====== Dynasore 10μM R04 exp180 ======
==== Mechanism of Action ====
Putative dynamin GTPase inhibitor, blocks endocytosis
* **Class / Subclass 1:** Organelle Function / Vesicule Trafficking Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%Dynasore%%
* **Synonyms:** N/A
* **CAS #:** 304448-55-3
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/135533054|135533054]]
* **IUPAC:** %%N-[(E)-(3,4-dihydroxyphenyl)methylideneamino]-3-hydroxynaphthalene-2-carboxamide%%
* **INCHI Name:** InChI=1S/C18H14N2O4/c21-15-6-5-11(7-17(15)23)10-19-20-18(24)14-8-12-3-1-2-4-13(12)9-16(14)22/h1-10,21-23H,(H,20,24)/b19-10+
* **INCHI Key:** SYNDQCRDGGCQRZ-VXLYETTFSA-N
* **Molecular Weight:** 322.3
* **Canonical SMILES:** C1=CC=C2C=C(C(=CC2=C1)C(=O)NN=CC3=CC(=C(C=C3)O)O)O
* **Isomeric SMILES:** C1=CC=C2C=C(C(=CC2=C1)C(=O)N/N=C/C3=CC(=C(C=C3)O)O)O
* **Molecular Formula:** C18H14N2O4
{{:chemogenomics:structures:chem-0113.svg?nolink}}
* **Supplier Name:** ChemCruz
* **Catalog #:** SC-202592
* **Lot #:** B2216
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C18H14N2O4 323.10263; found 323.10352
* **Platform ID:** Dynasore
* **Min:** -1.6097; **Max:** 96.5116
{{:chemogenomics:dose_response:dr_211.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |8.6593 |
| IC30 |10.6253 |
| IC40 |12.5655 |
| IC50 |14.6562 |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 04
* **Dose**: 10µM
* **Days of incubation**: 8
* **Doublings**: 5.6
* **Numbers of reads**: 23091101
==== 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^
|23/8|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Dynasore_10uM_Round-4_exp180.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp180.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:S:SEPHS1|SEPHS1]]|-3.56|<0.01|
|[[:human_genes:H:HSP90B1|HSP90B1]]|-3.39|<0.01|
|[[:human_genes:S:SEC31A|SEC31A]]|-3.38|<0.01|
|[[:human_genes:K:KPTN|KPTN]]|-3.38|<0.01|
|[[:human_genes:N:NPRL3|NPRL3]]|-3.34|<0.01|
|[[:human_genes:A:ACSL4|ACSL4]]|-3.33|<0.01|
|[[:human_genes:D:DNAJC3|DNAJC3]]|-3.29|<0.01|
|[[:human_genes:S:SMC1A|SMC1A]]|-3.27|0.06|
|[[:human_genes:R:RPP21|RPP21]]|-2.96|<0.01|
|[[:human_genes:P:PEX7|PEX7]]|-2.85|<0.01|
|[[:human_genes:T:TNFAIP3|TNFAIP3]]|-2.80|<0.01|
|[[:human_genes:T:TUBB|TUBB]]|-2.75|0.06|
|[[:human_genes:V:VKORC1L1|VKORC1L1]]|-2.73|<0.01|
|[[:human_genes:D:DEPDC5|DEPDC5]]|-2.71|<0.01|
|[[:human_genes:D:DERL1|DERL1]]|-2.68|0.02|
|[[:human_genes:S:SLC25A37|SLC25A37]]|-2.67|<0.01|
|[[:human_genes:G:GCLM|GCLM]]|-2.67|<0.01|
|[[:human_genes:P:PEX1|PEX1]]|-2.66|<0.01|
|[[:human_genes:S:SZT2|SZT2]]|-2.64|<0.01|
|[[:human_genes:G:GCLC|GCLC]]|-2.63|<0.01|
|[[:human_genes:X:XPOT|XPOT]]|-2.60|0.02|
|[[:human_genes:L:LDLRAP1|LDLRAP1]]|-2.54|0.03|
|[[:human_genes:H:HEXIM1|HEXIM1]]|-2.52|0.02|
|[[:human_genes:C:CDKN2AIP|CDKN2AIP]]|-2.49|0.02|
|[[:human_genes:A:AAAS|AAAS]]|-2.44|0.08|
|[[:human_genes:C:C12orf66|C12orf66]]|-2.35|0.04|
|[[:human_genes:N:NUP35|NUP35]]|-2.26|0.06|
|[[:human_genes:G:GSS|GSS]]|-2.25|0.06|
|[[:human_genes:D:DNAJB11|DNAJB11]]|-2.25|0.06|
|[[:human_genes:C:CXorf56|CXorf56]]|-2.23|0.06|
|[[:human_genes:P:POLR2D|POLR2D]]|2.16|0.25|
|[[:human_genes:S:SDHAF2|SDHAF2]]|2.17|0.27|
|[[:human_genes:S:SLC31A1|SLC31A1]]|2.18|0.25|
|[[:human_genes:A:ALAD|ALAD]]|2.19|0.25|
|[[:human_genes:C:CASP8AP2|CASP8AP2]]|2.23|0.39|
|[[:human_genes:N:NFYA|NFYA]]|2.23|0.25|
|[[:human_genes:R:RPAP1|RPAP1]]|2.25|0.38|
|[[:human_genes:P:PRPF19|PRPF19]]|2.27|0.27|
|[[:human_genes:C:COPB2|COPB2]]|2.28|0.37|
|[[:human_genes:T:TRMT2A|TRMT2A]]|2.28|0.18|
|[[:human_genes:E:EIF4G1|EIF4G1]]|2.30|0.18|
|[[:human_genes:N:NFYC|NFYC]]|2.32|0.09|
|[[:human_genes:T:TTK|TTK]]|2.34|0.34|
|[[:human_genes:U:UBA6|UBA6]]|2.35|0.08|
|[[:human_genes:C:CAPRIN1|CAPRIN1]]|2.36|0.08|
|[[:human_genes:Z:ZC3H4|ZC3H4]]|2.39|0.20|
|[[:human_genes:G:GCN1L1|GCN1L1]]|2.41|0.07|
|[[:human_genes:P:PAFAH1B1|PAFAH1B1]]|2.42|0.42|
|[[:human_genes:Z:ZNF207|ZNF207]]|2.42|0.19|
|[[:human_genes:E:EIF4A1|EIF4A1]]|2.59|0.03|
|[[:human_genes:H:HMBS|HMBS]]|2.61|0.06|
|[[:human_genes:K:KPNA1|KPNA1]]|2.70|0.04|
|[[:human_genes:R:RBM25|RBM25]]|2.73|0.13|
|[[:human_genes:C:C12orf49|C12orf49]]|2.87|<0.01|
|[[:human_genes:A:ALAS1|ALAS1]]|2.95|0.01|
|[[:human_genes:U:UTP20|UTP20]]|2.97|0.13|
|[[:human_genes:Q:QKI|QKI]]|3.00|<0.01|
|[[:human_genes:M:MARCH5|MARCH5]]|3.42|<0.01|
|[[:human_genes:S:SLFN11|SLFN11]]|3.81|<0.01|
|[[:human_genes:F:FADS2|FADS2]]|4.08|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp436|Dynasore 7μM R08 exp436]]|0.145||
|[[:results:exp416|Tubacin 1.6μM R07 exp416]]|0.107||
|[[:results:exp84|UM0125461 0.74μM R02 exp84]]|0.079||
|[[:results:exp517|Quercetin 20μM R08 exp517]]|0.068||
|[[:results:exp122|Golgicide-A 4μM R03 exp122]]|0.057||
|[[:results:exp78|Pterostilbene 16μM R02 exp78]]|0.054||
|[[:results:exp356|Docosahexaenoic-acid 50μM R07 exp356]]|0.076||
|[[:results:exp175|3-Bromopyruvate 7μM R04 exp175]]|0.071||
|[[:results:exp348|Cyclosporin-A 3μM R07 exp348]]|0.062||
|[[:results:exp227|Cryptotanshinone 12μM R05 exp227]]|0.059||
|[[:results:exp450|Artemisinin 50μM R08 exp450]]|0.053||
{{:chemogenomics:comparison_plots:exp180_vs_exp436.png?nolink |}}
{{:chemogenomics:comparison_plots:exp180_vs_exp416.png?nolink |}}
{{:chemogenomics:comparison_plots:exp180_vs_exp84.png?nolink |}}
{{:chemogenomics:comparison_plots:exp180_vs_exp517.png?nolink |}}
{{:chemogenomics:comparison_plots:exp122_vs_exp180.png?nolink |}}
{{:chemogenomics:comparison_plots:exp180_vs_exp78.png?nolink |}}
{{:chemogenomics:comparison_plots:exp180_vs_exp356.png?nolink |}}
{{:chemogenomics:comparison_plots:exp175_vs_exp180.png?nolink |}}
{{:chemogenomics:comparison_plots:exp180_vs_exp348.png?nolink |}}
{{:chemogenomics:comparison_plots:exp180_vs_exp227.png?nolink |}}
{{:chemogenomics:comparison_plots:exp180_vs_exp450.png?nolink |}}
^GO Term^Fold Change^Genes^
|response to human chorionic gonadotropin|295.96|GCLM,GCLC|
|response to L-phenylalanine derivative|236.77|GCLM,GCLC|
|nonribosomal peptide biosynthetic process|126.84|GCLM,GCLC,GSS|
|misfolded protein binding|93.46|DNAJC3,DERL1,DNAJB11|
|acid-amino acid ligase activity|84.56|GCLM,GCLC,GSS|
|negative regulation of TORC1 signaling|57.75|KPTN,NPRL3,DEPDC5,SZT2|
|cellular response to amino acid starvation|49.33|KPTN,NPRL3,DEPDC5,SZT2|
|response to amino acid starvation|46.43|KPTN,NPRL3,DEPDC5,SZT2|
|negative regulation of TOR signaling|35.87|KPTN,NPRL3,DEPDC5,SZT2|
|regulation of TORC1 signaling|27.53|KPTN,NPRL3,DEPDC5,SZT2|
^GO Term^Fold Change^Genes^
|protoporphyrinogen IX biosynthetic process|207.18|ALAS1,HMBS,ALAD|
|protoporphyrinogen IX metabolic process|165.74|ALAS1,HMBS,ALAD|