Page last updated: 2024-12-09
necrostatin-5
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
Necrostatin-5: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 1913406 |
| CHEMBL ID | 396100 |
| SCHEMBL ID | 12682848 |
| MeSH ID | M0509603 |
Synonyms (25)
| Synonym |
|---|
| STL304760 |
| {[3-(4-methoxyphenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl}acetonitrile |
| EU-0071015 |
| CHEMDIV1_003052 |
| OPREA1_435788 |
| OPREA1_213608 |
| necrostatin-5 |
| nec-5 |
| 2-[[3,4,5,6,7,8-hexahydro-3-(4-methoxyphenyl)-4-oxo[1]benzothieno[2,3-d]pyrimidin-2-yl]thio]-acetonitrile |
| CHEMBL396100 |
| AKOS000510375 |
| 2-[[3-(4-methoxyphenyl)-4-oxo-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-2-yl]sulfanyl]acetonitrile |
| HMS595K16 |
| 337349-54-9 |
| SCHEMBL12682848 |
| DTXSID50365590 |
| 2-((3-(4-methoxyphenyl)-4-oxo-3,4,5,6,7,8-hexahydrobenzo[4,5]thieno[2,3-d]pyrimidin-2-yl)thio)acetonitrile |
| necrostatin-5, >=98% (hplc), solid |
| sr-01000428980 |
| SR-01000428980-1 |
| J-019308 |
| NCGC00387519-02 |
| 2 [[3,4,5,6,7,8-hexahydro-3-(4-methoxyphenyl)-4-oxo[1]benzothieno[2, 3- d]pyrimidin-2-yl]thio]-acetonitrile |
| CS-0086886 |
| HY-124546 |
Research Excerpts
Bioavailability
| 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 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (5)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| G | Vesicular stomatitis virus | Potency | 4.7724 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 4.7724 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 4.7724 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 4.7724 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 4.7724 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (45)
Molecular Functions (18)
Ceullar Components (22)
Bioassays (14)
| 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. |
| AID497869 | Inhibition of TNF-alpha-induced NF-kappaB activation expressed in FADD deficient human Jurkat cells at 30 uM by luciferase reporter gene assay | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Identification of RIP1 kinase as a specific cellular target of necrostatins. |
| AID497862 | Inhibition of human RIP1 K45M mutant autophosphorylation expressed in FADD deficient human Jurkat cells at 10 to 30 uM | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Identification of RIP1 kinase as a specific cellular target of necrostatins. |
| AID497866 | Inhibition of to HSP90 in FADD deficient human Jurkat cells assessed as RIP protein degradation at 30 uM by Western blot | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Identification of RIP1 kinase as a specific cellular target of necrostatins. |
| AID497854 | Inhibition of human RIP1 K45M mutant autophosphorylation expressed in Sf9 cells | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Identification of RIP1 kinase as a specific cellular target of necrostatins. |
| AID497853 | Inhibition of cellular necroptosis in TNFalpha treated FADD deficient human Jurkat cells | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Identification of RIP1 kinase as a specific cellular target of necrostatins. |
| AID497868 | Inhibition of TNF-alpha-induced NF-kappaB activation expressed in HEK293T cells at 30 uM by luciferase reporter gene assay | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Identification of RIP1 kinase as a specific cellular target of necrostatins. |
| AID497865 | Inhibition of FITC-geldanamycin binding to HSP90 in human Jurkat cell lysates at 30 uM by fluorimetric assay | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Identification of RIP1 kinase as a specific cellular target of necrostatins. |
| AID306286 | Inhibition of TNF-alpha-induced necroptosis in FADD-deficient Jurkat T cells | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5 | Structure-activity relationship analysis of a novel necroptosis inhibitor, Necrostatin-5. |
| AID497851 | Inhibition of human RIP1 K45M mutant autophosphorylation expressed in HEK293T cells | 2008 | Nature chemical biology, May, Volume: 4, Issue:5 | Identification of RIP1 kinase as a specific cellular target of necrostatins. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (6)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (33.33) | 29.6817 |
| 2010's | 2 (33.33) | 24.3611 |
| 2020's | 2 (33.33) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 17.97
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 (17.97) All Compounds (24.57) |
Study Types
| 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 | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||