Page last updated: 2024-12-10
cp 481715
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
quinoxaline-2-carboxylic acid (4-carbamoyl-1-(3-fluorobenzyl)-2,7-dihydroxy-7-methyloctyl)amide: a CCR1 antagonist and NSAID; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 5311123 |
| CHEMBL ID | 1628706 |
| SCHEMBL ID | 995030 |
| MeSH ID | M0456678 |
Synonyms (22)
| Synonym |
|---|
| cp-481,715 |
| n-[(2s,3s,5r)-5-carbamoyl-1-(3-fluorophenyl)-3,8-dihydroxy-8-methylnonan-2-yl]quinoxaline-2-carboxamide |
| cp-481715 |
| CHEMBL1628706 , |
| 2-quinoxalinecarboxamide, n-((1s,2s,4r)-4-(aminocarbonyl)-1-((3-fluorophenyl)methyl)-2,7-dihydroxy-7-methyloctyl)- |
| cp 481715 |
| 212790-31-3 |
| quinoxaline-2-carboxylic acid (4-carbamoyl-1-(3-fluorobenzyl)-2,7-dihydroxy-7-methyloctyl)amide |
| x3tda066me , |
| unii-x3tda066me |
| bdbm50398338 |
| n-((1s,2s,4r)-4-(aminocarbonyl)-1-((3-fluorophenyl)methyl)-2,7-dihydroxy-7-methyloctyl)-2-quinoxaline carboxamide |
| gtpl3497 |
| cp481715 |
| YEQJVHQCUDMXFG-FHZYATBESA-N , |
| quinoxaline-2-carboxylic acid [4(r)-carbamoyl-1(s)-(3-fluoro-benzyl)-2(s),7-dihydroxy-7-methyl-octyl]-amide |
| SCHEMBL995030 |
| DTXSID00175540 |
| Q27076895 |
| AT25906 |
| n-((2s,3s,5r)-5-carbamoyl-1-(3-fluorophenyl)-3,8-dihydroxy-8-methylnonan-2-yl)quinoxaline-2-carboxamide |
| AKOS040751285 |
Research Excerpts
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " The pharmacodynamic activity of CP-481,715 was detected ex vivo by demonstrating a dose-related and linear increase in the amount of macrophage inflammatory protein-1alpha, CCL3, required to induce CD11b upregulation." | ( Phase I evaluation of the safety, pharmacokinetics and pharmacodynamics of CP-481,715. Chow, VF; Clucas, AT; Gladue, RP; Shah, A; Zhang, YD, 2007) | 0.34 |
| "The safety and pharmacokinetic (PK)/pharmacodynamic (PD) profile of the novel CCR1 antagonist CCX354 was evaluated in double-blind, placebo-controlled, single- and multiple-dose phase I studies (1-300 mg/day oral doses)." | ( Pharmacokinetic and pharmacodynamic evaluation of the novel CCR1 antagonist CCX354 in healthy human subjects: implications for selection of clinical dose. Bekker, P; Dairaghi, DJ; Ertl, LS; Jaen, JC; Johnson, DA; Miao, S; Pennell, AM; Powers, JP; Schall, TJ; Seitz, LC; Wang, Y; Zeng, Y; Zhang, P, 2011) | 0.37 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (3)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 1.3230 | 0.0000 | 0.6902 | 10.0000 | AID707910 |
| C-C chemokine receptor type 1 | Homo sapiens (human) | IC50 (µMol) | 0.0490 | 0.0007 | 0.2002 | 2.5000 | AID1573704; AID1573705 |
| C-C chemokine receptor type 1 | Homo sapiens (human) | Ki | 0.0740 | 0.0010 | 0.0330 | 0.0740 | AID707909 |
| C-C chemokine receptor type 5 | Homo sapiens (human) | Ki | 0.0660 | 0.0021 | 0.2306 | 0.8520 | AID707904 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (45)
Molecular Functions (14)
Ceullar Components (17)
Bioassays (7)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID707904 | Binding affinity to CCR5 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Chemokine receptor antagonists. |
| AID707908 | Lipophilicity, log P of the compound | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Chemokine receptor antagonists. |
| AID1573704 | Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Discovery and optimization of pyrazole amides as antagonists of CCR1. |
| AID707910 | Binding affinity to muscarinic M2 receptor | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Chemokine receptor antagonists. |
| AID1573705 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3 | Discovery and optimization of pyrazole amides as antagonists of CCR1. |
| AID707909 | Binding affinity to CCR1 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Chemokine receptor antagonists. |
| AID1346789 | Human CCR1 (Chemokine receptors) | 2003 | The Journal of biological chemistry, Oct-17, Volume: 278, Issue:42 | CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (9)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (55.56) | 29.6817 |
| 2010's | 4 (44.44) | 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] | ||
Market Indicators
Research Demand Index: 11.89
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 (11.89) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 3 (33.33%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (66.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||