SDZ NKT 343: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9851211 |
| CHEMBL ID | 106092 |
| SCHEMBL ID | 17105734 |
| MeSH ID | M0292847 |
| Synonym |
|---|
| NCGC00159557-01 |
| CHEMBL106092 , |
| bdbm50066168 |
| (s)-pyrrolidine-1,2-dicarboxylic acid 2-{[(s)-1-(benzyl-methyl-carbamoyl)-2-naphthalen-2-yl-ethyl]-amide} 1-[(2-nitro-phenyl)-amide] |
| 180046-99-5 |
| sdz nkt 343 |
| sdznkt343 |
| 1-[[(2-nitrophenyl)amino]carbonyl]-l-prolyl-n-methyl-3-(2-naphthalenyl)-n-(phenylmethyl)-l-alaninamide |
| AKOS024457074 |
| DTXSID30431762 |
| SCHEMBL17105734 |
| J-011496 |
| (s)-n2-((s)-1-(benzyl(methyl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-n1-(2-nitrophenyl)pyrrolidine-1,2-dicarboxamide |
| HMS3677I22 |
| (2s)-2-n-[(2s)-1-[benzyl(methyl)amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]-1-n-(2-nitrophenyl)pyrrolidine-1,2-dicarboxamide |
| HMS3413I22 |
| l-alaninamide, 1-[[(2-nitrophenyl)amino]carbonyl]-l-prolyl-n-methyl-3-(2-naphthalenyl)-n-(phenylmethyl)- |
| 1-[[(2-nitrophenyl)amino]carbonyl]-l-prolyl-n-methyl-3-(2-naphthalenyl)-n-(phenylmethyl)-l-alaninami |
| AKOS040745360 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "3. SDZ NKT 343 caused an increase in EC50 as well as reduction in the number of binding sites (Bmax) determined for [3H]-substance P, suggesting a non-competitive interaction at the human NK1 receptor." | ( Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Brown, MC; Buchheit, KH; Campbell, EA; Docherty, R; Ewan, S; Hedley, L; James, IF; Ko, S; McIntyre, P; Urban, LA; Walpole, CS, 1998) | 1.09 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 12.5893 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 11.2202 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 14.1254 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| [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) |
|---|---|---|---|---|---|---|---|
| Substance-P receptor | Homo sapiens (human) | IC50 (µMol) | 82.4000 | 0.0000 | 0.0952 | 6.8130 | AID208422 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| tachykinin receptor activity | Substance-P receptor | Homo sapiens (human) |
| protein binding | Substance-P receptor | Homo sapiens (human) |
| substance P receptor activity | Substance-P receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Substance-P receptor | Homo sapiens (human) |
| cell surface | Substance-P receptor | Homo sapiens (human) |
| dendrite | Substance-P receptor | Homo sapiens (human) |
| sperm flagellum | Substance-P receptor | Homo sapiens (human) |
| cell body | Substance-P receptor | Homo sapiens (human) |
| sperm head | Substance-P receptor | Homo sapiens (human) |
| sperm midpiece | Substance-P receptor | Homo sapiens (human) |
| plasma membrane | Substance-P receptor | Homo sapiens (human) |
| sperm midpiece | Substance-P receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508628 | Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347154 | Primary screen GU AMC 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. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID208422 | In vitro binding affinity towards Tachykinin receptor 1 by measuring its ability to displace [3H]SP (0.6 nM) binding to membranes from Cos-7 cells transiently transfected with the hNK-1R | 1998 | Journal of medicinal chemistry, Aug-13, Volume: 41, Issue:17 | 2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models. |
| [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 | 4 (57.14) | 18.2507 |
| 2000's | 1 (14.29) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 2 (28.57) | 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 (12.59) 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 | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||