| AID1401122 | Displacement of [3H]DAMGO from mu-opioid receptor in guinea pig brain membranes after 30 mins by scintillation counting method | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Selective kappa opioid antagonists for treatment of addiction, are we there yet? |
| AID1872115 | Binding affinity to human KOP stably expressed in CHO cell membrane assessed as [35S]GTPgammaS binding incubated for 90 mins 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. |
| AID757452 | Neurotoxicity in C57BL/6J mouse assessed as sedative effect at 10 to 60 mg/kg, po after 60 mins by rotarod test | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID1630475 | Binding affinity to DOR (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID757459 | Antinociceptive activity in C57BL/6J mouse at 1 to 60 mg/kg, po after 60 mins by warm water tail withdrawal assay | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID1872121 | Displacement of [3H]diprenorphine from rat KOP stably expressed in CHO cell membrane | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID727343 | Displacement of [3H]DAMGO from rat cloned MOR expressed in CHO cells after 90 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of κ opioid receptor antagonists. |
| AID375494 | Displacement of [3H]diprenorphine from human cloned mu receptor by cell based assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID375495 | Displacement of [3H]diprenorphine from human cloned delta receptor by cell based assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID727471 | Displacement of DPDPE from DOR in guinea pig brain membrane fraction after 30 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of κ opioid receptor antagonists. |
| AID1872119 | Displacement of [3H]DAMGO from rat MOP stably expressed in CHO cell membrane | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID727337 | Antinociceptive activity in icv dosed C57B1/6J mouse assessed as tail withdrawal latency measured in every 10 mins for 1 hr by warm water tail withdrawal assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of κ opioid receptor antagonists. |
| AID1872129 | Antinociceptive activity in icv dosed C57BL/6J mouse assessed as tail withdrawal latency from warm water | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1872117 | Displacement of [3H]DPDPE from mouse DOP stably expressed in CHO cell membrane incubated for 90 mins by 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. |
| AID375488 | Binding affinity to kappa opioid receptor in guinea pig brain membrane | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID1401123 | Displacement of [3H]DPDPE from delta-opioid receptor in guinea pig brain membranes after 30 mins by scintillation counting method | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Selective kappa opioid antagonists for treatment of addiction, are we there yet? |
| AID757449 | Prevention of cocaine-induced reinstatement of extinguished cocaine seeking behavior in C57BL/6J mouse at 30 to 60 mg/kg, po qd for 2 days followed by additional cycle of cocaine place conditioning at 30 mins post last dose measured on day 3 | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID1630474 | Binding affinity to MOR (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID727345 | Displacement of [3H]diprenorphine from rat cloned KOR expressed in CHO cells after 90 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of κ opioid receptor antagonists. |
| AID757455 | Antinociceptive activity in C57BL/6J mouse at 60 mg/kg, po after 140 mins by warm water tail withdrawal assay | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID757456 | Antagonist activity at kappa opioid receptor in po dosed C57BL/6J mouse assessed as inhibition of po dosed U50,488-induced antinociception effect incubated for 3 hrs prior to testing by warm water tail withdrawal assay | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID1630477 | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID1630478 | Displacement of [3H]diprenorphine from human DOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID757458 | Antinociceptive activity in C57BL/6J mouse at 0.3 mg/kg, po after 60 mins by warm water tail withdrawal assay | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID375493 | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor by cell based assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID757460 | Antinociceptive activity in po dosed C57BL/6J mouse after 40 mins by warm water tail withdrawal assay | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID727344 | Displacement of [3H]DPDPE from mouse cloned DOR expressed in CHO cells after 90 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of κ opioid receptor antagonists. |
| AID1872128 | Toxicity in icv dosed C57BL/6J mouse assessed as antinociceptive activity tolerance | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1872116 | Displacement of [3H]DAMGO from rat MOP stably expressed in CHO cell membrane incubated for 90 mins by 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. |
| AID375497 | Antagonist activity at human cloned kappa opioid receptor assessed as inhibition of 50 nM U50488H-stimulated GTPgammaS binding by cell based assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID727470 | Displacement of DAGO from MOR in guinea pig brain membrane fraction after 30 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of κ opioid receptor antagonists. |
| AID375498 | Antagonist activity at human cloned mu opioid receptor assessed as inhibition of 100 nM loperamide-stimulated GTPgammaS binding by cell based assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID1872056 | Half life in mouse liver microsomes | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| AID1401121 | Displacement of [3H]CI-977 from kappa opioid receptor in guinea pig brain membranes after 30 mins by scintillation counting method | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Selective kappa opioid antagonists for treatment of addiction, are we there yet? |
| AID375496 | Ratio of Ki for human cloned mu opioid receptor to Ki for human cloned kappa opioid receptor | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID757457 | Antinociceptive activity in C57BL/6J mouse at 1 to 30 mg/kg, po after 120 mins by warm water tail withdrawal assay | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID1401124 | Antagonist activity at KOR in Japanese white rabbit vas deferens assessed as inhibition of asimadoline-induced suppression of electric field stimulated twitch response after 30 mins | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Selective kappa opioid antagonists for treatment of addiction, are we there yet? |
| AID375492 | Antagonist activity at kappa opioid receptor in rabbit vas deferens assessed as reversal of asimadoline-suppressed electrically-stimulated twitch response | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID1872104 | Binding affinity to human MOP stably expressed in CHO cell membrane assessed as [35S]GTPgammaS binding incubated for 90 mins 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. |
| AID757451 | Prevention of stress-induced reinstatement of extinguished cocaine seeking behavior in C57BL/6J mouse at 60 mg/kg, po qd for 2 days measured 3 hrs post last dose by forced swim test | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID1630476 | Antagonist activity against KOR in rabbit vas deferens smooth muscles assessed as inhibition of asimadoline-induced response | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID1872118 | Displacement of dynorphin A-(1-13) amide (Dyn A-(1-13) amide) from rat KOP stably expressed in CHO cell membrane incubated for 90 mins by 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. |
| AID375491 | Ratio of IC50 for mu opioid receptor in guinea pig brain membrane to IC50 for kappa opioid receptor in guinea pig brain membrane | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID757450 | Prevention of stress-induced reinstatement of extinguished cocaine cocaine seeking behavior in C57BL/6J mouse at 30 mg/kg, po qd for 2 days measured 3 hrs post last dose by forced swim test | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID375489 | Binding affinity to mu opioid receptor in guinea pig brain membrane | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID1630479 | Displacement of [3H]U69,593 from human KOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID375490 | Binding affinity to delta opioid receptor in guinea pig brain membrane | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. |
| AID757454 | Antagonist activity at kappa opioid receptor in po dosed C57BL/6J mouse assessed as inhibition of icv dosed U50,488-induced antinociception effect incubated for 3 hrs prior to testing by warm water tail withdrawal assay | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3
| The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior. |
| AID727472 | Displacement of [3H]Cl-977 from KOR in guinea pig brain membrane fraction after 30 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of κ opioid receptor antagonists. |
| AID1630473 | Binding affinity to KOR (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-d-Pro-Phe-Trp] (CJ-15,208). |
| AID1872127 | Antinociceptive activity in icv dosed C57BL/6J mouse assessed as tail withdrawal latency from warm water measured after 1 hr for every 10 mins | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
| Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural Sources. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |