oglemilast: a PDE4 inhibitor and NSAID; no further info available 1/2006 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 11387409 |
| CHEMBL ID | 4297520 |
| SCHEMBL ID | 220245 |
| MeSH ID | M0493520 |
| Synonym |
|---|
| HY-15178 |
| grc 3886 |
| 778576-62-8 |
| oglemilast |
| 67gxq6wcc6 , |
| grc-3886 |
| oglemilast [inn] |
| grc3886 |
| unii-67gxq6wcc6 |
| n-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)-8-(methylsulfonamido)dibenzo[b,d]furan-1-carboxamide |
| AKOS016005519 |
| CS-0844 |
| SCHEMBL220245 |
| grc 3845 |
| oglemilast [who-dd] |
| n-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)-8-((methylsulfonyl)amino)dibenzo(b,d)furan-1-carboxamide |
| NCGC00379066-01 |
| DB12375 |
| BCP21392 |
| n-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)-8-(methanesulfonamido)dibenzofuran-1-carboxamide |
| Q27264129 |
| CHEMBL4297520 |
| F84855 |
| MS-29580 |
| DTXSID70999058 |
| n-(3,5-dichloropyridin-4(1h)-ylidene)-4-(difluoromethoxy)-8-[(methanesulfonyl)amino]dibenzo[b,d]furan-1-carboxamide |
| 4-difluoromethoxy-8-methanesulfonylamino-dibenzofuran-1-carboxylic acid (3,5-dichloro-pyridin-4-yl)-amide |
| A853039 |
| okfdrahpfkmajh-uhfffaoysa-n |
| 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 |
| 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 | 0.3379 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 3.3786 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 11.9877 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 3.3786 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.3786 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.3786 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.3786 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Homo sapiens (human) | IC50 (µMol) | 0.1660 | 0.0000 | 1.1463 | 10.0000 | AID1619495 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| 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. |
| 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. |
| 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. |
| AID1713838 | Antiinflammatory activity in Swiss albino mouse model of LPS-induced sepsis assessed as reduction in TNFalpha production at 1 mg/kg, po administered 30 mins before LPS stimulation and measured after 90 min by ELISA relative to control | 2016 | Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22 | In vivo effective dibenzo[b,d]furan-1-yl-thiazoles as novel PDE-4 inhibitors. |
| AID1713836 | Antiinflammatory activity in Swiss albino mouse model of LPS-induced sepsis assessed as reduction in TNFalpha production at 10 mg/kg, po administered 30 mins before LPS stimulation and measured after 90 min by ELISA relative to control | 2016 | Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22 | In vivo effective dibenzo[b,d]furan-1-yl-thiazoles as novel PDE-4 inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (20.00) | 29.6817 |
| 2010's | 2 (40.00) | 24.3611 |
| 2020's | 2 (40.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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 (18.47) All Compounds (24.57) |
| 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 | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||