CTOP [Ligand Id: 1674] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL507214
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • MC1 receptor/Melanocortin receptor 1 in Human [ChEMBL: CHEMBL3795] [GtoPdb: 282] [UniProtKB: Q01726]
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  • μ receptor in Human [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Antagonist activity against delta opioid receptor in mouse vas deference assessed as effect on DPDPE-induced response F 4.87 pIC50 13500 nM IC50 J. Med. Chem. (2008) 51: 5866-5870 [PMID:18800771]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Displacement of [3H]DSLET from DOR in rat brain membrane measured after 2 hrs B 6.59 pKi 258 nM Ki J Med Chem (2016) 59: 9243-9254 [PMID:27676089]
ChEMBL Inhibition of [3H]-DPDPE binding to Opioid receptor delta 1 of rat brain membranes B 4.87 pIC50 13500 nM IC50 J. Med. Chem. (1986) 29: 2370-2375 [PMID:2878079]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Displacement of [3H]U69,593 from KOR in guinea pig brain membrane measured after 2 hrs B 4.83 pKi 14900 nM Ki J Med Chem (2016) 59: 9243-9254 [PMID:27676089]
MC1 receptor/Melanocortin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3795] [GtoPdb: 282] [UniProtKB: Q01726]
ChEMBL Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin. F 7 pEC50 100 nM EC50 J. Med. Chem. (2004) 47: 1514-1526 [PMID:14998337]
μ receptor in Human [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb - - 9.7 pKi - - - Mol Pharmacol (1994) 45: 330-4 [PMID:8114680]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Displacement of [3H]DAMGO from MOR in rat brain membrane measured after 2 hrs B 8.89 pKi 1.3 nM Ki J Med Chem (2016) 59: 9243-9254 [PMID:27676089]
ChEMBL Compound was evaluated for the inhibition of binding of [3H]naloxone toOpioid receptor mu 1 of rat brain membranes B 8.55 pIC50 2.8 nM IC50 J. Med. Chem. (1986) 29: 2370-2375 [PMID:2878079]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Antagonist activity against mu opioid receptor in guinea pig ileum assessed as effect on TAPP-induced response F 8.55 pIC50 2.8 nM IC50 J. Med. Chem. (2008) 51: 5866-5870 [PMID:18800771]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]