CP 424391: a growth hormone secretagogue; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 216208 |
| CHEMBL ID | 113313 |
| SCHEMBL ID | 1147592 |
| MeSH ID | M0396083 |
| Synonym |
|---|
| cp 424391 |
| 2-amino-n-[(r)-2-((r)-3a-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-benzyloxymethyl-2-oxo-ethyl]-2-methyl-propionamide |
| bdbm50083974 |
| cp-424391 |
| cp-424,391 |
| cp-424391-18 |
| capromorelin |
| capimorelin |
| CHEMBL113313 , |
| 193273-66-4 |
| n-[(2r)-1-[(3ar)-3a-benzyl-2-methyl-3-oxo-6,7-dihydro-4h-pyrazolo[4,3-c]pyridin-5-yl]-1-oxo-3-phenylmethoxypropan-2-yl]-2-amino-2-methylpropanamide |
| 0mq44vun84 , |
| unii-0mq44vun84 |
| capromorelin [inn] |
| cp 424,391 |
| 329327-00-6 |
| capromorelin [green book] |
| 2-amino-n-((1r)-1-(((3ar)-3a-benzyl-2,3,3a,4,6,7-hexahydro-2-methyl-3-oxo-5h-pyrazolo(4,3-c)pyridin-5-yl)carbonyl)-2-(benzyloxy)ethyl)-2-methylpropionamide |
| propanamide, 2-amino-n-(2-(2,3,3a,4,6,7-hexahydro-2-methyl-3-oxo-3a-(phenylmethyl)-5h-pyrazolo(4,3-c)pyridin-5-yl)-2-oxo-1-((phenylmethoxy)methyl)ethyl)-2-methyl-, (r-(r*,r*))- |
| capromorelin [mi] |
| SCHEMBL1147592 |
| DTXSID5057886 , |
| AKOS027326852 |
| 2-amino-n-((r)-1-((r)-3a-benzyl-2-methyl-3-oxo-3a,4,6,7-tetrahydro-2h-pyrazolo[4,3-c]pyridin-5(3h)-yl)-3-(benzyloxy)-1-oxopropan-2-yl)-2-methylpropanamide |
| Q5036299 |
| EX-A2367 |
| DB15205 |
| n-[(2r)-1-[(3ar)-2-methyl-3-oxo-3a-(phenylmethyl)-6,7-dihydro-4h-pyrazolo[4,3-c]pyridin-5-yl]-1-oxo-3-(phenylmethoxy)propan-2-yl]-2-amino-2-methylpropanamide |
| A880277 |
| capromoreline |
| dtxcid6031673 |
| capromorelinum |
| capromorelina |
| elura |
| AC-35748 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Following initial screening and baseline blood collections, participants received ascending oral doses (20, 50 and then 100 mg at least 1-week apart) of capromorelin after pre-dose blood collection, followed by blood collections over the following 12 h for pharmacokinetic analysis and 1-week and 4-week follow-up blood collections for safety evaluations." | ( Pharmacokinetics of the ghrelin agonist capromorelin in a single ascending dose Phase-I safety trial in spinal cord-injured and able-bodied volunteers. Brown, DJ; Ellis, AG; Frauman, AG; Furness, JB; Millard, M; Zeglinski, PT, 2015) | 0.42 |
| " Pharmacokinetic behaviour was broadly similar between groups, with both exhibiting dose-dependent increases in Cmax and AUC0-∞." | ( Pharmacokinetics of the ghrelin agonist capromorelin in a single ascending dose Phase-I safety trial in spinal cord-injured and able-bodied volunteers. Brown, DJ; Ellis, AG; Frauman, AG; Furness, JB; Millard, M; Zeglinski, PT, 2015) | 0.42 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Growth hormone secretagogue receptor type 1 | Homo sapiens (human) | IC50 (µMol) | 1.0140 | 0.0004 | 0.5892 | 6.0000 | AID1505552; AID73176 |
| Growth hormone secretagogue receptor type 1 | Homo sapiens (human) | Ki | 0.0070 | 0.0002 | 0.0336 | 0.0906 | AID92297 |
| [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) |
|---|---|---|---|---|---|---|---|
| Growth hormone secretagogue receptor type 1 | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0030 | 0.0013 | 0.0154 | 0.0600 | AID1692742 |
| Growth hormone secretagogue receptor type 1 | Homo sapiens (human) | EC50 (µMol) | 0.0009 | 0.0002 | 0.0087 | 0.0660 | AID1505553 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| growth hormone secretagogue receptor activity | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| G protein-coupled receptor activity | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| growth hormone-releasing hormone receptor activity | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| peptide hormone binding | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Growth hormone secretagogue receptor type 1 | Rattus norvegicus (Norway rat) |
| plasma membrane | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| cell surface | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| neuron projection | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| membrane raft | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| synaptic membrane | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| Schaffer collateral - CA1 synapse | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| postsynapse | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| glutamatergic synapse | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| plasma membrane | Growth hormone secretagogue receptor type 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1505553 | Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists. |
| AID175851 | In vitro effective concentration required for 50% stimulation of GH release in rat pituitary cell cultures. | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery and biological characterization of capromorelin analogues with extended half-lives. |
| AID177159 | In vivo effective dose required for 50% stimulation of GH release in anesthetized rat model. | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery and biological characterization of capromorelin analogues with extended half-lives. |
| AID9720 | Plasma elimination half-life (08 h) was determined in canine following intravenous (iv) administration (1 mg/kg). | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery and biological characterization of capromorelin analogues with extended half-lives. |
| AID1692742 | Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon. |
| AID73176 | Binding affinity for human growth hormone GH secretagogue (hGHsr) receptor | 2000 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1 | Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues. |
| AID1505552 | Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists. |
| AID1505555 | Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis relative to GHRP-6 | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists. |
| AID1859422 | Stimulation of growth hormone secretion in Wistar rat pituitary cells measured after 15 mins | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | An insight into the multifunctional role of ghrelin and structure activity relationship studies of ghrelin receptor ligands with clinical trials. |
| AID8530 | Plasma clearance was determined in canine following intravenous (iv) administration of drug (1 mg/kg). | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery and biological characterization of capromorelin analogues with extended half-lives. |
| AID180671 | The effective concentration against rat pituitary cell GH release assay | 2000 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1 | Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues. |
| AID92297 | In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand. | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery and biological characterization of capromorelin analogues with extended half-lives. |
| AID18968 | Lipophilicity by octanol water distribution coefficient | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery and biological characterization of capromorelin analogues with extended half-lives. |
| AID9895 | Volume of distribution was determined in canine following intravenous (iv) administration of drug (1 mg/kg). | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Discovery and biological characterization of capromorelin analogues with extended half-lives. |
| [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 | 11 (34.38) | 29.6817 |
| 2010's | 15 (46.88) | 24.3611 |
| 2020's | 6 (18.75) | 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 (11.84) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 7 (20.59%) | 5.53% |
| Reviews | 3 (8.82%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 24 (70.59%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||