====== SB202190 10μM R03 exp148 ====== ==== Mechanism of Action ==== Inhibits p38‘± (MAPK14)and p38‘_ (MAPK11) kinase, ATP competitive * **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole%% * **Synonyms:** N/A * **CAS #:** 152121-30-7 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/5169|5169]] * **IUPAC:** %%4-[4-(4-fluorophenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]phenol%% * **INCHI Name:** InChI=1S/C20H14FN3O/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(25)8-4-15/h1-12,25H,(H,23,24) * **INCHI Key:** QHKYPYXTTXKZST-UHFFFAOYSA-N * **Molecular Weight:** 331.3 * **Canonical SMILES:** C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)O * **Isomeric SMILES:** N/A * **Molecular Formula:** C20H14FN3O {{:chemogenomics:structures:chem-0099.svg?nolink}} * **Supplier Name:** Selleck Chemicals * **Catalog #:** S1077 * **Lot #:** 01 * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C20H14FN3O 332.11937; found 332.11933 * **Platform ID:** SB202190 * **Min:** 4.3648; **Max:** 53.7816 {{:chemogenomics:dose_response:dr_119.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |2.7330 | | IC30 |7.9975 | | IC40 |19.2844 | | IC50 |43.2506 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 03 * **Dose**: 10µM * **Days of incubation**: 8 * **Doublings**: 6.9 * **Numbers of reads**: 10145836 ==== 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^ |2/0|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/SB202190_10uM_Round-3_exp148.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp148.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:S:SLC5A3|SLC5A3]]|-3.94|<0.01| |[[:human_genes:K:KDSR|KDSR]]|-3.66|<0.01| |[[:human_genes:Q:QARS|QARS]]|-2.85|0.32| |[[:human_genes:G:GPR107|GPR107]]|-2.54|0.10| |[[:human_genes:E:ETV3|ETV3]]|-2.47|0.18| |[[:human_genes:H:HMBS|HMBS]]|-2.38|0.18| |[[:human_genes:R:RGP1|RGP1]]|-2.36|0.27| |[[:human_genes:K:KCNK13|KCNK13]]|-2.33|0.18| |[[:human_genes:E:EXTL1|EXTL1]]|-2.30|0.49| |[[:human_genes:A:ALAD|ALAD]]|-2.30|0.21| |[[:human_genes:S:SUCLA2|SUCLA2]]|-2.26|0.18| |[[:human_genes:C:CNTNAP5|CNTNAP5]]|-2.26|0.18| |[[:human_genes:R:RABGGTB|RABGGTB]]|-2.25|0.25| |[[:human_genes:T:TMEM186|TMEM186]]|-2.25|0.18| |[[:human_genes:S:SLC47A1|SLC47A1]]|-2.24|0.18| |[[:human_genes:M:MOCS3|MOCS3]]|-2.24|0.31| |[[:human_genes:S:SLC38A1|SLC38A1]]|-2.20|0.20| |[[:human_genes:K:KIAA1432|KIAA1432]]|-2.16|0.21| |[[:human_genes:A:ANKRD36B|ANKRD36B]]|-2.12|0.30| |[[:human_genes:R:RUNDC1|RUNDC1]]|-2.08|0.27| |[[:human_genes:A:ATP5H|ATP5H]]|-2.07|0.27| |[[:human_genes:P:PGGT1B|PGGT1B]]|-2.06|0.28| |[[:human_genes:F:FECH|FECH]]|-2.04|0.29| |[[:human_genes:N:NUDT22|NUDT22]]|-2.02|0.46| |[[:human_genes:W:WDR20|WDR20]]|-2.02|0.30| |[[:human_genes:S:SAFB|SAFB]]|-2.01|0.35| |[[:human_genes:Z:ZDHHC23|ZDHHC23]]|-2.01|0.30| |[[:human_genes:C:CCDC47|CCDC47]]|-2.01|0.30| |[[:human_genes:C:C6orf118|C6orf118]]|-2.00|0.54| |[[:human_genes:P:PABPC1L|PABPC1L]]|-2.00|0.46| |[[:human_genes:P:PFN2|PFN2]]|1.92|0.56| |[[:human_genes:Z:ZNF791|ZNF791]]|1.92|0.56| |[[:human_genes:N:NUP133|NUP133]]|1.92|0.56| |[[:human_genes:A:ASH1L|ASH1L]]|1.93|0.56| |[[:human_genes:T:TIMM44|TIMM44]]|1.94|0.63| |[[:human_genes:C:CLEC1B|CLEC1B]]|1.95|0.56| |[[:human_genes:R:RGL3|RGL3]]|1.96|0.56| |[[:human_genes:A:ATRX|ATRX]]|1.97|0.56| |[[:human_genes:G:GLTSCR2|GLTSCR2]]|1.99|0.64| |[[:human_genes:T:TCERG1|TCERG1]]|2.00|0.60| |[[:human_genes:P:PES1|PES1]]|2.01|0.63| |[[:human_genes:T:TRIM49B|TRIM49B]]|2.02|0.56| |[[:human_genes:A:ANKRD55|ANKRD55]]|2.03|0.56| |[[:human_genes:P:PSMB7|PSMB7]]|2.03|0.56| |[[:human_genes:C:CNOT4|CNOT4]]|2.03|0.50| |[[:human_genes:A:ARRDC3|ARRDC3]]|2.05|0.56| |[[:human_genes:M:MIA2|MIA2]]|2.09|0.50| |[[:human_genes:W:WNT5A|WNT5A]]|2.11|0.50| |[[:human_genes:I:IPPK|IPPK]]|2.13|0.50| |[[:human_genes:E:ERG|ERG]]|2.14|0.50| |[[:human_genes:G:GGA3|GGA3]]|2.16|0.50| |[[:human_genes:T:TMEM232|TMEM232]]|2.21|0.50| |[[:human_genes:A:APBA1|APBA1]]|2.27|0.50| |[[:human_genes:F:FDPS|FDPS]]|2.29|0.50| |[[:human_genes:M:MMP15|MMP15]]|2.29|0.45| |[[:human_genes:S:SUGT1|SUGT1]]|2.29|0.56| |[[:human_genes:I:IDE|IDE]]|2.34|0.50| |[[:human_genes:N:NOP16|NOP16]]|2.39|0.74| |[[:human_genes:R:RPS23|RPS23]]|2.44|0.28| |[[:human_genes:M:MAPK1|MAPK1]]|2.49|0.28| ^Screen^Correlation^Plot^ |[[:results:exp149|SB203580 25μM R03 exp149]]|0.054|| {{:chemogenomics:comparison_plots:exp148_vs_exp149.png?nolink |}} ^GO Term^Fold Change^Genes^ |protein geranylgeranyltransferase activity|318.83|RABGGTB,PGGT1B| |protein geranylgeranylation|255.06|RABGGTB,PGGT1B| |protoporphyrinogen IX metabolic process|191.30|HMBS,ALAD,FECH| |porphyrin-containing compound biosynthetic process|91.09|HMBS,ALAD,SUCLA2,FECH| |tetrapyrrole biosynthetic process|91.09|HMBS,ALAD,SUCLA2,FECH| |heme biosynthetic process|76.52|HMBS,ALAD,FECH| |porphyrin-containing compound metabolic process|55.45|HMBS,ALAD,SUCLA2,FECH| |tetrapyrrole metabolic process|47.23|HMBS,ALAD,SUCLA2,FECH| No GO term hits below threshold. (FDR <0.05)