Page last updated: 2024-12-11
sb 273005
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 | 9868426 |
| CHEMBL ID | 86992 |
| SCHEMBL ID | 244675 |
| MeSH ID | M0379710 |
Synonyms (21)
| Synonym |
|---|
| CHEMBL86992 , |
| bdbm50083763 |
| [(s)-8-[2-(6-methylamino-pyridin-2-yl)-ethoxy]-3-oxo-2-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1h-benzo[c]azepin-4-yl]-acetic acid |
| [8-[2-(6-methylamino-pyridin-2-yl)-ethoxy]-3-oxo-2-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1h-benzo[c]azepin-4-yl]-acetic acid |
| S7540 |
| SCHEMBL244675 |
| (s)-8-[2-[6-(methylamino)pyridin-2-yl]-1-ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1h-2-benzazepine-4-acetic acid |
| 1h-2-benzazepine-4-acetic acid, 2,3,4,5-tetrahydro-8-(2-(6-(methylamino)-2-pyridinyl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-, (4s)- |
| unii-hg7my8v9aa |
| hg7my8v9aa , |
| sb-273005 |
| AKOS027323781 |
| 205678-31-5 |
| sb273005 |
| NCGC00386438-01 |
| 2-[(4s)-8-[2-[6-(methylamino)pyridin-2-yl]ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-4,5-dihydro-1h-2-benzazepin-4-yl]acetic acid |
| CCG-269246 |
| (s)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1h-benzo[c]azepin-4-yl)acetic acid |
| A924365 |
| HY-19307 |
| CS-0015050 |
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 (3)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Integrin beta-3 | Homo sapiens (human) | IC50 (µMol) | 4.0007 | 0.0001 | 0.6323 | 10.0000 | AID217306; AID217313; AID220876; AID32990; AID82356 |
| Integrin beta-3 | Homo sapiens (human) | Ki | 1.9006 | 0.0010 | 0.9845 | 9.1400 | AID217314; AID220880 |
| Integrin alpha-V | Homo sapiens (human) | IC50 (µMol) | 0.0011 | 0.0001 | 0.6256 | 10.0000 | AID217306; AID217313; AID82356 |
| Integrin alpha-V | Homo sapiens (human) | Ki | 0.0012 | 0.0010 | 0.0021 | 0.0035 | AID217314 |
| Integrin alpha-IIb | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 0.7309 | 10.0000 | AID220876; AID32990 |
| Integrin alpha-IIb | Homo sapiens (human) | Ki | 3.8000 | 0.0020 | 2.3352 | 9.1400 | AID220880 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (86)
Molecular Functions (25)
Ceullar Components (38)
Bioassays (15)
| 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. |
| AID217314 | Binding affinity for Vitronectin receptor (alpha V beta 3) | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic. |
| AID29071 | Half life period in rat | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic. |
| AID220876 | Inhibition of integrin alphaIIb-beta3 in platelet aggregation assay | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin. |
| AID217306 | Inhibition of binding to human Vitronectin receptor (integrin alphaV-beta3) | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Molecular model of the alpha(IIb)beta(3) integrin. |
| AID82356 | HEK cell adhesion mediated by alpha v beta 3 integrin | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic. |
| AID217313 | Inhibition of Vitronectin receptor, integrin alphaV-beta3 expressed in HEK 293 cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin. |
| AID32990 | Inhibition of human alphaIIb-beta3 integrin in platelet aggregation assay | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Molecular model of the alpha(IIb)beta(3) integrin. |
| AID27902 | Plasma clearance in rat | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic. |
| AID29434 | Oral bioavailability in rat | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic. |
| AID220880 | Binding affinity for alpha IIb beta-3 integrin | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic. |
| [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 | 3 (50.00) | 29.6817 |
| 2010's | 1 (16.67) | 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: 12.82
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 (12.82) 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] | ||