Page last updated: 2024-11-12
gyki 47261
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9927197 |
| CHEMBL ID | 197726 |
| SCHEMBL ID | 1895281 |
| MeSH ID | M0377192 |
Synonyms (11)
| Synonym |
|---|
| CHEMBL197726 |
| gyki-47261 |
| gyki 47261 , |
| SCHEMBL1895281 |
| 220445-20-5 |
| unii-05588g41r2 |
| 05588g41r2 , |
| benzenamine, 4-(8-chloro-2-methyl-11h-imidazo(1,2-c)(2,3)benzodiazepin-6-yl)- |
| NCGC00371089-01 |
| Q27236081 |
| 4-(8-chloro-2-methyl-11h-imidazo[1,2-c][2,3]benzodiazepin-6-yl)aniline |
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 (7)
Potency Measurements
| 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 | 1.0684 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 11.9877 | 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 | 11.9877 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 11.9877 | 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 (10)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| AID255730 | Effective p.o. dose tested for anticonvulsant activity using maximal electroshock seizure model in mouse (value range= 17.9-32.1 mg/kg) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Potential metabolites of a condensed 2,3-benzodiazepine derivative. |
| AID256109 | Activity tested as behavioural change in mouse at an i.p. dose of 100 mg/kg; (loss of righting reflex) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Potential metabolites of a condensed 2,3-benzodiazepine derivative. |
| AID255719 | Effective i.p. dose tested for muscle relaxant activity using inclined screen test in mouse (value range= 29.4-45.2 mg/kg) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Potential metabolites of a condensed 2,3-benzodiazepine derivative. |
| AID256108 | Activity tested as behavioural change in mouse at a p.o. dose of 200 mg/kg; (loss of righting reflex) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Potential metabolites of a condensed 2,3-benzodiazepine derivative. |
| AID255907 | Evaluated for inhibition of AMPA (5 uM) evoked spreading depression in isolated retina prepared from young chicken | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Potential metabolites of a condensed 2,3-benzodiazepine derivative. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (7)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (57.14) | 29.6817 |
| 2010's | 1 (14.29) | 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] | ||
Market Indicators
Research Demand Index: 12.72
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 (12.72) 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 | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||