Assay ID | Title | Year | Journal | Article |
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
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
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
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID382897 | Effect on internalization of mu opioid receptor in HEK293 cells | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
| Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues. |
AID749876 | Inhibition of mu opioid receptor in guinea pig ileum/longitudinal muscle with myenteric plexus assessed as inhibition of electrically-stimulated muscle contraction | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID408419 | Apparent permeability from apical to basolateral side of the human Caco-2 membrane | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. |
AID1252985 | Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID1667818 | Displacement of [3H]-DPDPE from Wistar rat delta opioid receptor incubated for 3 hrs by liquid scintillation counting method | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID1277617 | Displacement of [3H]DAMGO from rat cortical MOR by liquid scintillation counting method | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation. |
AID239174 | Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
| Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-]. |
AID151138 | Inhibition of Mu opioid receptor of mouse vas deferens | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID695712 | Displacement of [3H]DPDPE from delta-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID1196472 | Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology at 3.3 uM measured over 30 mins by label free binding assay relative to DPDPE | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
AID1456633 | Selectivity ratio of Ki for displacement of [3H]DPDPE from delta-opioid receptor in Wistar rat membrane to Ki for displacement of [3H]DAMGO from mu-opioid receptor in Wistar rat brain membrane | | | |
AID1917879 | Displacement of [3H]DAMGO from human cloned mu-opioid receptor by radioligand binding assay | 2022 | Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
| Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery. |
AID1196466 | Displacement of [3H]U69,593 from guinea pig cortex/cerebella kappa opioid receptor after 2 hrs by liquid scintillation counting analysis | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
AID695714 | Selectivity ratio of Ki for delta-opioid receptor to Ki for mu-opioid receptor | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID698512 | Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID1562920 | Displacement of [3H]JWH-018 from CB1R/CB2R in Wistar rat brain membranes at 10 uM after 60 mins by liquid scintillation analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors. |
AID1807976 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 0.67 to 20 nmol, icv measured after 20 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID408418 | Metabolic stability assessed as half life in human Caco-2 cell homogenate | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. |
AID382893 | Displacement of [3H]DAMGO from mu opioid receptor in human SH-SY5Y cells | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
| Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues. |
AID149817 | Displacement of [3H]Ile5,6-deltorphin II from opioid receptor delta 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID1807964 | Inhibition of electric-field induced mouse vas deferens contraction | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID398178 | Stability in rat brain homogenates assessed as degradation half life | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
| Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2. |
AID1277621 | Selectivity ratio of Ki for rat cortical DOR to Ki for rat cortical MOR | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation. |
AID749873 | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membranes | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID151432 | Concentration required for inhibition of [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | 2000 | Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
| Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids. |
AID295477 | Displacement of [3H]deltorphin2 from delta opioid receptor in rat brain membrane | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
| Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2. |
AID1456636 | Half life in Kunming mouse brain homogenate at 500 uM by RP-HPLC method | | | |
AID695713 | Displacement of [3H]diprenorphine from kappa-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID339696 | Half life in rat brain membrane homogenate | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
AID695936 | Selectivity ratio of Ki for DOP receptor expressed in CHO-K1 cells to Ki for MOP receptor expressed in CHO-K1 cells | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
| Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives. |
AID1277620 | Selectivity ratio of Ki for guinea pig KOR to Ki for rat cortical MOR | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation. |
AID151616 | Binding affinity towards Opioid receptor mu 1 | 2000 | Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
| Synthesis and binding activity of endomorphin-1 analogues containing beta-amino acids. |
AID698513 | Agonist activity at delta opioid receptor in Kunming mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction in presence of delta opioid receptor antagonist naltrindole | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID277678 | Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
| Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID1252982 | Displacement of [3H]-DAMGO from mu opioid receptor (unknown origin) transfected in HEK293 cells | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID408417 | Displacement of [3H]DAMGO from delta opioid receptor in rat brain membrane | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. |
AID339692 | Displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
AID293121 | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked muscle contractions | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
AID339693 | Selectivity ratio of Ki for displacement of [3H]DAMGO from mu opioid receptor over Ki for displacement of [3H]Ile5,6deltorphin from delta opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
AID1253002 | Antinociceptive activity in mouse assessed as inhibition of tail flick at 4 mg/kg, iv measured at 5 to 60 mins | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID1252984 | Selectivity ratio of Ki for delta opioid receptor (unknown origin) to Ki for mu opioid receptor (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID695707 | Apparent permeability across human Caco2 cells at 200 uM by LC/MS analysis | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID151447 | Inhibitory activity against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance. |
AID698516 | Agonist activity at human FLAG-tagged mu opioid receptor expressed in HEK293 cells assessed as induction of ERK1/2 phosphorylation after 10 mins by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID408424 | Agonist activity at mu opioid receptor in human SHSY5Y cells assessed as inhibition of forskolin-stimulated cAMP production | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. |
AID587666 | Agonist activity at opioid receptor in mu rat brain membrane by [35S]GTPgammaS binding assay relative to baseline in presence of opioid-selective antagonist naloxone | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
AID749871 | Inhibition of delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID1371090 | Displacement of [3H]-DPDPE from delta opioid receptor in Wistar rat brain membranes preincubated for 3 hrs measured after 1 hr by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
| Original endomorphin-1 analogues exhibit good analgesic effects. |
AID1807965 | Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID195718 | In vitro effective dose against [35S]GTP-gamma-S, binding to rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID698510 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID1196467 | Selectivity ratio of Ki for rat cortex delta opioid receptor to Ki for rat cortex mu opioid receptor | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
AID1249927 | Displacement of [3H]diprenorphine from zebrafish delta1b opioid receptor expressed in HEK293 cell membranes by radioligand displacement assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms. |
AID1807960 | Displacement of [3H]-U69593 from KOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID698520 | Half life in mouse brain homogenates | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID1249925 | Displacement of [3H]diprenorphine from zebrafish mu opioid receptor expressed in HEK293 cell membranes by radioligand displacement assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms. |
AID339690 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
AID1667822 | Half life in Kunming mouse brain homogenate at 10'-2 mol/L by RP-HPLC analysis | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID698511 | Selectivity ratio of IC50 for mu opioid receptor in guinea pig ileum to IC50 for delta opioid receptor in Kunming mouse vas deferens | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID587667 | Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay relative to baseline | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
AID1277618 | Displacement of [3H]U69,593 from guinea pig KOR after 2 hrs by liquid scintillation counting method | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation. |
AID1872050 | Stability in mouse brain homogenate assessed as half life | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
AID1456637 | Half life in Kunming mouse plasma at 500 uM by RP-HPLC method | | | |
AID277682 | Agonist activity at mu opioid receptor by inhibition of electrically evoked muscle contraction in guinea pig ileum | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
| Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID408421 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. |
AID295478 | Selectivity for rat mu opioid receptor over rat delta opioid | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
| Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2. |
AID408422 | Selectivity for rat mu opioid receptor over rat delta opioid receptor | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. |
AID587664 | Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
AID242329 | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
| Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-]. |
AID1277619 | Displacement of [3H]DPDPE from rat cortical DOR after 2.5 hrs by liquid scintillation counting method | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation. |
AID587665 | Half life in rat brain homogenate by RP-HPLC | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
AID587662 | Displacement of [3H][Ile5,6]deltorphin2 from delta opioid receptor in rat brain membrane homogenate by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
AID1252999 | Antinociceptive activity in mouse prolonged tonic phase inflammatory pain model assessed as inhibition of formalin-induced licking/biting behavior at 4 mg/kg, iv | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID277684 | Agonist activity at delta opioid receptor by inhibition of electrically evoked muscle contraction in isolated mouse vas deferens | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
| Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID1807970 | Metabolic stability in Kunming mouse serum assessed as half life measured upto 480 mins by RP-HPLC analysis | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1075901 | Half life in human plasma by RP-HPLC analysis | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
| Delivery of a lactose derivative of endomorphin 1 to the brain via the olfactory epithelial pathway. |
AID426389 | Agonist activity at delta opioid receptor in mouse vas deference assessed as inhibition of electrically-stimulated contraction | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. |
AID1807972 | Antinociceptive activity in icv dosed Kunming mouse model assessed as increase in paw withdrawal latency by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1807963 | Inhibition of electric-field induced guinea pig ileum contraction | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID295476 | Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
| Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2. |
AID151770 | Displacement of [3H]DAMGO from Opioid receptor mu 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID1808010 | Chronic antinociceptive tolerance in Kunming mouse pretreated with compound followed by repeated compound addition at 20 nmol, icv once daily for 7 days and measured after 5 mins by radiant heat paw withdrawal test | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID231320 | Relative affinity for delta and kappa opioid receptors | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID1667820 | Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID1808004 | Tolerance ratio of ED50 for Kunming mouse pretreated with 3 times ED50 of compound for 2 hrs followed by challenge with second dose of compound to ED50 for Kunming mouse pretreated with saline for 2 hrs followed by compound addition | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1807974 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 0.67 to 20 nmol, icv measured after 5 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID426387 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. |
AID1249928 | Selectivity index, ratio of Ki for zebrafish delta1a opioid receptor to Ki for zebrafish mu opioid receptor | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms. |
AID277680 | Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
| Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID195849 | In vitro percent maximal stimulation of [35S]GTP-gamma-S, binding by the compound in rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID1667824 | Antinociceptive activity in kunming mouse models assessed as inhibition of tail-flick response by tail-flick assay | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID293117 | Displacement of [3H]deltorphin 2 from delta opioid receptor in rat brain P2 synaptosome | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
AID587663 | Selectivity ratio of Ki for delta opioid receptor in rat brain to mu opioid receptor in rat brain | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
AID695715 | Selectivity ratio of Ki for kappa-opioid receptor to Ki for mu-opioid receptor | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID1252998 | Antinociceptive activity in mouse acute phase inflammatory pain model assessed as inhibition of formalin-induced licking/biting behavior at 4 mg/kg, iv | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID1808003 | Antinociceptive tolerance in Kunming mouse pretreated with 3 times ED50 of compound for 2 hrs followed by challenge with second dose of compound by radiant heat paw withdrawal test | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1807980 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 20 mins with naloxonazine followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1196465 | Displacement of [3H]DPDPE from rat cortex delta opioid receptor after 2.5 hrs by liquid scintillation counting analysis | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
AID695722 | Antinociceptive activity in Sprague-Dawley rat chronic constriction injury model assessed as paw withdrawal threshold to von Frey filament-induced pain 16 umol/kg, iv administered as bolus injection measured at 15 mins | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID398174 | Displacement of [3H][Ile5,6]deltorphin-2 from delta opioid receptor in Wistar rat brain membrane | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
| Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2. |
AID12705 | Half-life in rat brain homogenate | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID1667819 | Displacement of[3H]-U69,593 from Wistar rat kappa opioid receptor incubated for 1.5 hrs by liquid scintillation counting method | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID1807973 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 0.67 to 20 nmol, icv by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID698508 | Displacement of [3H]DPDPE from Myc-tagged delta opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID1371089 | Displacement of [3H]-DAMGO from mu opioid receptor in Wistar rat brain membranes preincubated for 1 hr measured after 1hr by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
| Original endomorphin-1 analogues exhibit good analgesic effects. |
AID151771 | Displacement of [3H]endomorphin-2 from Opioid receptor mu 1 of rat brain membranes | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID1872052 | Stability in rat plasma assessed as half life | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
AID1807982 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 30 mins with nor-BNI followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1252989 | Antinociceptive activity in mouse assessed as inhibition of tail flick at 2 to 20 nmol, icv measured after 30 mins | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID1252986 | Antinociceptive activity in icv dosed mouse assessed as inhibition of tail flick measured at 5 to 60 mins | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID1807983 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 10 micromol/kg, sc by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID751788 | Antiallodynic activity in Sprague-Dawley rat chronic constriction injury model assessed as change in ipsilateral hindpaw withdrawal threshold at 0.16 to 16 umol/kg, iv administered as single bolus dose separated by 2 to 3 days wash-out period | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Peripherally acting novel lipo-endomorphin-1 peptides in neuropathic pain without producing constipation. |
AID1807978 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 10 mins with naloxone followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID695711 | Displacement of [3H]DAMGO from mu-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID293116 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain P2 synaptosome | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
AID339695 | Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
AID1667834 | Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method relative to control | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID1196471 | Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as change in cell morphology at 3.3 uM measured over 30 mins by label free binding assay relative to DAMGO | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
AID1196475 | Half life in rat brain homogenate at 10 uM | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
AID1252988 | Antinociceptive activity in mouse assessed as inhibition of tail flick at 2 to 20 nmol, icv measured up to 30 mins relative to control | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID587661 | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane homogenate by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Design, synthesis, pharmacological evaluation, and structure-activity study of novel endomorphin analogues with multiple structural modifications. |
AID1807971 | Octanol/buffer distribution coefficient, log D of the compound at pH 7.4 by RP-HPLC analysis | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID698507 | Displacement of [3H]DAMGO from FLAG-tagged mu opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID277689 | Antinociceptive activity in Swiss Albino mouse assessed as effect on paw licking by hot plate method at 10 ug | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
| Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID149744 | Inhibition of Opioid receptor mu 1 of guinea pig ileum | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID695935 | Agonist activity at MOP receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
| Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives. |
AID398173 | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membrane | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
| Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2. |
AID1872018 | Displacement of [3H]U69593 from KOP (unknown origin) stably expressed in HEK293 cells by liquid scintillation counter analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
AID1807961 | Selectivity index, ratio of Ki for displacement of [3H]DPDPE from DOR in Wistar rat brain membranes to Ki for displacement of [3H]DAMGO from MOR in Wistar rat brain membranes | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID148592 | Displacement of [3H]dynorphin A from Opioid receptor kappa 1 of rat brain membranes (DAMGO/DADLE quenching of mu/delta receptor binding) | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID1371095 | Antinociceptive activity in Kunming mouse assessed as increase in latency to withdrawal by measuring AUC at 10 mg/kg, sc measured up to 45 mins post dose by tail-flick test | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
| Original endomorphin-1 analogues exhibit good analgesic effects. |
AID1808013 | Toxicity in icv dosed Kunming mouse assessed as inhibition of gastrointestinal transit by measuring charcoal distance travel by charcoal meal test | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1872048 | Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulation | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
AID398175 | Selectivity ratio of IC50 for delta opioid receptor to IC50 for mu opioid receptor in Wistar rat brain membrane | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
| Biological activity of endomorphin and [Dmt1]endomorphin analogs with six-membered proline surrogates in position 2. |
AID1456659 | Antinociceptive activity in mouse model of thermal-induced nociception assessed as increase in latency to tail withdrawal at 10 nmol/kg, icv measured up to 60 mins by tail flick test | | | |
AID1667825 | Antinociceptive activity in kunming mouse models assessed as maximum possible effect at 0.4 nmol, icv measured from 5 to 60 mins by warm water tail-flick assay relative to control | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID339694 | Selectivity ratio of Ki for displacement of [3H]endomorphin-2 from mu opioid receptor over Ki for displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
AID1807962 | Selectivity index, ratio of Ki for displacement of [3H]-U69593 from KOR in Wistar rat brain membranes to Ki for displacement of [3H]DAMGO from MOR in Wistar rat brain membranes | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID698515 | Agonist activity at human FLAG-tagged mu opioid receptor expressed in HEK293 cells assessed as induction of ERK1/2 phosphorylation at 10 nM after 10 mins by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID695716 | Agonist activity at mu-opioid receptor in human SH-SY5Y cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by immunoassay | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID449582 | Binding affinity to human mu opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
| Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor. |
AID1371091 | Selectivity ratio of Ki from delta opioid receptor in Wistar rat brain membranes to Ki from mu opioid receptor in Wistar rat brain membranes | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
| Original endomorphin-1 analogues exhibit good analgesic effects. |
AID1667828 | Antinociceptive activity in kunming mouse models assessed as effective dose after icv administration measured from 5 to 60 mins by warm water tail-flick assay | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID698514 | Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter relative to control | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID1872049 | Stability in mouse serum assessed as half life | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
AID1371093 | Half life in Kunming mouse plasma at 500 uM by RP-HPLC analysis | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
| Original endomorphin-1 analogues exhibit good analgesic effects. |
AID749872 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membranes | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Effect of anchoring 4-anilidopiperidines to opioid peptides. |
AID226741 | Relative inhibition of mu opioid receptor of guinea pig ileum and mouse vas deferens | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. |
AID408423 | Agonist activity at mu opioid receptor in human SHSY5Y cells assessed as inhibition of forskolin-stimulated cAMP production at 100 nM | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. |
AID1667836 | Antinociceptive activity in kunming mouse models assessed as maximum possible effect at 4 nmol, icv measured from 5 to 60 mins by warm water tail-flick assay relative to control | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID1456634 | Displacement of [3H]DAMGO from mu-opioid receptor in Wistar rat brain membrane after 1 hr by microbeta scintillation counting method | | | |
AID293118 | Selectivity for rat mu opioid receptor over rat delta opioid receptor | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
AID426390 | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated contraction | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. |
AID695938 | Apparent permeability across human Caco2 cells st 200 uM measured over 150 mins by LC/MS analysis | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
| Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives. |
AID698509 | Selectivity ratio of Ki for Myc-tagged delta opioid receptor to Ki for FLAG-tagged mu opioid receptor | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID695933 | Displacement of [3H]DPDPE from DOP receptor expressed in CHO-K1 cells after overnight incubation by beta counting method | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
| Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives. |
AID698506 | Agonist activity at delta opioid receptor in Kunming mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID1667823 | Half life in Kunming mouse serum at 10'-2 mol/L by RP-HPLC analysis | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID277691 | Antinociceptive activity in Swiss Albino mouse assessed as effect on jumping by hot plate method at 10 ug | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
| Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID1807979 | Antinociceptive activity in Kunming mouse model assessed as increase in paw withdrawal latency at 20 nmol, icv pretreated for 4 hrs with beta-FNA followed by compound addition and measured upto 10 mins by radiant heat paw withdrawal assay | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID695934 | Displacement of [3H]DAMGO from MOP receptor expressed in CHO-K1 cells after overnight incubation by beta counting method | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
| Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives. |
AID1667817 | Displacement of [3H]-DAMGO from Wistar rat mu opioid receptor incubated for 1 hr by liquid scintillation counting method | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
| Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications. |
AID277690 | Antinociceptive activity in Swiss Albino mouse assessed as effect on rearing by hot plate method at 10 ug | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
| Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2). |
AID1872053 | Stability in human plasma assessed as half life | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
AID1196468 | Selectivity ratio of Ki for guinea pig cortex/cerebella kappa opioid receptor to Ki for rat cortex mu opioid receptor | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
AID1456635 | Displacement of [3H]DPDPE from delta-opioid receptor in Wistar rat brain membrane after 3 hrs by microbeta scintillation counting method | | | |
AID1808002 | Antinociceptive tolerance in Kunming mouse pretreated with saline for 2 hrs followed by compound addition by radiant heat paw withdrawal test | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1252983 | Displacement of [3H]-DPDPE from delta opioid receptor (unknown origin) transfected in HEK293 cells | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration. |
AID339691 | Displacement of [3H]endomorphin-2 from mu opioid receptor in Wistar rat brain | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
| New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. |
AID698517 | Agonist activity at human FLAG-tagged mu opioid receptor expressed in HEK293 cells assessed as induction of ERK1/2 phosphorylation at 1 pM after 10 mins by Western blot analysis | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID1807969 | Metabolic stability in Kunming mouse brain assessed as half life measured upto 480 mins by RP-HPLC analysis | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1808015 | Toxicity in Kunming mouse model assessed as conditioned place preference time at 20 nmol, icv | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1196464 | Displacement of [3H]DAMGO from rat cortex mu opioid receptor after 30 mins by liquid scintillation counting analysis | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities. |
AID201473 | Potency for inhibition of forskolin-stimulated cyclic AMP accumulation in SH-SY5Y cells | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance. |
AID1808014 | Toxicity in Kunming mouse assessed as inhibition of gastrointestinal transit at 10 micromol/kg, sc by charcoal meal test (Rvb = 70.3 +/- 3 %) | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1808016 | Toxicity in Kunming mouse model assessed as conditioned place preference time at 10 micromol/kg, sc | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1807959 | Displacement of [3H]DPDPE from DOR in Wistar rat brain membranes measured after 3 hrs by scintillation counting method | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID293119 | Agonist activity at mu opioid receptor in Hartley guinea pig intestine assessed as inhibition of electrically evoked myenteric plexus longitudinal muscle contractions | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists. |
AID695937 | Half life in human Caco2 cell homogenate at 200 uM by LC/MS analysis | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
| Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives. |
AID1371094 | Antinociceptive activity in Kunming mouse assessed as increase in latency to withdrawal by measuring AUC at 20 nmol/kg, i.c.v measured up to 45 mins post dose by tail-flick test | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
| Original endomorphin-1 analogues exhibit good analgesic effects. |
AID695706 | Half life in human plasma at 1 mg/ml by RP-HPLC analysis | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID151468 | Binding affinity towards Opioid receptor mu 1 by displacing [3H]DAMGO in rat brain membranes. | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistance. |
AID408420 | Displacement of [3H]DAMGO from mu opioid receptor in human SHSY5Y cells | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. |
AID1807958 | Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1807966 | Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
| Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects. |
AID1371092 | Half life in Kunming mouse 15% brain homogenate at 500 uM by RP-HPLC analysis | 2017 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
| Original endomorphin-1 analogues exhibit good analgesic effects. |
AID695718 | Plasma concentration in Sprague-Dawley rat at 10 umol/kg, po from 30 to 60 mins by LC/MS analysis | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID1249926 | Displacement of [3H]diprenorphine from zebrafish delta1a opioid receptor expressed in HEK293 cell membranes by radioligand displacement assay | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms. |
AID698518 | Antinociceptive activity in icv dosed Kunming mouse assessed as inhibition of heat-induced tail flick after 5 to 60 mins | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
| A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map). |
AID1346364 | Human mu receptor (Opioid receptors) | 1997 | Nature, Apr-03, Volume: 386, Issue:6624
| A potent and selective endogenous agonist for the mu-opiate receptor. |
AID1346361 | Human delta receptor (Opioid receptors) | 1998 | FEBS letters, Nov-13, Volume: 439, Issue:1-2
| Endomorphins fully activate a cloned human mu opioid receptor. |
AID1346364 | Human mu receptor (Opioid receptors) | 1998 | FEBS letters, Nov-13, Volume: 439, Issue:1-2
| Endomorphins fully activate a cloned human mu opioid receptor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |