====== SB203580 25μM R03 exp149 ======
==== Mechanism of Action ====
p38 MAP kinase inhibitor
* **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor
* **Class / Subclass 2:** Proteostasis / Autophagy Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole%%
* **Synonyms:** RWJ 64809
* **CAS #:** 152121-47-6
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/176155|176155]]
* **IUPAC:** %%4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine%%
* **INCHI Name:** InChI=1S/C21H16FN3OS/c1-27(26)18-8-4-16(5-9-18)21-24-19(14-2-6-17(22)7-3-14)20(25-21)15-10-12-23-13-11-15/h2-13H,1H3,(H,24,25)
* **INCHI Key:** CDMGBJANTYXAIV-UHFFFAOYSA-N
* **Molecular Weight:** 377.4
* **Canonical SMILES:** CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F
* **Isomeric SMILES:** N/A
* **Molecular Formula:** C21H16FN3OS
{{:chemogenomics:structures:chem-0100.svg?nolink}}
* **Supplier Name:** Selleck Chemicals
* **Catalog #:** S1076
* **Lot #:** 08
* **LCMS:** Tr 1.10 min, m/z 378+ [M+H]+, 376- [M-H]-
* **Platform ID:** SB203580
* **Min:** -0.3115; **Max:** 90.3000
{{:chemogenomics:dose_response:dr_120.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |19.1742 |
| IC30 |22.4861 |
| IC40 |25.6234 |
| IC50 |28.8863 |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 03
* **Dose**: 25µM
* **Days of incubation**: 8
* **Doublings**: 7.1
* **Numbers of reads**: 11544089
==== 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|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/SB203580_25uM_Round-3_exp149.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp149.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:K:KDSR|KDSR]]|-4.78|<0.01|
|[[:human_genes:S:SLC5A3|SLC5A3]]|-4.21|<0.01|
|[[:human_genes:V:VPS25|VPS25]]|-3.77|0.01|
|[[:human_genes:F:FLVCR1|FLVCR1]]|-3.30|<0.01|
|[[:human_genes:P:PGGT1B|PGGT1B]]|-2.58|0.05|
|[[:human_genes:G:GPR107|GPR107]]|-2.56|0.05|
|[[:human_genes:G:GNAS|GNAS]]|-2.44|0.08|
|[[:human_genes:S:SPTSSA|SPTSSA]]|-2.41|0.08|
|[[:human_genes:S:SPTLC2|SPTLC2]]|-2.38|0.09|
|[[:human_genes:S:SLC7A5|SLC7A5]]|-2.29|0.13|
|[[:human_genes:C:CEPT1|CEPT1]]|-2.22|0.18|
|[[:human_genes:A:AGGF1|AGGF1]]|-2.20|0.26|
|[[:human_genes:C:CHKA|CHKA]]|-2.18|0.20|
|[[:human_genes:G:GDF1|GDF1]]|-2.15|0.23|
|[[:human_genes:P:PCYT1A|PCYT1A]]|-2.11|0.26|
|[[:human_genes:S:SLC52A2|SLC52A2]]|-2.10|0.26|
|[[:human_genes:K:KCNN1|KCNN1]]|-2.10|0.58|
|[[:human_genes:I:ITGA5|ITGA5]]|-2.07|0.26|
|[[:human_genes:K:KIAA1432|KIAA1432]]|-2.07|0.26|
|[[:human_genes:C:CDIPT|CDIPT]]|-2.06|0.77|
|[[:human_genes:P:PLAA|PLAA]]|-2.01|0.35|
|[[:human_genes:H:HIST1H2AK|HIST1H2AK]]|-1.96|0.43|
|[[:human_genes:G:GFM1|GFM1]]|-1.91|0.71|
|[[:human_genes:P:PCDHB10|PCDHB10]]|-1.90|0.63|
|[[:human_genes:A:ATP7B|ATP7B]]|-1.90|0.54|
|[[:human_genes:C:CDC14A|CDC14A]]|-1.90|0.54|
|[[:human_genes:N:NKX6-3|NKX6-3]]|-1.88|0.57|
|[[:human_genes:R:RAF1|RAF1]]|-1.87|0.58|
|[[:human_genes:P:PABPC1L|PABPC1L]]|-1.87|0.71|
|[[:human_genes:C:CADPS|CADPS]]|-1.87|0.71|
|[[:human_genes:R:RASL10A|RASL10A]]|1.96|0.57|
|[[:human_genes:S:SESTD1|SESTD1]]|1.97|0.54|
|[[:human_genes:N:NMI|NMI]]|1.98|0.57|
|[[:human_genes:G:GFI1|GFI1]]|1.99|0.54|
|[[:human_genes:O:OR2A14|OR2A14]]|2.01|0.54|
|[[:human_genes:N:NPIPB4|NPIPB4]]|2.04|0.54|
|[[:human_genes:W:WBSCR22|WBSCR22]]|2.04|0.74|
|[[:human_genes:P:PAPSS1|PAPSS1]]|2.04|0.54|
|[[:human_genes:M:MASTL|MASTL]]|2.10|0.69|
|[[:human_genes:L:LEMD3|LEMD3]]|2.12|0.61|
|[[:human_genes:P:PLEKHA2|PLEKHA2]]|2.17|0.54|
|[[:human_genes:G:GPR87|GPR87]]|2.18|0.54|
|[[:human_genes:A:ASH1L|ASH1L]]|2.18|0.54|
|[[:human_genes:R:RPL13A|RPL13A]]|2.19|0.60|
|[[:human_genes:E:EFR3A|EFR3A]]|2.20|0.54|
|[[:human_genes:P:PAF1|PAF1]]|2.23|0.57|
|[[:human_genes:R:RAB5C|RAB5C]]|2.25|0.54|
|[[:human_genes:F:FLJ45513|FLJ45513]]|2.25|0.54|
|[[:human_genes:P:PNN|PNN]]|2.28|0.57|
|[[:human_genes:C:CBLB|CBLB]]|2.29|0.54|
|[[:human_genes:S:SUPT6H|SUPT6H]]|2.35|0.54|
|[[:human_genes:E:EIF5B|EIF5B]]|2.37|0.76|
|[[:human_genes:N:NKTR|NKTR]]|2.38|0.54|
|[[:human_genes:D:DNM2|DNM2]]|2.45|0.74|
|[[:human_genes:Z:ZNF571|ZNF571]]|2.45|0.54|
|[[:human_genes:R:RPL36A-HNRNPH2|RPL36A-HNRNPH2]]|2.45|0.74|
|[[:human_genes:N:NOP58|NOP58]]|2.46|0.54|
|[[:human_genes:N:NPIPB3|NPIPB3]]|2.48|0.65|
|[[:human_genes:Z:ZNF431|ZNF431]]|2.66|0.54|
|[[:human_genes:T:TEX10|TEX10]]|2.78|0.51|
^Screen^Correlation^Plot^
|[[:results:exp538|ZLN024 50μM R08 exp538]]|0.086||
|[[:results:exp422|Wiskostatin 3μM R07 exp422]]|0.083||
|[[:results:exp152|SGC2043 10μM R03 exp152]]|0.068||
|[[:results:exp83|Trametinib 10μM R02 exp83]]|0.062||
|[[:results:exp530|Thioridazine 5μM R08 exp530]]|0.051||
|[[:results:exp326|CCT251545 20μM R07 exp326]]|0.096||
|[[:results:exp77|Prochlorperazine 5.2μM R02 exp77]]|0.091||
|[[:results:exp358|FK-506 5μM R07 exp358]]|0.084||
|[[:results:exp47|Lapatinib 5μM R01 exp47]]|0.083||
|[[:results:exp457|Bisphenol F 50μM R08 exp457]]|0.078||
|[[:results:exp114|A-196 10μM R03 exp114]]|0.071||
|[[:results:exp164|Q15 1 to 2μM on day4 R04 exp164]]|0.07||
|[[:results:exp508|NN-Dimethylsphingosine 2.5μM R08 exp508]]|0.069||
|[[:results:exp465|Cannabidiol 13μM R08 exp465]]|0.068||
|[[:results:exp344|Chlorpromazine 10μM R07 exp344]]|0.064||
|[[:results:exp293|Myriocin 25μM R06 exp293]]|0.063||
|[[:results:exp461|BS-181 20μM R08 exp461]]|0.063||
|[[:results:exp341|BRD2 inhibitor II 20μM R07 exp341]]|0.06||
|[[:results:exp233|EPZ-5676 30μM R05 exp233]]|0.057||
|[[:results:exp169|BH1 1μM R04 exp169]]|0.055||
|[[:results:exp506|Momordin-Ic 10μM R08 exp506]]|0.054||
|[[:results:exp495|IWR1 50μM R08 exp495]]|0.054||
|[[:results:exp131|L-74142 5μM R03 exp131]]|0.054||
|[[:results:exp148|SB202190 10μM R03 exp148]]|0.054||
|[[:results:exp483|FTY720 3μM R08 exp483]]|0.052||
|[[:results:exp467|CAY10603 0.55μM R08 exp467]]|0.052||
|[[:results:exp280|Daidzin 10μM R06 exp280]]|0.051||
{{:chemogenomics:comparison_plots:exp149_vs_exp538.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp422.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp152.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp83.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp530.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp326.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp77.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp358.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp47.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp457.png?nolink |}}
{{:chemogenomics:comparison_plots:exp114_vs_exp149.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp164.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp508.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp465.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp344.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp293.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp461.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp341.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp233.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp169.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp506.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp495.png?nolink |}}
{{:chemogenomics:comparison_plots:exp131_vs_exp149.png?nolink |}}
{{:chemogenomics:comparison_plots:exp148_vs_exp149.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp483.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp467.png?nolink |}}
{{:chemogenomics:comparison_plots:exp149_vs_exp280.png?nolink |}}
^GO Term^Fold Change^Genes^
|CDP-choline pathway|296.05|CEPT1,CHKA,PCYT1A|
|sphingoid metabolic process|88.82|KDSR,SPTSSA,SPTLC2|
|phosphatidylcholine biosynthetic process|74.01|CEPT1,CHKA,PCYT1A|
No GO term hits below threshold. (FDR <0.05)