UFP-512 [Ligand Id: 9006] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL442577 (UFP-512)
  • δ receptor in Human [GtoPdb: 317] [UniProtKB: P41143]
  • 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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  • 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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  • κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor in Human [GtoPdb: 317] [UniProtKB: P41143]
GtoPdb Measuring displacement of [3H]-diprenorphine in vitro - 10.2 pKi - - - Peptides (2008) 29: 93-103 [PMID:18069089]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Antagonist activity at delta opioid receptor in mouse vas deferens assessed as effect on deltorphin 2-induced response F 9.9 pKd 0.13 nM Kd J. Med. Chem. (2008) 51: 5109-5117 [PMID:18680274]
ChEMBL Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction F 5.76 pIC50 1724 nM IC50 J. Med. Chem. (2008) 51: 5109-5117 [PMID:18680274]
ChEMBL In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD) F 9.92 pIC50 0.12 nM IC50 J. Med. Chem. (2002) 45: 5556-5563 [PMID:12459023]
ChEMBL Agonist activity at delta opioid receptor in mouse vas deference F 9.92 pIC50 0.12 nM IC50 Bioorg. Med. Chem. (2010) 18: 6024-6030 [PMID:20637637]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Inhibition of [3H]DPDPE binding to Opioid receptor delta 1 of rat brain P2 synaptosomes B 9.35 pKi 0.44 nM Ki J. Med. Chem. (2002) 45: 5556-5563 [PMID:12459023]
ChEMBL Displacement of [3H]deltorphin2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane B 9.35 pKi 0.44 nM Ki J. Med. Chem. (2008) 51: 5109-5117 [PMID:18680274]
ChEMBL Displacement of [3H]deltorphin 2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane B 9.36 pKi 0.44 nM Ki Bioorg. Med. Chem. (2010) 18: 6024-6030 [PMID:20637637]
μ receptor in Human [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb Measuring displacement of [3H]-diprenorphine in vitro - 8 pKi - - - Peptides (2008) 29: 93-103 [PMID:18069089]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Inhibition of [3H]DAGO binding to Opioid receptor mu 1 of rat brain P2 synaptosomes B 7.27 pKi 53.9 nM Ki J. Med. Chem. (2002) 45: 5556-5563 [PMID:12459023]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane B 7.27 pKi 53.9 nM Ki J. Med. Chem. (2008) 51: 5109-5117 [PMID:18680274]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane B 7.27 pKi 53.9 nM Ki Bioorg. Med. Chem. (2010) 18: 6024-6030 [PMID:20637637]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL In vitro inhibitory activity against electrically evoked contractions of guinea pig ileum (GPI) F 5.76 pIC50 1724 nM IC50 J. Med. Chem. (2002) 45: 5556-5563 [PMID:12459023]
ChEMBL Agonist activity at mu opioid receptor in Hartley guinea pig small intestine F 5.76 pIC50 1724 nM IC50 Bioorg. Med. Chem. (2010) 18: 6024-6030 [PMID:20637637]
Mu-opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5430] [UniProtKB: Q8CGM4]
ChEMBL Agonist activity at mu opioid receptor in Hartley guinea pig ileum myenteric plexus longitudinal muscle assessed as inhibition of electrically-stimulated muscle contraction F 9.92 pIC50 0.12 nM IC50 J. Med. Chem. (2008) 51: 5109-5117 [PMID:18680274]
κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
GtoPdb Measuring displacement of [3H]-diprenorphine in vitro - 6.66 pKi - - - Peptides (2008) 29: 93-103 [PMID:18069089]

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]