PF-06409577 20μM R07 exp389 [The Human Chemical-Genetic Interaction Map Project]

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====== PF-06409577 20μM R07 exp389 ======
==== Mechanism of Action ====
Activates AMPK, lowers cholesterol levels in NAFLD/NASH preclinical models
  * **<color #00a2e8>Class / Subclass 1:</color>** Signal Transduction / Kinase Activator




==== Technical Notes ====
<accordion collapsed='true'>
<panel title='Compound References' collapsed='true'>
    * **<color #00a2e8>PubChem Name:</color>** %%6-Chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylic acid%%
    * **<color #00a2e8>Synonyms:</color>** N/A
    * **<color #00a2e8>CAS #:</color>** 1467057-23-3
    * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/71748255|71748255]]
    * **<color #00a2e8>IUPAC:</color>** %%6-chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic acid%%
    * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C19H16ClNO3/c20-16-9-17-14(15(10-21-17)18(22)23)8-13(16)11-2-4-12(5-3-11)19(24)6-1-7-19/h2-5,8-10,21,24H,1,6-7H2,(H,22,23)
    * **<color #00a2e8>INCHI Key:</color>** FHQXLWCFSUSXBF-UHFFFAOYSA-N
    * **<color #00a2e8>Molecular Weight:</color>** 341.8
    * **<color #00a2e8>Canonical SMILES:</color>** C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=C3)C(=CN4)C(=O)O)Cl)O
    * **<color #00a2e8>Isomeric SMILES:</color>** N/A
    * **<color #00a2e8>Molecular Formula:</color>** C19H16ClNO3
{{:chemogenomics:structures:chem-0231.svg?nolink}}
</panel>


<panel title='Compound Supplier' collapsed='true'>
    * **<color #00a2e8>Supplier Name:</color>** Med Chem Express
    * **<color #00a2e8>Catalog #:</color>** HY-103683
    * **<color #00a2e8>Lot #:</color>** 27233
</panel>


<panel title='Compound Characterization' collapsed='true'>
    * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+Na)+ Calcd for C19H16ClNO3 364.07109; found 364.07064
</panel>


<panel title='Dose Response Curve' collapsed='true'>
    * **<color #00a2e8>Platform ID:</color>** PF-06409577
    * **<color #00a2e8>Min:</color>** -1.6834; **<color #00a2e8>Max:</color>** 29.3429
{{:chemogenomics:dose_response:dr_396.png?nolink&500 |}}
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|< 300px 100px 200px >|
^ 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    |
\\ 
</panel>
</accordion>
==== Screen Summary ====
    * **<color #00a2e8>Round</color>**: 07
    * **<color #00a2e8>Dose</color>**: 20µM
    * **<color #00a2e8>Days of incubation</color>**: 8
    * **<color #00a2e8>Doublings</color>**: 6.1
    * **<color #00a2e8>Numbers of reads</color>**: 20658744


==== 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^
|1/10|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/PF-06409577_20uM_Round-7_exp389.txt|Scores]]</color>|<button type="primary" size="sm" modal="ScorePlot">View</button>|<button type="primary" size="sm" modal="modal_hits">View</button>|<button type="primary" size="sm" modal="modal_screen_similarity">View</button>|<button type="default" size="sm" modal="modal_go_sensitive">View</button>|<button type="primary" size="sm" modal="modal_go_resistant">View</button>|
<modal id='ScorePlot' size='lg' title='PF-06409577 20μM R07 exp389'>
{{:chemogenomics:cranks_plots:exp389.png?nolink}}
</modal>


<modal id="modal_hits" size="sm" title="Top 30 S/R Genes">
^Gene^CRANKS Score^FDR^
|[[:human_genes:P:PNMA1|PNMA1]]|-2.94|0.03|
|[[:human_genes:A:AHCYL1|AHCYL1]]|-2.73|0.13|
|[[:human_genes:L:LAMTOR4|LAMTOR4]]|-2.53|0.19|
|[[:human_genes:W:WDR20|WDR20]]|-2.45|0.16|
|[[:human_genes:S:SLC7A11|SLC7A11]]|-2.31|0.23|
|[[:human_genes:M:MCM9|MCM9]]|-2.27|0.31|
|[[:human_genes:P:PLEKHA6|PLEKHA6]]|-2.26|0.23|
|[[:human_genes:P:PRAMEF25|PRAMEF25]]|-2.24|0.68|
|[[:human_genes:Z:ZC3H7B|ZC3H7B]]|-2.24|0.33|
|[[:human_genes:T:TGS1|TGS1]]|-2.23|0.23|
|[[:human_genes:G:GPR152|GPR152]]|-2.23|0.23|
|[[:human_genes:P:PRAMEF26|PRAMEF26]]|-2.23|0.68|
|[[:human_genes:K:KDSR|KDSR]]|-2.21|0.23|
|[[:human_genes:K:KDM6B|KDM6B]]|-2.13|0.38|
|[[:human_genes:P:PRUNE|PRUNE]]|-2.10|0.38|
|[[:human_genes:T:TRIP4|TRIP4]]|-2.07|0.35|
|[[:human_genes:F:FAM64A|FAM64A]]|-2.06|0.35|
|[[:human_genes:N:NAF1|NAF1]]|-2.06|0.35|
|[[:human_genes:S:SESTD1|SESTD1]]|-2.04|0.37|
|[[:human_genes:D:DKC1|DKC1]]|-2.03|0.68|
|[[:human_genes:Z:ZDHHC23|ZDHHC23]]|-2.02|0.38|
|[[:human_genes:M:MTRNR2L9|MTRNR2L9]]|-2.00|0.68|
|[[:human_genes:C:CNBD1|CNBD1]]|-1.98|0.38|
|[[:human_genes:Z:ZSWIM8|ZSWIM8]]|-1.98|0.38|
|[[:human_genes:S:SASH3|SASH3]]|-1.97|0.38|
|[[:human_genes:P:PRPF18|PRPF18]]|-1.96|0.44|
|[[:human_genes:C:CCDC82|CCDC82]]|-1.96|0.44|
|[[:human_genes:G:GGPS1|GGPS1]]|-1.95|0.38|
|[[:human_genes:M:MURC|MURC]]|-1.94|0.38|
|[[:human_genes:C:CMTR2|CMTR2]]|-1.94|0.38|
|[[:human_genes:S:SRD5A3|SRD5A3]]|2.08|0.19|
|[[:human_genes:C:CCL16|CCL16]]|2.11|0.22|
|[[:human_genes:N:NUP160|NUP160]]|2.11|0.36|
|[[:human_genes:D:DRD3|DRD3]]|2.16|0.13|
|[[:human_genes:S:STK38|STK38]]|2.17|0.12|
|[[:human_genes:I:IPMK|IPMK]]|2.17|0.12|
|[[:human_genes:S:SLC25A1|SLC25A1]]|2.18|0.12|
|[[:human_genes:D:DNAJC21|DNAJC21]]|2.20|0.12|
|[[:human_genes:C:CD52|CD52]]|2.22|0.12|
|[[:human_genes:E:EIF4B|EIF4B]]|2.23|0.12|
|[[:human_genes:G:GNA13|GNA13]]|2.24|0.12|
|[[:human_genes:G:G3BP1|G3BP1]]|2.28|0.10|
|[[:human_genes:A:AGBL5|AGBL5]]|2.29|0.22|
|[[:human_genes:B:BMP15|BMP15]]|2.31|0.09|
|[[:human_genes:S:STIL|STIL]]|2.34|0.12|
|[[:human_genes:K:KPNB1|KPNB1]]|2.34|0.45|
|[[:human_genes:R:RIC8A|RIC8A]]|2.36|0.08|
|[[:human_genes:S:SPC25|SPC25]]|2.42|0.32|
|[[:human_genes:M:MSI2|MSI2]]|2.49|0.08|
|[[:human_genes:U:UBE2Q2L|UBE2Q2L]]|2.56|0.47|
|[[:human_genes:I:IPPK|IPPK]]|2.72|0.01|
|[[:human_genes:L:LRRC30|LRRC30]]|2.74|0.03|
|[[:human_genes:D:DEPDC5|DEPDC5]]|2.88|<0.01|
|[[:human_genes:N:NPRL3|NPRL3]]|2.93|0.03|
|[[:human_genes:N:NPRL2|NPRL2]]|3.27|<0.01|
|[[:human_genes:S:STK11|STK11]]|4.77|<0.01|
|[[:human_genes:S:STRADA|STRADA]]|5.37|<0.01|
|[[:human_genes:P:PRKAG1|PRKAG1]]|5.88|<0.01|
|[[:human_genes:P:PRKAA1|PRKAA1]]|6.45|<0.01|
|[[:human_genes:P:PRKAB1|PRKAB1]]|7.12|<0.01|
</modal>


<modal id="modal_screen_similarity" size="lg" title="Correlated Screens">
^Screen^Correlation^Plot^
|[[:results:exp100|NFN1 1μM R03 exp100]]|0.069|<button type="primary" size="small" modal="1">View</button>|
|[[:results:exp510|Nicotine 3000μM R08 exp510]]|0.064|<button type="primary" size="small" modal="2">View</button>|
</modal>


<modal id="1" size="lg" title="NFN1 1μM R03 exp100  vs  PF-06409577 20μM R07 exp389">
{{:chemogenomics:comparison_plots:exp100_vs_exp389.png?nolink |}}
</modal>

<modal id="2" size="lg" title="Nicotine 3000μM R08 exp510  vs  PF-06409577 20μM R07 exp389">
{{:chemogenomics:comparison_plots:exp389_vs_exp510.png?nolink |}}
</modal>



<modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">No GO term hits below threshold. (FDR <0.05)</modal>
<modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">
^GO Term^Fold Change^Genes^
|GATOR1 complex|552.63|NPRL2,NPRL3|
|Seh1-associated complex|236.84|NPRL2,NPRL3,DEPDC5|
|cAMP-dependent protein kinase activity|221.05|PRKAA1,PRKAG1|
|negative regulation of TORC1 signaling|67.39|PRKAA1,STK11,NPRL2,NPRL3,DEPDC5|
|negative regulation of TOR signaling|41.87|PRKAA1,STK11,NPRL2,NPRL3,DEPDC5|
|regulation of TORC1 signaling|32.13|PRKAA1,STK11,NPRL2,NPRL3,DEPDC5|
|alcohol biosynthetic process|24.56|PRKAA1,IPPK,IPMK,SRD5A3|
|regulation of TOR signaling|20.47|PRKAA1,STK11,NPRL2,NPRL3,DEPDC5|
|protein kinase complex|18.93|PRKAB1,PRKAA1,PRKAG1,STRADA,STK11|
|positive regulation of autophagy|18.93|PRKAA1,STK11,NPRL2,NPRL3,DEPDC5|
|cellular response to nutrient levels|14.29|PRKAB1,PRKAA1,PRKAG1,NPRL2,NPRL3,DEPDC5|
|cellular response to extracellular stimulus|12.70|PRKAB1,PRKAA1,PRKAG1,NPRL2,NPRL3,DEPDC5|
|cellular response to external stimulus|10.17|PRKAB1,PRKAA1,PRKAG1,NPRL2,NPRL3,DEPDC5|
|small molecule biosynthetic process|8.63|PRKAB1,PRKAA1,PRKAG1,IPPK,SLC25A1,IPMK,SRD5A3|
|negative regulation of intracellular signal transduction|7.54|PRKAA1,STK11,NPRL2,NPRL3,DEPDC5,STK38,DRD3|
|phosphotransferase activity, alcohol group as acceptor|6.54|PRKAB1,PRKAA1,PRKAG1,STRADA,STK11,IPPK,IPMK,STK38|
|phosphorylation|6.13|PRKAB1,PRKAA1,PRKAG1,STRADA,STK11,IPPK,IPMK,STK38|
|kinase activity|6.06|PRKAB1,PRKAA1,PRKAG1,STRADA,STK11,IPPK,IPMK,STK38|
</modal>