tenovin-1: a SIRT1 inhibitor with antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 1013376 |
| CHEMBL ID | 1436543 |
| CHEBI ID | 94482 |
| SCHEMBL ID | 907582 |
| MeSH ID | M000601763 |
| Synonym |
|---|
| 380315-80-0 |
| n-(4-acetamidophenylcarbamothioyl)-4-tert-butylbenzamide |
| NCGC00181351-01 |
| OPREA1_317255 |
| n-{[4-(acetylamino)phenyl]carbamothioyl}-4-tert-butylbenzamide |
| STK077754 |
| AKOS000492892 |
| n-[(4-acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide |
| dtxsid1046920 , |
| cas-380315-80-0 |
| dtxcid9026920 |
| tox21_112809 |
| tenovin-1 |
| CHEMBL1436543 |
| tenovin 1 |
| S8000 |
| BRD-K05977823-001-01-2 |
| CCG-208685 |
| HY-13423 |
| CS-1512 |
| AB00109204-01 |
| SCHEMBL907582 |
| n-[[[4-(acetylamino)phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)benzamide |
| unii-biq6aid2b7 |
| n-[[[4-(acetylamino)phenyl]amino]thioxomethyl-4-(1,1-dimethylethyl)]benzamide |
| WOWJIWFCOPZFGV-UHFFFAOYSA-N |
| n-((4-acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide |
| HMS3648C12 |
| J-524320 |
| EX-A146 |
| n-[4-({[(4-tert-butylphenyl)formamido]methanethioyl}amino)phenyl]acetamide |
| CHEBI:94482 |
| HMS3653D17 |
| mfcd02914760 |
| NCGC00181351-05 |
| BIQ6AID2B7 , |
| benzamide, n-(((4-(acetylamino)phenyl)amino)thioxomethyl)-4-(1,1-dimethylethyl)- |
| SW133688-2 |
| BCP06745 |
| Q27166342 |
| n-[(4-acetamidoanilino)-sulfanylidenemethyl]-4-tert-butylbenzamide |
| tenovin-1 - cas 380315-80-0 |
| n -[[[4-(acetylamino)phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)benzamide |
| Z56060122 |
| AS-16764 |
| sr-01000946350 |
| SR-01000946350-1 |
| AMY24210 |
| SB19404 |
| EN300-657177 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Class | Description |
|---|---|
| thioureas | Compounds of general formula RR'NC(=S)NR''R'''. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| USP1 protein, partial | Homo sapiens (human) | Potency | 35.4813 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
| AR protein | Homo sapiens (human) | Potency | 3.7532 | 0.0002 | 21.2231 | 8,912.5098 | AID743035; AID743036; AID743042; AID743053; AID743054; AID743063 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 30.1065 | 0.0002 | 14.3764 | 60.0339 | AID720692 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 2.2387 | 0.0054 | 28.0263 | 1,258.9301 | AID1346985 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 1.8207 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743078; AID743080; AID743091 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 1.4960 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 12.5893 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 8.9125 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 2.8226 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 4.9844 | 0.0056 | 12.3677 | 36.1254 | AID624032; AID624044 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 0.8078 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 1.3333 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
| Ataxin-2 | Homo sapiens (human) | Potency | 1.3333 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID644487 | Inhibition of recombinant human SitT1 at 60 uM by Fluor de Lys fluorescence assay | 2012 | Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5 | Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. |
| AID644488 | Inhibition of recombinant human SitT1 by Fluor de Lys fluorescence assay | 2012 | Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5 | Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. |
| AID644486 | Inhibition of recombinant human SitT2 at 60 uM by Fluor de Lys fluorescence assay | 2012 | Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5 | Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. |
| AID644490 | Inhibition of SirT1 assessed as increase in p53 expression in human MCF7 cells at 5 uM after 6 hrs by Western blotting | 2012 | Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5 | Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. |
| AID644489 | Inhibition of SirT1 assessed as increase in p53 expression in human MCF7 cells at 10 uM after 6 hrs by Western blotting | 2012 | Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5 | Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. |
| AID644485 | Inhibition of recombinant human SitT2 by Fluor de Lys fluorescence assay | 2012 | Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5 | Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. |
| AID644491 | Inhibition of SirT1 assessed as increase in p53 expression in human MCF7 cells at 2 uM after 6 hrs by Western blotting | 2012 | Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5 | Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. |
| AID644483 | Solubility of the compound in water by UV spectrophotometry | 2012 | Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5 | Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 13 (68.42) | 24.3611 |
| 2020's | 6 (31.58) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (22.14) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 19 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||