felotaxel: an antineoplastic agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 6433100 |
| CHEMBL ID | 102405 |
| SCHEMBL ID | 3894792 |
| MeSH ID | M0292124 |
| Synonym |
|---|
| 3-[2-(3,4-dimethoxy-phenyl)-ethoxy]-2-(4,6-dimethyl-pyrimidin-2-yloxy)-3,3-diphenyl-propionic acid |
| bdbm50079417 |
| L017653 |
| CHEMBL102405 , |
| 3-[2-(3,4-dimethoxyphenyl)ethoxy]-2-(4,6-dimethylpyrimidin-2-yl)oxy-3,3-diphenylpropanoic acid |
| SCHEMBL3894792 |
| felotaxel |
| 2-[(4,6-dimethylpyrimidine-2-yl)oxy]-3-[2-(3,4-dimethoxyphenyl)ethoxy]-3,3-diphenylpropionic acid |
| lu224332 |
| AKOS040751783 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The purpose of this research was to evaluate the pharmacokinetic profiles of felotaxel in rats and the protein binding in plasma." | ( Preclinical pharmacokinetic analysis of felotaxel (SHR110008), a novel derivative of docetaxel, in rats and its protein binding ability in vitro. Ding, Y; Jia, Y; Liu, W; Lu, C; Ma, Z; Song, Y; Wen, A; Yang, J; Yang, L; Zhu, Y, 2012) | 0.38 |
| " Pharmacokinetic studies in animal models are the important components in clinical development of this agent." | ( Application of a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to the pharmacokinetics, tissue distribution and excretion studies of felotaxel (SHR110008) in tumor-bearing mice. Ding, L; Ding, Y; Jia, Y; Jin, X; Lu, C; Ma, Z; Wang, C; Wen, A; Yang, J; Yang, L; Zhu, Y, 2012) | 0.38 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Endothelin receptor type B | Homo sapiens (human) | Ki | 0.0071 | 0.0001 | 0.0543 | 0.3710 | AID66686 |
| Endothelin-1 receptor | Homo sapiens (human) | Ki | 0.0035 | 0.0000 | 0.4300 | 10.0000 | AID68481 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| endothelin receptor activity | Endothelin receptor type B | Homo sapiens (human) |
| protein binding | Endothelin receptor type B | Homo sapiens (human) |
| peptide hormone binding | Endothelin receptor type B | Homo sapiens (human) |
| type 1 angiotensin receptor binding | Endothelin receptor type B | Homo sapiens (human) |
| phosphatidylinositol phospholipase C activity | Endothelin-1 receptor | Homo sapiens (human) |
| endothelin receptor activity | Endothelin-1 receptor | Homo sapiens (human) |
| protein binding | Endothelin-1 receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Endothelin receptor type B | Homo sapiens (human) |
| nuclear membrane | Endothelin receptor type B | Homo sapiens (human) |
| plasma membrane | Endothelin receptor type B | Homo sapiens (human) |
| plasma membrane | Endothelin-1 receptor | Homo sapiens (human) |
| plasma membrane | Endothelin-1 receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID172174 | Percent reduction of big ET-induced blood pressure increase in drug treated rats with LU 135252 and 10 mg/Kg of compound given perorally was reported as (AUD 30 min) in mmHg(min) | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
| AID172172 | Inhibition of big ET-induced blood pressure increase in drug treated rats with LU 135252 and 10 mg/Kg of compound given perorally was reported as (AUD 30 min) in mmHg(min) | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
| AID189542 | Compound was tested for %inhibition of big ET-induced bronchospasm in guinea pigs with LU 135252 and balanced ETA/B receptor antagonists at 10 mg/kg oral dose was reported as (AUD 30 min) in mL(min) | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
| AID68481 | Inhibition of [125I]-ET-1 (ETA assay) binding to human cloned Endothelin A receptor in CHO cells | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
| AID189545 | Compound was tested for inhibition of big ET-induced bronchospasm in drug treated guinea pigs with LU 135252 and balanced ETA/B receptor antagonists at 10 mg/kg oral dose was reported as (AUD 30 min) in mL(min) | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
| AID68495 | Selectivity for Endothelin A receptor compared to Endothelin B receptor. | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
| AID66686 | Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
| [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 | 1 (20.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 4 (80.00) | 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 (12.53) 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] | ||