Page last updated: 2024-11-12
cebranopadol
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 11848225 |
| CHEMBL ID | 2364605 |
| CHEMBL ID | 3962932 |
| CHEMBL ID | 3545616 |
| SCHEMBL ID | 566256 |
| SCHEMBL ID | 154336 |
| SCHEMBL ID | 14183935 |
| SCHEMBL ID | 10035739 |
| SCHEMBL ID | 19336241 |
| MeSH ID | M000595300 |
Synonyms (57)
| Synonym |
|---|
| cebranopadol [usan:inn] |
| 863513-91-1 |
| grt 6005 |
| grt6005 |
| spiro(cyclohexane-1,1'(3'h)-pyrano(3,4-b)indol)-4-amine, 6'-fluoro-4',9'-dihydro-n,n-dimethyl-4-phenyl-, trans- |
| cebranopadol |
| unii-7gdw9s3gn3 |
| trans-6'-fluoro-n,n-dimethyl-4-phenyl-4',9''-dihydro-3'h-spiro(cyclohexane-1,1'-pyrano(3,4-b)indol)-4-amine |
| 7gdw9s3gn3 , |
| HY-15536 |
| CS-1323 |
| cebranopadol (usan/inn) |
| D10436 |
| cebranopadol [usan] |
| cebranopadol [inn] |
| SCHEMBL566256 |
| 6-fluoro-n,n-dimethyl-1'-phenylspiro[4,9-dihydro-3h-pyrano[3,4-b]indole-1,4'-cyclohexane]-1'-amine |
| gtpl8866 |
| CHEMBL2364605 |
| grt-6005 |
| SCHEMBL154336 |
| SCHEMBL14183935 |
| SCHEMBL10035739 |
| AKOS025290738 |
| SCHEMBL19336241 |
| CHEMBL3962932 |
| CHEMBL3545616 |
| us9120797, 24 |
| us9120797, 25 |
| bdbm177926 |
| EX-A1095 |
| (1r,4r)-6'-fluoro-n,n-dimethyl-4-phenyl-4',9'-dihydro-3'h-spiro[cyclohexane-1,1'-pyrano[3,4-b]indole]-4-amine |
| bdbm50101112 |
| bdbm50101095 |
| (1r,4r)-6'-fluoro-n,n-dimethyl-4-phenyl-4',9'-dihydro-3'h-spiro[cyclohexane-1,1'-pyrano[3,4-b]indol]-4-amine |
| NCGC00378895-01 |
| 6-fluoro-n,n-dimethyl-1'-phenyl-spiro[4,9-dihydro-3h-pyrano[3,4-b]indole-1,4'-cyclohexane]-1'-amine |
| cebranopadol(grt-6005) |
| DB12830 |
| cebranopadol ((1??,4??)stereoisomer) |
| AKOS032953927 |
| 863513-93-3 |
| AS-35183 |
| BCP09612 |
| Q19596315 |
| SB16531 |
| FT-0774945 |
| F85492 |
| (1alpha,4alpha)-cebranopadol |
| MS-26183 |
| 863513-91-1 (free base) |
| cebranopadol ((1alpha,4alpha)stereoisomer) |
| NCGC00378895-02 |
| bdbm50533342 |
| grt6005 (1alpha,4alpha)stereoisomer |
| DTXSID001031965 |
| AC-36077 |
Research Excerpts
Bioavailability
| 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 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (8)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 6.0081 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 8.4866 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0007 | 0.0000 | 0.4197 | 10.0000 | AID1628147 |
| Nociceptin receptor | Homo sapiens (human) | Ki | 0.0009 | 0.0000 | 0.0337 | 0.5000 | AID1628146 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 0.0012 | 0.0000 | 0.3263 | 9.4000 | AID1628149 |
| Nociceptin receptor | Homo sapiens (human) | EC50 (µMol) | 0.0130 | 0.0001 | 0.0089 | 0.0630 | AID1628148 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (72)
Molecular Functions (26)
Ceullar Components (29)
Bioassays (17)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1628149 | Agonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility. |
| AID1628146 | Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility. |
| AID1628148 | Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility. |
| AID1628147 | Displacement of [N-allyl-2,3-3H]naloxone from recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 90 mins by scintillation counting method | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1346329 | Human kappa receptor (Opioid receptors) | 2014 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 349, Issue:3 | Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. |
| AID1346411 | Rat kappa receptor (Opioid receptors) | 2014 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 349, Issue:3 | Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. |
| AID1346400 | Rat mu receptor (Opioid receptors) | 2014 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 349, Issue:3 | Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. |
| AID1346361 | Human delta receptor (Opioid receptors) | 2014 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 349, Issue:3 | Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. |
| AID1346299 | Human NOP receptor (Opioid receptors) | 2014 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 349, Issue:3 | Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. |
| AID1346294 | Rat NOP receptor (Opioid receptors) | 2014 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 349, Issue:3 | Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. |
| AID1346364 | Human mu receptor (Opioid receptors) | 2014 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 349, Issue:3 | Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (6)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 3 (50.00) | 24.3611 |
| 2020's | 3 (50.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 40.18
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 strong demand-to-supply ratio for research on this compound.
| This Compound (40.18) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (16.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (83.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||