|SHMT2]]|2.56|0.04| |[[:human_genes:T:TRMT61A|TRMT61A]]|2.57|0.04| |[[:human_genes:H:HNRNPH1|HNRNPH1]]|2.58|0.02| |[[:human_genes:N:NDUFAF7|NDUFAF7]]|2.58|0.02| |[[:human_genes:W:WDR66|WDR66]]|2.58|0.07| |[[:human_genes:N:NFRKB|NFRKB]]|2.62|0.01| |[[:human_genes:S:SLC7A1|SLC7A1]]|2.64|0.06| |[[:human_genes:S:STARD7|STARD7]]|2.68|0.02| |[[:human_genes:A:ADIPOR1|ADIPOR1]]|2.72|<0.01| |[[:human_genes:C:CTDSP1|CTDSP1]]|2.87|<0.01| |[[:human_genes:R:RAF1|RAF1]]|2.93|<0.01| |[[:human_genes:W:WDR20|WDR20]]|2.97|<0.01| |[[:human_genes:B:BEND3|BEND3]]|3.00|<0.01| |[[:human_genes:L:LRRC63|LRRC63]]|3.01|0.18| |[[:human_genes:R:RHOH|RHOH]]|3.05|<0.01| |[[:human_genes:E:EIF4A1|EIF4A1]]|3.06|<0.01| |[[:human_genes:S:SLC25A51|SLC25A51]]|3.35|<0.01| |[[:human_genes:P:PIK3CD|PIK3CD]]|3.42|<0.01| |[[:human_genes:A:ACSL4|ACSL4]]|4.00|<0.01| |[[:human_genes:M:MDH1|MDH1]]|4.54|<0.01| |[[:human_genes:S:SLC43A3|SLC43A3]]|7.16|<0.01| ^Screen^Correlation^Plot^ |[[:results:exp439|QNZ 0.01μM R08 exp439]]|0.093|| |[[:results:exp431|Rotenone 0.07μM R08 exp431]]|0.085|| |[[:results:exp445|∆-9-Tetrahydrocannabinol 30μM R08 exp445]]|0.079|| |[[:results:exp513|ONC212 0.15μM R08 exp513]]|0.073|| |[[:results:exp21|MLN-4924 0.2μM R00 exp21]]|0.07|| |[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.066|| |[[:results:exp492|iCRT14 30μM R08 exp492]]|0.066|| |[[:results:exp212|Phenformin 20μM R05 exp212]]|0.063|| |[[:results:exp440|Aphidicolin 0.4μM R08 exp440]]|0.062|| |[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.06|| |[[:results:exp134|MS023 2μM R03 exp134]]|0.06|| |[[:results:exp529|Thimerosal 0.85μM R08 exp529]]|0.06|| |[[:results:exp499|LY2090314 0.003μM R08 exp499]]|0.059|| |[[:results:exp535|Trimetrexate 0.03μM R08 exp535]]|0.057|| |[[:results:exp48|Mubritinib 0.2μM R01 exp48]]|0.057|| |[[:results:exp274|Citral 50μM R06 exp274]]|0.056|| |[[:results:exp359|FK-506 30μM R07 exp359]]|0.056|| |[[:results:exp532|TIC10 10μM R08 exp532]]|0.055|| |[[:results:exp534|Trientine 500μM R08 exp534]]|0.055|| |[[:results:exp269|Bisphenol A 100μM R06 exp269]]|0.054|| |[[:results:exp275|Citral 75μM R06 exp275]]|0.053|| |[[:results:exp248|UM0131023 0.05μM R05 exp248]]|0.052|| {{:chemogenomics:comparison_plots:exp439_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp431_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp445_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp513.png?nolink |}} {{:chemogenomics:comparison_plots:exp21_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp488.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp492.png?nolink |}} {{:chemogenomics:comparison_plots:exp212_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp440_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp489.png?nolink |}} {{:chemogenomics:comparison_plots:exp134_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp529.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp499.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp535.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp48.png?nolink |}} {{:chemogenomics:comparison_plots:exp274_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp359_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp532.png?nolink |}} {{:chemogenomics:comparison_plots:exp447_vs_exp534.png?nolink |}} {{:chemogenomics:comparison_plots:exp269_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp275_vs_exp447.png?nolink |}} {{:chemogenomics:comparison_plots:exp248_vs_exp447.png?nolink |}} No GO term hits below threshold. (FDR <0.05) No GO term hits below threshold. (FDR <0.05)