RN 1747: a TRPV4 agonist; structure in first source [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 5068295 |
| CHEMBL ID | 4303584 |
| MeSH ID | M0540705 |
| Synonym |
|---|
| 1-benzyl-4-(4-chloro-2-nitrophenyl)sulfonylpiperazine |
| 4-chloro-2-nitro-1-((4-benzylpiperazinyl)sulfonyl)benzene |
| rn-1747 |
| 1024448-59-6 |
| rn 1747 |
| gtpl4295 |
| rn1747 |
| 1-benzyl-4-[(4-chloro-2-nitrobenzene)sulfonyl]piperazine |
| AKOS022168684 |
| 1-benzyl-4-(4-chloro-2-nitrobenzenesulfonyl)piperazine |
| MS-10440 |
| 1-(4-chloro-2-nitrophenyl)sulfonyl-4-benzylpiperazine |
| 1-(4-chloro-2-nitrophenyl)sulfonyl- 4-benzylpiperazine |
| c17h18cln3o4s |
| HB1186 |
| DTXSID80408000 |
| J-000691 |
| mfcd04154169 |
| rn-1747, >=98% (hplc) |
| NCGC00370824-01 |
| HMS3678D03 |
| ZB1552 |
| 1-benzyl-4-((4-chloro-2-nitrophenyl)sulfonyl)piperazine |
| Q27088564 |
| HMS3414D03 |
| EX-A3072 |
| CS-0017520 |
| CHEMBL4303584 , |
| HY-19976 |
| bdbm50545035 |
| ZQB44859 |
| AC-36308 |
| AKOS040742557 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 13.4504 | AID1645841 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 0.7564 | AID1645840 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Transient receptor potential cation channel subfamily V member 4 | Mus musculus (house mouse) | EC50 | 0.7700 | AID1667132 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 ISSN: 2472-5560 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1667132 | Agonist activity at mouse TRPV4 | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8 ISSN: 1464-3405 | Recent advances in TRPV4 agonists and antagonists. |
| AID1346615 | Rat TRPV4 (Transient Receptor Potential channels) | 2009 | Biochemical and biophysical research communications, Nov-20, Volume: 389, Issue:3 ISSN: 1090-2104 | Identification and characterization of novel TRPV4 modulators. |
| AID1346607 | Mouse TRPV4 (Transient Receptor Potential channels) | 2009 | Biochemical and biophysical research communications, Nov-20, Volume: 389, Issue:3 ISSN: 1090-2104 | Identification and characterization of novel TRPV4 modulators. |
| AID1346605 | Human TRPV4 (Transient Receptor Potential channels) | 2009 | Biochemical and biophysical research communications, Nov-20, Volume: 389, Issue:3 ISSN: 1090-2104 | Identification and characterization of novel TRPV4 modulators. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (12.50) | 29.6817 |
| 2010's | 4 (50.00) | 24.3611 |
| 2020's | 3 (37.50) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (12.50%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (87.50%) | 84.16% |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| phorbol-12,13-didecanoate, (1ar-(1aalpha,1bbeta,4aalpha,7aalpha,7balpha,8alpha,9beta,9aalpha))-isomer | decanoate ester; diester; phorbol ester; primary allylic alcohol; tertiary alpha-hydroxy ketone | TRPV4 agonist | 2020 | 2020 | 4.0 | high | 0 | 0 | 0 | 0 | 1 | 0 | |
| hc-067047 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |||
| rn 1734 | 2009 | 2020 | 9.5 | medium | 0 | 0 | 0 | 1 | 1 | 0 | |||
| 5,6-epoxy-8,11,14-eicosatrienoic acid | EET | mouse metabolite | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| histamine | aralkylamino compound; imidazoles | human metabolite; mouse metabolite; neurotransmitter | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| leucine | amino acid zwitterion; L-alpha-amino acid; leucine; proteinogenic amino acid; pyruvate family amino acid | algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; plant metabolite; Saccharomyces cerevisiae metabolite | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| pyrroles | pyrrole; secondary amine | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | ||
| pregnenolone | 20-oxo steroid; 3beta-hydroxy-Delta(5)-steroid; C21-steroid | human metabolite; mouse metabolite | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| pregnenolone sulfate | steroid sulfate | EC 2.7.1.33 (pantothenate kinase) inhibitor; human metabolite | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| phorbol-12,13-didecanoate | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |||
| hc-067047 | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |||
| rn 1734 | 2009 | 2019 | 10.0 | medium | 0 | 0 | 0 | 1 | 1 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | high | 0 | 0 | 0 | 0 | 1 | 0 | |
| Disease Models, Animal | 0 | 2020 | 2020 | 4.0 | high | 0 | 0 | 0 | 0 | 1 | 0 | |
| Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | high | 0 | 0 | 0 | 0 | 1 | 0 |
| Article | Year |
|---|---|
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5 | 2019 |