RN 1747: a TRPV4 agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| 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 |
| 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 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 13.4504 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 0.7564 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Transient receptor potential cation channel subfamily V member 4 | Mus musculus (house mouse) | EC50 (µMol) | 0.7700 | 0.1500 | 1.3800 | 6.3000 | AID1667132 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 | Identification and characterization of novel TRPV4 modulators. |
| [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 | 1 (12.50) | 29.6817 |
| 2010's | 4 (50.00) | 24.3611 |
| 2020's | 3 (37.50) | 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 (18.42) All Compounds (24.57) |
| 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% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||