achalensolide: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 21634938 |
| CHEMBL ID | 190054 |
| MeSH ID | M0519761 |
| Synonym |
|---|
| ACON1_000437 |
| MEGXP0_001629 |
| NCGC00169080-01 |
| BRD-K35557514-001-01-0 |
| CHEMBL190054 |
| achalensolide |
| (3ar,5s,5as,9ar)-5,8-dimethyl-1-methylidene-4,5,5a,6,9,9a-hexahydro-3ah-azuleno[6,5-b]furan-2,7-dione |
| NCGC00169080-02 |
| AKOS040734186 |
| 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 | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Nuclear factor NF-kappa-B p105 subunit | Homo sapiens (human) | IC100 (µMol) | 50.0000 | 10.0000 | 10.0000 | 10.0000 | AID242927 |
| Nuclear factor NF-kappa-B p100 subunit | Homo sapiens (human) | IC100 (µMol) | 50.0000 | 10.0000 | 10.0000 | 10.0000 | AID242927 |
| Transcription factor p65 | Homo sapiens (human) | IC100 (µMol) | 50.0000 | 5.0000 | 9.0000 | 10.0000 | AID242927; AID262798 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| 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. |
| 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. |
| 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. |
| 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. |
| AID243231 | Concentration required for complete inhibition of Nuclear factor kappa B DNA binding | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Quantitative structure-activity relationship of sesquiterpene lactones as inhibitors of the transcription factor NF-kappaB. |
| AID242927 | Concentration required for complete inhibition of Nuclear factor kappa B DNA binding | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Quantitative structure-activity relationship of sesquiterpene lactones as inhibitors of the transcription factor NF-kappaB. |
| AID262798 | Inhibition of NF-kappaB DNA binding by EMSA | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Development of a structural model for NF-kappaB inhibition of sesquiterpene lactones using self-organizing neural networks. |
| [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 | 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] | ||
| 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] | ||