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];
Life Sci (1986) 38: 2221-9 [PMID:2872570]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]