====== Losmapimod 1μM R07 exp376 ======
==== Mechanism of Action ====
Inhibits p38‘±/‘_ MAP kinases
* **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%Losmapimod%%
* **Synonyms:** GSK-AHAB; GW856553X; SB856553
* **CAS #:** 585543-15-3
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/11552706|11552706]]
* **IUPAC:** %%6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)pyridine-3-carboxamide%%
* **INCHI Name:** InChI=1S/C22H26FN3O2/c1-13-17(9-15(10-18(13)23)21(28)26-16-6-7-16)19-8-5-14(11-24-19)20(27)25-12-22(2,3)4/h5,8-11,16H,6-7,12H2,1-4H3,(H,25,27)(H,26,28)
* **INCHI Key:** KKYABQBFGDZVNQ-UHFFFAOYSA-N
* **Molecular Weight:** 383.5
* **Canonical SMILES:** CC1=C(C=C(C=C1F)C(=O)NC2CC2)C3=NC=C(C=C3)C(=O)NCC(C)(C)C
* **Isomeric SMILES:** N/A
* **Molecular Formula:** C22H26FN3O2
{{:chemogenomics:structures:chem-0223.svg?nolink}}
* **Supplier Name:** Selleck Chemicals
* **Catalog #:** S7215
* **Lot #:** S721 501
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C22H26FN3O2 384.20818; found 384.20948
* **Platform ID:** Losmapimod
* **Min:** -20.8875; **Max:** -2.4013
{{:chemogenomics:dose_response:dr_491.png?nolink&500 |}}
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^ 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 |
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==== Screen Summary ====
* **Round**: 07
* **Dose**: 1µM
* **Days of incubation**: 8
* **Doublings**: 7.1
* **Numbers of reads**: 22591304
==== 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^
|0/0|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Losmapimod_1uM_Round-7_exp376.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp376.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:V:VPS25|VPS25]]|-3.16|0.20|
|[[:human_genes:V:VEZT|VEZT]]|-2.67|0.10|
|[[:human_genes:A:ACTC1|ACTC1]]|-2.53|0.10|
|[[:human_genes:C:CRYBA2|CRYBA2]]|-2.53|0.10|
|[[:human_genes:O:ORC3|ORC3]]|-2.29|0.68|
|[[:human_genes:S:ST6GALNAC6|ST6GALNAC6]]|-2.21|0.41|
|[[:human_genes:V:VPS53|VPS53]]|-2.20|0.68|
|[[:human_genes:Z:ZNF681|ZNF681]]|-2.18|0.68|
|[[:human_genes:R:RSRC2|RSRC2]]|-2.15|0.78|
|[[:human_genes:P:PGGT1B|PGGT1B]]|-2.09|0.68|
|[[:human_genes:A:ADNP|ADNP]]|-2.05|0.68|
|[[:human_genes:C:CLMN|CLMN]]|-2.04|0.68|
|[[:human_genes:A:ASB3|ASB3]]|-2.04|0.68|
|[[:human_genes:B:BRIP1|BRIP1]]|-2.02|0.68|
|[[:human_genes:U:UBE2I|UBE2I]]|-2.00|0.68|
|[[:human_genes:E:EXOC3L1|EXOC3L1]]|-1.95|0.68|
|[[:human_genes:U:UST|UST]]|-1.94|0.68|
|[[:human_genes:A:APBB1IP|APBB1IP]]|-1.94|0.68|
|[[:human_genes:C:CCDC27|CCDC27]]|-1.93|0.68|
|[[:human_genes:P:PNRC2|PNRC2]]|-1.91|0.68|
|[[:human_genes:E:EFHC2|EFHC2]]|-1.90|0.68|
|[[:human_genes:P:PDE2A|PDE2A]]|-1.90|0.68|
|[[:human_genes:R:RSRC1|RSRC1]]|-1.88|0.68|
|[[:human_genes:F:FOXD4L1|FOXD4L1]]|-1.87|0.68|
|[[:human_genes:L:LDHA|LDHA]]|-1.86|0.68|
|[[:human_genes:C:CLEC4F|CLEC4F]]|-1.84|0.68|
|[[:human_genes:H:HDAC8|HDAC8]]|-1.83|0.68|
|[[:human_genes:I:IZUMO3|IZUMO3]]|-1.83|0.68|
|[[:human_genes:N:NSD1|NSD1]]|-1.83|0.68|
|[[:human_genes:K:KIF13A|KIF13A]]|-1.82|0.68|
|[[:human_genes:D:DENND3|DENND3]]|1.95|0.65|
|[[:human_genes:E:ERN1|ERN1]]|1.95|0.69|
|[[:human_genes:R:RPS14|RPS14]]|1.96|0.69|
|[[:human_genes:P:PSMD1|PSMD1]]|1.96|0.72|
|[[:human_genes:F:FAM71E1|FAM71E1]]|1.97|0.69|
|[[:human_genes:A:ARID3B|ARID3B]]|1.98|0.69|
|[[:human_genes:L:LOC100505679|LOC100505679]]|2.00|0.81|
|[[:human_genes:K:KPNB1|KPNB1]]|2.01|0.81|
|[[:human_genes:R:RPS3A|RPS3A]]|2.03|0.69|
|[[:human_genes:C:CDK8|CDK8]]|2.05|0.65|
|[[:human_genes:C:COPB1|COPB1]]|2.08|0.72|
|[[:human_genes:S:SKIV2L|SKIV2L]]|2.09|0.69|
|[[:human_genes:S:SEC13|SEC13]]|2.10|0.69|
|[[:human_genes:M:MGST1|MGST1]]|2.12|0.61|
|[[:human_genes:I:IQCG|IQCG]]|2.13|0.52|
|[[:human_genes:A:ABCB10|ABCB10]]|2.13|0.52|
|[[:human_genes:G:GATSL1|GATSL1]]|2.15|0.57|
|[[:human_genes:N:NUP155|NUP155]]|2.18|0.65|
|[[:human_genes:C:CCND3|CCND3]]|2.22|0.69|
|[[:human_genes:F:FSCN3|FSCN3]]|2.23|0.52|
|[[:human_genes:A:AAAS|AAAS]]|2.24|0.52|
|[[:human_genes:S:SCFD2|SCFD2]]|2.27|0.39|
|[[:human_genes:B:BCL11A|BCL11A]]|2.28|0.39|
|[[:human_genes:Z:ZNF331|ZNF331]]|2.28|0.39|
|[[:human_genes:R:RANGAP1|RANGAP1]]|2.30|0.57|
|[[:human_genes:L:LEPREL4|LEPREL4]]|2.32|0.39|
|[[:human_genes:F:FAM9B|FAM9B]]|2.32|0.57|
|[[:human_genes:E:ECD|ECD]]|2.37|0.72|
|[[:human_genes:R:RAD51|RAD51]]|2.39|0.65|
|[[:human_genes:P:PCNA|PCNA]]|2.47|0.72|
^Screen^Correlation^Plot^
|[[:results:exp421|VHL-ligand-1 20μM R07 exp421]]|0.051||
{{:chemogenomics:comparison_plots:exp376_vs_exp421.png?nolink |}}
No GO term hits below threshold. (FDR <0.05)
^GO Term^Fold Change^Genes^
|nuclear pore|30.03|RANGAP1,AAAS,NUP155,SEC13,KPNB1|