ID Source | ID |
---|---|
PubMed CID | 10486131 |
PubMed CID | 3081578 |
PubMed CID | 16133805 |
CHEMBL ID | 217379 |
CHEMBL ID | 407832 |
MeSH ID | M0006909 |
Synonym |
---|
gtpl1621 |
dynorphin a-(1-8) |
NCGC00163193-01 |
dynorphin(1-8)-oh |
tyr-gly-gly-phe-leu-arg-arg-ile-oh |
bdbm50128080 |
CHEMBL217379 , |
dynorphin a (1-8) |
MS-31830 |
HY-P2159 |
CS-0109301 |
AKOS040744586 |
l-arginine, n2-(n-(n2-(n2-(n-(n-(n-(n-l-tyrosylglycyl)glycyl)-l-phenylalanyl)-l-leucyl)-l-arginyl)-l-arginyl)-l-isoleucyl)- |
dynorphin a (1-9) |
tyr-gly-gly-phe-leu-arg-arg-ile-arg-oh |
bdbm50128088 |
CHEMBL407832 , |
(2s)-2-[[(2s,3s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[2-[[2-[[(2s)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylidene |
tyr-gly-gly-phe-leu-arg-arg-ile-arg |
dynorphin a(1-9) |
dynorphin a (swine) |
dynorphin a1-17 |
dynorphin a porcine, >=95% (hplc) |
NCGC00167144-01 |
dynorphin (1-17) |
dynorphin a (1-17) |
80448-90-4 |
unii-9m18t0td14 |
9m18t0td14 , |
Y-100015 |
dynorphin acetate |
AKOS024457469 |
dynorphin a amide, porcine |
mfcd00079857 |
JMNJYGMAUMANNW-FIXZTSJVSA-N |
bdbm50096785 |
dynorphin a (porcine) |
dyn-a17 |
porcine dynorphin a (1-17) |
dynorphin a (human) |
dynorphin a (rat) |
dynorphin a (bos taurus) |
dynorphin a (pig) |
dynorphin [mi] |
dyn a 1-17 |
dynorphin 17 |
F87314 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
glucocerebrosidase | Homo sapiens (human) | Potency | 7.9433 | AID2101 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Delta-type opioid receptor | Mus musculus (house mouse) | IC50 | 0.0397 | AID226081 |
Delta-type opioid receptor | Mus musculus (house mouse) | Ki | 0.0092 | AID149069 |
Mu-type opioid receptor | Homo sapiens (human) | Ki | 0.0229 | AID150975; AID331199 |
Delta-type opioid receptor | Homo sapiens (human) | Ki | 0.0081 | AID149069; AID331200 |
Kappa-type opioid receptor | Homo sapiens (human) | Ki | 0.0024 | AID148006; AID331198 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Mu-type opioid receptor | Homo sapiens (human) | EC50 | 0.2138 | AID1229433 |
Delta-type opioid receptor | Homo sapiens (human) | EC50 | 0.0186 | AID1229436 |
Kappa-type opioid receptor | Homo sapiens (human) | EC50 | 0.0024 | AID1171840; AID1229439; AID331201; AID375524 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347154 | Primary screen GU AMC 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 ISSN: 2211-1247 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1346329 | Human kappa receptor (Opioid receptors) | 1998 | NIDA research monograph, Mar, Volume: 178ISSN: 1046-9516 | Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. |
AID1346329 | Human kappa receptor (Opioid receptors) | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 ISSN: 0022-2623 | Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues. |
AID1346361 | Human delta receptor (Opioid receptors) | 1998 | NIDA research monograph, Mar, Volume: 178ISSN: 1046-9516 | Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. |
AID1346329 | Human kappa receptor (Opioid receptors) | 1995 | Proceedings of the National Academy of Sciences of the United States of America, Jul-18, Volume: 92, Issue:15 ISSN: 0027-8424 | kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system. |
AID1346364 | Human mu receptor (Opioid receptors) | 1998 | NIDA research monograph, Mar, Volume: 178ISSN: 1046-9516 | Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. |
AID1346341 | Mouse kappa receptor (Opioid receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Jul-15, Volume: 90, Issue:14 ISSN: 0027-8424 | Cloning and functional comparison of kappa and delta opioid receptors from mouse brain. |
AID150975 | In vitro binding affinity to human Opioid receptor mu 1 on CHO cell membranes using [3H]diprenorphine displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 ISSN: 0022-2623 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID149069 | In vitro binding affinity to human Opioid receptor delta 1 on CHO cell membranes using [3H]diprenorphine displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 ISSN: 0022-2623 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID228157 | Binding affinity towards human kappa,mu,delta receptors was calculated as the ratio; 1/7.7/1.8 | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 ISSN: 0022-2623 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID148006 | In vitro binding affinity towards human Opioid receptor kappa 1 on CHO cell membranes using [3H]diprenorphine displacement. | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 ISSN: 0022-2623 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID228160 | Binding affinity towards human kappa,mu,delta receptors was calculated as the ratio; 1/9.5/3.9 | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 ISSN: 0022-2623 | Structure-activity relationships of dynorphin a analogues modified in the address sequence. |
AID152408 | Opioid receptors antagonist activity in smooth-muscle tissue of guinea pig ileum (GPI) | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID761674 | Displacement of [131I]-[D-Ala2,4'-I-Phe8]alpha-Neoendorphin from opioid receptor in CD-1 mouse brain after 90 mins by competitive binding assay | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 ISSN: 1464-3405 | Sandmeyer reaction repurposed for the site-selective, non-oxidizing radioiodination of fully-deprotected peptides: studies on the endogenous opioid peptide α-neoendorphin. |
AID150232 | Opioid receptors antagonist activity in smooth-muscle tissue of guinea pig ileum (GPI) in presence of NLX | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID149732 | Binding affinity against Opioid receptor mu 1 in guinea pig brain homogenate using [3H]- PL-17 as radioligand | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID152409 | Opioid receptors antagonist activity in smooth-muscle tissue of guinea pig ileum (GPI) in presence of CTAP | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID1229436 | Agonist activity at human recombinant delta opioid receptor expressed in CHO cells co-expressing Galphaq66Di5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 ISSN: 1948-5875 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
AID331203 | Displacement of [3H]diprenorphine from human kappa/mu opioid chimera 4 receptor | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 ISSN: 1464-3405 | Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. |
AID331199 | Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO-K1 cells | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 ISSN: 1464-3405 | Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. |
AID149847 | Selectivity for kappa and mu opioid receptors of guinea pig brain and ileum respectively | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. |
AID149619 | Binding affinity against Opioid receptor delta 1 in guinea pig brain homogenate using [3H]- DPDPE as radioligand | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID331202 | Displacement of [3H]diprenorphine from human kappa/mu opioid chimera 3 receptor | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 ISSN: 1464-3405 | Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. |
AID1229438 | Intrinsic activity at human recombinant delta opioid receptor expressed in CHO cells co-expressing Galphaq66Di5 assessed as efficacy ratio by measuring stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay relative to DPDPE | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 ISSN: 1948-5875 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
AID150250 | Opioid receptors antagonist activity in smooth-muscle tissue mouse vas deferens (MVD) in presence of NLX | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID226072 | Inhibition of [3H]PL-17 binding to mu opioid receptor of guinea pig brain homogenate | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. |
AID331198 | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO-K1 cells | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 ISSN: 1464-3405 | Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. |
AID1229439 | Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 ISSN: 1948-5875 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
AID226071 | Inhibition of [3H]DPDPE binding to delta opioid receptor of guinea pig brain homogenate | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. |
AID331201 | Agonist activity at human kappa opioid receptor transfected in CHO cells by [35S]GTP-gamma-S binding assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 ISSN: 1464-3405 | Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. |
AID375531 | Antagonist activity at human recombinant kappa opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dynorphin A-induced intracellular calcium mobilization at up to 10 uM | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 ISSN: 1520-4804 | Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists. |
AID232185 | Ratio of guinea pig brain Vs peripheral guinea pig ileum selectivies at kappa and mu opioid receptor | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID150249 | Opioid receptors antagonist activity in smooth-muscle tissue mouse vas deferens (MVD) in presence of ICI | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID1171840 | Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 ISSN: 1520-4804 | Synthesis and κ-opioid receptor activity of furan-substituted salvinorin A analogues. |
AID331200 | Displacement of [3H]diprenorphine from human delta opioid receptor expressed in CHO-K1 cells | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 ISSN: 1464-3405 | Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. |
AID1229435 | Intrinsic activity at human recombinant mu opioid receptor expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as efficacy ratio by measuring stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay relative to EM | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 ISSN: 1948-5875 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
AID1229433 | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells co-expressing C-terminally modified GGalphaqi5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 ISSN: 1948-5875 | Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines. |
AID150248 | Opioid receptors antagonist activity in smooth-muscle tissue mouse vas deferens (MVD) in presence of CTAP | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID147934 | Relative affinity for delta and kappa opioid receptors of guinea pig brain homogenate | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. |
AID226076 | Inhibition of mu-selective antagonist binding to opioid receptor of guinea pig ileum | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. |
AID226081 | Inhibition of delta-selective antagonist binding to opioid receptor of mouse vas dferens | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. |
AID141519 | Relative affinity for mu and kappa opioid receptors of guinea pig brain homogenate | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. |
AID148554 | Binding affinity against Opioid receptor kappa 1 in guinea pig brain homogenate using [3H]- U-69593 as radioligand | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID375524 | Antagonist activity at human recombinant kappa opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dynorphin A-induced intracellular calcium mobilization | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 ISSN: 1520-4804 | Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists. |
AID150247 | Opioid receptors antagonist activity in smooth-muscle tissue mouse vas deferens (MVD) | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogues. |
AID226073 | Inhibition of [3H]U-69593 binding to kappa opioid receptor of guinea pig brain homogenate | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 ISSN: 0022-2623 | Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs. |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 8 (29.63) | 18.7374 |
1990's | 10 (37.04) | 18.2507 |
2000's | 4 (14.81) | 29.6817 |
2010's | 3 (11.11) | 24.3611 |
2020's | 2 (7.41) | 2.80 |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 1 (3.33%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 29 (96.67%) | 84.16% |
Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
---|---|---|---|---|---|---|---|---|---|---|---|---|
Burns | 0 | 1995 | 1995 | 29.0 | low | 0 | 0 | 1 | 0 | 0 | 0 | |
Injuries, Spinal Cord | 0 | 1985 | 1985 | 39.0 | low | 0 | 1 | 0 | 0 | 0 | 0 | |
Muscle Contraction | 0 | 2003 | 2003 | 21.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Polycystic Ovarian Syndrome | 0 | 1995 | 1995 | 29.0 | low | 1 | 0 | 1 | 0 | 0 | 0 | |
Polycystic Ovary Syndrome | 0 | 1995 | 1995 | 29.0 | low | 1 | 0 | 1 | 0 | 0 | 0 | |
Spinal Cord Injuries | 0 | 1985 | 1985 | 39.0 | low | 0 | 1 | 0 | 0 | 0 | 0 | |
Addiction, Opioid | 0 | 1998 | 1998 | 26.0 | low | 0 | 0 | 1 | 0 | 0 | 0 | |
Chemical Dependence | 0 | 1998 | 1998 | 26.0 | low | 0 | 0 | 1 | 0 | 0 | 0 | |
Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Disease Models, Animal | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Muscle Contraction | 0 | 2003 | 2003 | 21.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Opioid-Related Disorders | 0 | 1998 | 1998 | 26.0 | low | 0 | 0 | 1 | 0 | 0 | 0 | |
Substance-Related Disorders | 0 | 1998 | 1998 | 26.0 | low | 0 | 0 | 1 | 0 | 0 | 0 | |
Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Muscle Contraction | 0 | 1990 | 1993 | 32.5 | medium | 0 | 0 | 2 | 0 | 0 | 0 |