SB-611812: urotensin-II antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 10278166 |
| CHEMBL ID | 1164033 |
| SCHEMBL ID | 6542569 |
| MeSH ID | M0502238 |
| Synonym |
|---|
| 2,6-dichloro-n-[4-chloro-3-(2-dimethylaminoethoxy)phenyl]-4-(trifluoromethyl)benzenesulfonamide |
| 2,6-dichloro-n-(4-chloro-3-(2-(dimethylamino)ethoxy)phenyl)-4-(trifluoromethyl)benzenesulfonamide , |
| bdbm50320477 |
| CHEMBL1164033 , |
| sb-611812 |
| gtpl3531 |
| sb611812 |
| 2,6-dichloro-n-[4-chloro-3-(2-dimethylamino-ethoxy)-phenyl]-4-trifluoromethyl-benzenesulfonamide |
| SCHEMBL6542569 |
| AKOS024458282 |
| sb 611812 |
| 345892-71-9 |
| 2,6-dichloro-n-[4-chloro-3-[2-(dimethylamino)ethoxy]phenyl]-4-(trifluoromethyl)benzenesulfonamide |
| benzenesulfonamide,2,6-dichloro-n-[4-chloro-3-[2-(dimethylamino)ethoxy]phenyl]-4-(trifluoromethyl)- |
| NCGC00379178-01 |
| Q27088731 |
| benzenesulfonamide, 2,6-dichloro-n-[4-chloro-3-[2-(dimethylamino)ethoxy]phenyl]-4-(trifluoromethyl)- |
| MS-29142 |
| EX-A6822 |
| HY-10664 |
| CS-0002718 |
| 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 | 10.6840 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 16.9330 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 8.4866 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [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) |
|---|---|---|---|---|---|---|---|
| Urotensin-2 receptor | Rattus norvegicus (Norway rat) | Ki | 0.1210 | 0.0008 | 0.0409 | 0.1210 | AID485977 |
| [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. |
| AID1347169 | Tertiary RLuc qRT-PCR qHTS assay 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. |
| AID1347161 | Confirmatory 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. |
| AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 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. |
| 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. |
| 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. |
| 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. |
| AID485977 | Binding affinity to rat urotensin 2 receptor | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Urotensin-II receptor modulators as potential drugs. |
| AID485959 | Half life in rat | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Urotensin-II receptor modulators as potential drugs. |
| AID485958 | Oral bioavailability in rat | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Urotensin-II receptor modulators as potential drugs. |
| AID485978 | Reduction in atherosclerotic lesion size in Apo-E knockout mouse at 30 mg/kg, po qd for 10 weeks | 2010 | Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7 | Urotensin-II receptor modulators as potential drugs. |
| AID1346328 | Human UT receptor (Urotensin receptor) | 2005 | Journal of molecular and cellular cardiology, Nov, Volume: 39, Issue:5 | A role for urotensin II in restenosis following balloon angioplasty: use of a selective UT receptor blocker. |
| [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 | 6 (60.00) | 29.6817 |
| 2010's | 2 (20.00) | 24.3611 |
| 2020's | 2 (20.00) | 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 weak demand-to-supply ratio for research on this compound.
| This Compound (11.87) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 4 (36.36%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (63.64%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||