====== 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 |}}
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^ 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 |
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==== 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)