Page last updated: 2024-11-12
ly2033298
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 | 11536903 |
| CHEMBL ID | 3770346 |
| SCHEMBL ID | 2911831 |
| MeSH ID | M0525002 |
Synonyms (29)
| Synonym |
|---|
| 3-amino-5-chloro-n-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamide |
| 886047-13-8 |
| AKOS016002828 |
| 3-amino-5-chloro-n-cyclopropyl-6-methoxy-4-methyl-thieno[2,3-b]pyridine-2-carboxamide |
| ly2033298 |
| ly 2033298 |
| gtpl3262 |
| ly-2033298 |
| 3-amino-5-chloro-n-cyclopropyl-6-methoxy-4-methylthieno[4,5-e]pyridine-2-carboxamide |
| 3-amino-5-chloro-6-methoxy-4-methyl-thieno[2,3-b]pyridine-2-carboxylic acid cyclopropylamide |
| CTEGQKDJTBWFHW-UHFFFAOYSA-N , |
| SCHEMBL2911831 |
| c13h14cln3o2s |
| DTXSID10468233 |
| CHEMBL3770346 , |
| mfcd12912423 |
| ly2033298, >=98% (hplc) |
| NCGC00485302-01 |
| bdbm50249030 |
| DS-12966 |
| Q27082550 |
| ly2033298;ly-2033298 |
| C76948 |
| A861711 |
| unii-5yg6jk4ecm |
| 3-amino-5-chloro-n-cyclopropyl-6-methoxy-4-methylthieno(2,3-b)pyridine-2-carboxamide |
| thieno(2,3-b)pyridine-2-carboxamide, 3-amino-5-chloro-n-cyclopropyl-6-methoxy-4-methyl- |
| 5yg6jk4ecm , |
| IUE , |
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)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 1.6604 | 0.0000 | 0.6902 | 10.0000 | AID1474765; AID1474766 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.2250 | 0.0000 | 0.9905 | 10.0000 | AID1366204 |
| Cytochrome P450 3A4 | Homo sapiens (human) | EC50 (µMol) | 0.2250 | 0.0001 | 0.2328 | 3.2000 | AID1366204 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Other Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Kb | 0.2000 | 0.2000 | 0.2000 | 0.2000 | AID1513640 |
| Cannabinoid receptor 1 | Mus musculus (house mouse) | Kb | 0.2000 | 0.2000 | 0.2000 | 0.2000 | AID1513640 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (35)
Molecular Functions (26)
Ceullar Components (16)
Bioassays (11)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| AID1474766 | Displacement of [3H]NMS from wild-type human mAChR2 expressed in Flp-in-CHO cell membranes in presence of mAChR2 agonist xanomeline after 90 mins by scintillation counting analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. |
| AID1474765 | Displacement of [3H]NMS from wild-type human mAChR2 expressed in Flp-In-CHO cell membranes in presence of mAChR2 agonist acetylcholine after 90 mins by scintillation counting analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. |
| AID1513640 | Positive allosteric modulation of human M4 AchR expressed in CHO cells assessed as increase in acteylcholine-induced calcium mobilization by FLIPR assay | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1 | Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts. |
| AID1366204 | Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M |
| AID1345465 | Human M4 receptor (Acetylcholine receptors (muscarinic)) | 2008 | Proceedings of the National Academy of Sciences of the United States of America, Aug-05, Volume: 105, Issue:31 | Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia. |
| AID1345326 | Human M2 receptor (Acetylcholine receptors (muscarinic)) | 2012 | Molecular pharmacology, Jan, Volume: 81, Issue:1 | Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (8)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (12.50) | 29.6817 |
| 2010's | 5 (62.50) | 24.3611 |
| 2020's | 2 (25.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 22.54
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 (22.54) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (25.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (75.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||