====== Phenformin 20μM R05 exp212 ======
==== Mechanism of Action ====
Inhibits mitochondrial respiratory chain complex I, indirectly activates AMPK
* **Class / Subclass 1:** Organelle Function / Mitochondrial Inhibitor
* **Class / Subclass 2:** Metabolism / Metabolic Enzyme Activator
==== Technical Notes ====
* **PubChem Name:** %%Phenformin hydrochloride%%
* **Synonyms:** Phenethylbiguanide hydrochloride
* **CAS #:** 834-28-6
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/13266|13266]]
* **IUPAC:** %%1-(diaminomethylidene)-2-(2-phenylethyl)guanidine;hydrochloride%%
* **INCHI Name:** InChI=1S/C10H15N5.ClH/c11-9(12)15-10(13)14-7-6-8-4-2-1-3-5-8;/h1-5H,6-7H2,(H6,11,12,13,14,15);1H
* **INCHI Key:** YSUCWSWKRIOILX-UHFFFAOYSA-N
* **Molecular Weight:** 241.72
* **Canonical SMILES:** C1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl
* **Isomeric SMILES:** N/A
* **Molecular Formula:** C10H16ClN5
{{:chemogenomics:structures:chem-0094.svg?nolink}}
* **Supplier Name:** Sigma-Aldrich (Supelco)
* **Catalog #:** P7045
* **Lot #:** MKBV9127V
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C10H15N5 208.14493; found 208.14677
* **Platform ID:** PHENFORMINE
* **Min:** -0.7796; **Max:** 41.1406
{{:chemogenomics:dose_response:dr_109.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |4.1494 |
| IC30 |21.8108 |
| IC40 |85.0051 |
| IC50 |N/A |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 05
* **Dose**: 20µM
* **Days of incubation**: 8
* **Doublings**: 3.5
* **Numbers of reads**: 20548414
==== 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^
|3/6|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Phenformin_20uM_Round-5_exp212.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp212.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:G:GOT1|GOT1]]|-4.75|<0.01|
|[[:human_genes:S:SUCLG1|SUCLG1]]|-3.13|<0.01|
|[[:human_genes:E:ENO1|ENO1]]|-2.91|<0.01|
|[[:human_genes:L:LOC391322|LOC391322]]|-2.46|0.64|
|[[:human_genes:N:NUDT5|NUDT5]]|-2.41|0.30|
|[[:human_genes:C:CIC|CIC]]|-2.28|0.30|
|[[:human_genes:T:TBC1D3L|TBC1D3L]]|-2.27|0.56|
|[[:human_genes:T:TBC1D3K|TBC1D3K]]|-2.24|0.56|
|[[:human_genes:T:TBC1D3E|TBC1D3E]]|-2.22|0.56|
|[[:human_genes:T:TBC1D3I|TBC1D3I]]|-2.20|0.56|
|[[:human_genes:S:SMIM6|SMIM6]]|-2.17|0.40|
|[[:human_genes:U:UBE2N|UBE2N]]|-2.17|0.44|
|[[:human_genes:T:TAS2R60|TAS2R60]]|-2.16|0.40|
|[[:human_genes:C:CCL16|CCL16]]|-2.13|0.44|
|[[:human_genes:Z:ZNF229|ZNF229]]|-2.10|0.44|
|[[:human_genes:S:SOD1|SOD1]]|-2.07|0.54|
|[[:human_genes:N:NME6|NME6]]|-2.07|0.44|
|[[:human_genes:C:CD5L|CD5L]]|-2.05|0.44|
|[[:human_genes:R:RAPH1|RAPH1]]|-2.03|0.46|
|[[:human_genes:P:PTEN|PTEN]]|-2.02|0.44|
|[[:human_genes:N:NAGK|NAGK]]|-2.01|0.46|
|[[:human_genes:A:ADK|ADK]]|-2.01|0.44|
|[[:human_genes:C:CMC2|CMC2]]|-2.00|0.64|
|[[:human_genes:P:PDXK|PDXK]]|-2.00|0.44|
|[[:human_genes:T:TMEM60|TMEM60]]|-2.00|0.46|
|[[:human_genes:G:GCDH|GCDH]]|-2.00|0.46|
|[[:human_genes:R:RGCC|RGCC]]|-2.00|0.44|
|[[:human_genes:S:SERPINA6|SERPINA6]]|-1.99|0.44|
|[[:human_genes:K:KEAP1|KEAP1]]|-1.98|0.49|
|[[:human_genes:B:B4GALT5|B4GALT5]]|-1.98|0.44|
|[[:human_genes:D:DNAJC24|DNAJC24]]|2.19|0.10|
|[[:human_genes:I:IPMK|IPMK]]|2.19|0.10|
|[[:human_genes:C:COX7B|COX7B]]|2.20|0.10|
|[[:human_genes:C:C6orf203|C6orf203]]|2.21|0.10|
|[[:human_genes:A:ATP5F1|ATP5F1]]|2.22|0.13|
|[[:human_genes:Z:ZNF91|ZNF91]]|2.23|0.10|
|[[:human_genes:I:ITPK1|ITPK1]]|2.24|0.10|
|[[:human_genes:S:SCAP|SCAP]]|2.24|0.13|
|[[:human_genes:R:RXFP2|RXFP2]]|2.25|0.10|
|[[:human_genes:C:COA6|COA6]]|2.26|0.10|
|[[:human_genes:N:NRBP1|NRBP1]]|2.26|0.15|
|[[:human_genes:N:NBPF12|NBPF12]]|2.27|0.52|
|[[:human_genes:A:ATP5C1|ATP5C1]]|2.27|0.12|
|[[:human_genes:L:LARS2|LARS2]]|2.32|0.10|
|[[:human_genes:P:PDS5B|PDS5B]]|2.33|0.10|
|[[:human_genes:M:MRPS25|MRPS25]]|2.34|0.19|
|[[:human_genes:M:MRPL33|MRPL33]]|2.36|0.18|
|[[:human_genes:D:DHX35|DHX35]]|2.37|0.10|
|[[:human_genes:C:CAPRIN1|CAPRIN1]]|2.39|0.08|
|[[:human_genes:S:SERP2|SERP2]]|2.43|0.08|
|[[:human_genes:A:ATP5A1|ATP5A1]]|2.48|0.10|
|[[:human_genes:A:ATP5L|ATP5L]]|2.54|0.10|
|[[:human_genes:V:VARS2|VARS2]]|2.56|0.08|
|[[:human_genes:T:TRMT61A|TRMT61A]]|2.57|0.10|
|[[:human_genes:P:PMVK|PMVK]]|2.58|0.05|
|[[:human_genes:G:G3BP1|G3BP1]]|2.62|0.05|
|[[:human_genes:A:ATP5B|ATP5B]]|2.69|0.04|
|[[:human_genes:A:ACSL3|ACSL3]]|2.72|0.05|
|[[:human_genes:S:SLC25A51|SLC25A51]]|3.39|<0.01|
|[[:human_genes:P:PTPMT1|PTPMT1]]|3.48|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp439|QNZ 0.01μM R08 exp439]]|0.105||
|[[:results:exp241|QNZ 0.01μM R05 exp241]]|0.103||
|[[:results:exp431|Rotenone 0.07μM R08 exp431]]|0.102||
|[[:results:exp248|UM0131023 0.05μM R05 exp248]]|0.072||
|[[:results:exp492|iCRT14 30μM R08 exp492]]|0.06||
|[[:results:exp380|NMS-873 0.07μM R07 exp380]]|0.091||
|[[:results:exp13|Chloramphenicol 20μM R00 exp13]]|0.09||
|[[:results:exp65|Mubritinib 0.2μM R02 exp65]]|0.079||
|[[:results:exp447|Amiloride 100μM R08 exp447]]|0.063||
|[[:results:exp143|Phenformin 20μM R03 exp143]]|0.061||
|[[:results:exp48|Mubritinib 0.2μM R01 exp48]]|0.059||
|[[:results:exp191|Hypoxia 5%O2 R04 exp191]]|0.057||
|[[:results:exp290|LLY-283 2.6μM R06 exp290]]|0.051||
{{:chemogenomics:comparison_plots:exp212_vs_exp439.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp241.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp431.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp248.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp492.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp380.png?nolink |}}
{{:chemogenomics:comparison_plots:exp13_vs_exp212.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp65.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp447.png?nolink |}}
{{:chemogenomics:comparison_plots:exp143_vs_exp212.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp48.png?nolink |}}
{{:chemogenomics:comparison_plots:exp191_vs_exp212.png?nolink |}}
{{:chemogenomics:comparison_plots:exp212_vs_exp290.png?nolink |}}
No GO term hits below threshold. (FDR <0.05)
^GO Term^Fold Change^Genes^
|proton-transporting ATP synthase activity, rotational mechanism|197.26|ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB|
|mitochondrial proton-transporting ATP synthase complex|184.11|ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB|
|proton-transporting ATP synthase complex|172.60|ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB|
|proton channel activity|125.53|ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB|
|oxidative phosphorylation|44.63|SLC25A51,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,COA6,ATP5PB,COX7B|
|ligase activity|34.74|ACSL3,ATP5F1B,VARS2,ATP5MG,ATP5F1A,LARS2,ATP5F1C,ATP5PB,MTHFD1,ACSL4|
|aerobic respiration|31.34|SLC25A51,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,COA6,ATP5PB,COX7B|
|cellular respiration|26.15|SLC25A51,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,COA6,ATP5PB,COX7B|
|purine ribonucleotide biosynthetic process|25.25|ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4|
|ribonucleotide biosynthetic process|23.26|ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4|
|ribose phosphate biosynthetic process|22.43|ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4|
|purine nucleotide biosynthetic process|20.84|ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4|
|purine-containing compound biosynthetic process|19.99|ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4|
|purine ribonucleotide metabolic process|15.53|ACSL3,ATP5F1B,PMVK,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4|
|ribonucleotide metabolic process|14.62|ACSL3,ATP5F1B,PMVK,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4|
|mitochondrial inner membrane|12.06|PTPMT1,SLC25A51,ATP5F1B,ATP5MG,ATP5F1A,MRPL33,MRPS25,ATP5F1C,ATP5PB,COX7B|
|organophosphate biosynthetic process|11.71|PTPMT1,ACSL3,ATP5F1B,PMVK,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4,IPMK|
|mitochondrial envelope|9.56|PTPMT1,SLC25A51,ACSL3,ATP5F1B,ATP5MG,ATP5F1A,MRPL33,MRPS25,ATP5F1C,COA6,ATP5PB,COX7B,ACSL4|
|mitochondrial membrane|9.40|PTPMT1,SLC25A51,ACSL3,ATP5F1B,ATP5MG,ATP5F1A,MRPL33,MRPS25,ATP5F1C,ATP5PB,COX7B,ACSL4|