OC 144-093: inhibits P-glycoprotein-mediated drug resistance; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 6450807 |
| CHEMBL ID | 313113 |
| MeSH ID | M0365040 |
| Synonym |
|---|
| CHEMBL313113 , |
| ont 093 |
| 4-[2-[4-[(e)-3-ethoxyprop-1-enyl]phenyl]-4-[4-(propan-2-ylamino)phenyl]-1h-imidazol-5-yl]-n-propan-2-ylaniline |
| oc 144-093 |
| unii-pk2wd2xc83 |
| pk2wd2xc83 , |
| 216227-54-2 |
| benzenamine, 4,4'-(2-(4-((1e)-3-ethoxy-1-propenyl]phenyl)-1h-imidazole-4,5-diyl)bis(n-(1-methylethyl)- |
| ont-093 |
| (e)-4,4'-(2-(4-(3-ethoxyprop-1-en-1-yl)phenyl)-1h-imidazole-4,5-diyl)bis(n-isopropylaniline) |
| oc-144-093 |
| ontogen |
| bdbm50485462 |
| BCP24637 |
| ont093 |
| DB14069 |
| oc-144093 |
| benzenamine, 4,4'-(2-(4-((1e)-3-ethoxy-1-propenyl)phenyl)-1h-imidazole-4,5-diyl)bis(n-(1-methylethyl)- |
| 1166871-26-6 |
| benzenamine, 4-(2-(4-((1e)-3-ethoxy-1-propen-1-yl)phenyl)-4-(4-((1-methylethyl)amino)phenyl)-1h-imidazol-5-yl)-n-(1-methylethyl)- |
| 4-(2-(4-((e)-3-ethoxyprop-1-enyl)phenyl)-4-(4-(propan-2-ylamino)phenyl)-1h-imidazol-5-yl)-n-propan-2-ylaniline |
| HY-15134 |
| CS-0003784 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The MDR modulator, OC144-093, is a potential candidate for use in cancer therapy and exhibits potent biological activity in vitro and in vivo when combined with anticancer agents such as paclitaxel." | ( Drug interaction studies between paclitaxel (Taxol) and OC144-093--a new modulator of MDR in cancer chemotherapy. Bally, MB; Denyssevych, T; Dixon, R; Guns, ES; Mayer, L, ) | 0.13 |
| " The purpose of this study was to determine the degree of enhancement of the oral uptake of docetaxel on combination with orally administered OC144-093, a potent P-gp inhibitor." | ( Oral bioavailability of docetaxel in combination with OC144-093 (ONT-093). Beijnen, JH; Bosch, TM; Fitzpatrick, A; Kuppens, IE; Rosing, H; Schellens, JH; van Maanen, MJ, 2005) | 0.33 |
| "Doses of ONT-093 achieving serum concentrations associated with biological activity were well tolerated in combination with standard doses of paclitaxel." | ( A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Chi, KN; Chia, SK; Dixon, R; Gelmon, KA; Newman, MJ; Sikic, B; Wacher, VJ, 2005) | 0.33 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Elimination properties of paclitaxel were affected only upon multiple dosing of OC 144-093." | ( Drug interaction studies between paclitaxel (Taxol) and OC144-093--a new modulator of MDR in cancer chemotherapy. Bally, MB; Denyssevych, T; Dixon, R; Guns, ES; Mayer, L, ) | 0.36 |
| " The compound is also being evaluated for its potential enhancement of the oral bioavailability of drugs that are P-glycoprotein substrates requiring either high dosage forms or intravenous administration, and for the potential improvement of central nervous system penetration of P-glycoprotein substrate drugs." | ( ONT-093 (Ontogen). Folkes, A; Mistry, P, 2002) | 0.31 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 (µMol) | 0.0316 | 0.0002 | 2.3185 | 10.0000 | AID672543 |
| [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) |
|---|---|---|---|---|---|---|---|
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | ED50 | 0.0500 | 0.0500 | 1.5250 | 3.0000 | AID45816 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cytoplasm | ATP-dependent translocase ABCB1 | Homo sapiens (human) |
| plasma membrane | ATP-dependent translocase ABCB1 | Homo sapiens (human) |
| cell surface | ATP-dependent translocase ABCB1 | Homo sapiens (human) |
| membrane | ATP-dependent translocase ABCB1 | Homo sapiens (human) |
| apical plasma membrane | ATP-dependent translocase ABCB1 | Homo sapiens (human) |
| extracellular exosome | ATP-dependent translocase ABCB1 | Homo sapiens (human) |
| external side of apical plasma membrane | ATP-dependent translocase ABCB1 | Homo sapiens (human) |
| plasma membrane | ATP-dependent translocase ABCB1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID10112 | Half life in Dog plasma at a dosage 5 mg/kg after intravenous administration | 2000 | Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23 | 2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 2. |
| AID89353 | Compound concentration in plasma of healthy human (male) after 3-4h of 400 mg dose of compound given orally | 2000 | Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23 | 2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 2. |
| AID9496 | Oral bioavailability in dog (dose 10 mg/kg) | 2000 | Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23 | 2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 2. |
| AID45816 | Modulation of Pgp (P-glycoprotein) mediated multidrug resistance in CEM / VLB 1000 cell line | 2000 | Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23 | 2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 2. |
| AID672543 | Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein. |
| [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 | 8 (88.89) | 29.6817 |
| 2010's | 1 (11.11) | 24.3611 |
| 2020's | 0 (0.00) | 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 weak demand-to-supply ratio for research on this compound.
| This Compound (11.99) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (18.18%) | 5.53% |
| Reviews | 3 (27.27%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (54.55%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||