Page last updated: 2024-12-10
w 54011
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 5311122 |
| CHEMBL ID | 1628668 |
| SCHEMBL ID | 1843335 |
| MeSH ID | M0445346 |
Synonyms (13)
| Synonym |
|---|
| w54011 |
| n-[(4-dimethylaminophenyl)methyl]-7-methoxy-n-(4-propan-2-ylphenyl)-1,2,3,4-tetrahydronaphthalene-1-carboxamide |
| CHEMBL1628668 , |
| gtpl581 |
| DVYASSBBADJRAS-UHFFFAOYSA-N |
| n-[(4-dimethylaminophenyl)methyl]-n-(4-isopropylphenyl)-7-methoxy-1,2,3,4-tetrahydronaphthalene-1-carboxamide |
| SCHEMBL1843335 |
| NCGC00387773-01 |
| n-[(4-dimethylaminophenyl)methyl]-n-(4-isopropylphenyl)-7-methoxy-1,2,3,4-tetrahydronaphthalen-1-carboxamide |
| Q27089210 |
| EX-A7606 |
| bdbm50462086 |
| 405097-49-6 |
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 | 0.3011 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 5.3547 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 5.3547 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 5.3547 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 5.3547 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 5.3547 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| C5a anaphylatoxin chemotactic receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.0025 | 0.0020 | 0.0550 | 0.3000 | AID1393268; AID1393271 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (71)
Molecular Functions (20)
Ceullar Components (24)
Bioassays (11)
| 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. |
| 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. |
| 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. |
| AID1393270 | Half life in Wistar rat at 10 mg/kg, po or 1 mg/kg, iv | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Chemical Approaches to Modulating Complement-Mediated Diseases. |
| AID1506676 | Antagonist activity at of C5aR in in human macrophages assessed as half life of residence time for maintaining reduction in C5a-induced macrophage response | |||
| AID1393271 | Antagonist activity at C5aR1 in human neutrophils assessed as inhibition of 0.1 nM recombinant human C5a-induced intracellular calcium release | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Chemical Approaches to Modulating Complement-Mediated Diseases. |
| AID1393269 | Oral bioavailability in Wistar rat at 10 mg/kg | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Chemical Approaches to Modulating Complement-Mediated Diseases. |
| AID1393268 | Antagonist activity at C5aR1 in HMDM assessed as inhibition of 1 nM recombinant human C5a-induced intracellular calcium release preincubated for 1 hr followed by human C5a-induction and measured after 60 hrs by FLIPR assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Chemical Approaches to Modulating Complement-Mediated Diseases. |
| AID1347000 | Human C5a1 receptor (Complement peptide receptors) | 2002 | The Journal of biological chemistry, Dec-20, Volume: 277, Issue:51 | Identification of a potent and orally active non-peptide C5a receptor antagonist. |
| [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 | 1 (16.67) | 29.6817 |
| 2010's | 3 (50.00) | 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] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (16.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (83.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||