β-FNA [Ligand Id: 1631] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL473136 (Beta-Funaltrexamine)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Displacement of [3H]NTI from monocloned delta opioid receptor expressed in CHO cells B 7.56 pKi 27.78 nM Ki J Med Chem (2009) 52: 1416-1427 [PMID:19199782]
ChEMBL Displacement of [3H]NTI from delta opioid receptor expressed in CHO cells B 7.56 pKi 27.78 nM Ki Bioorg Med Chem Lett (2009) 19: 1825-1829 [PMID:19217280]
ChEMBL Compound was evaluated for binding affinity against [3H]- Cl-DPDPE labeled Opioid receptor delta 1 in guinea-pig brain homogenate. B 7.65 pKi 22.4 nM Ki Bioorg Med Chem Lett (1996) 6: 167-172
GtoPdb - - 7.9 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]norBNI from monocloned kappa opioid receptor expressed in CHO cells B 9.03 pKi 0.94 nM Ki J Med Chem (2009) 52: 1416-1427 [PMID:19199782]
ChEMBL Displacement of [3H]norBNI from kappa opioid receptor expressed in CHO cells B 9.03 pKi 0.94 nM Ki Bioorg Med Chem Lett (2009) 19: 1825-1829 [PMID:19217280]
GtoPdb - - 9.7 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Compound was evaluated for binding affinity against [3H]- bremazocine labeled kappa2 opioid receptor in guinea-pig brain homogenate. B 7.18 pKi 66.5 nM Ki Bioorg Med Chem Lett (1996) 6: 167-172
ChEMBL Compound was evaluated for binding affinity against [3H]- U-69593 labeled kappa1 opioid receptor in guinea-pig brain homogenate. B 9.05 pKi 0.9 nM Ki Bioorg Med Chem Lett (1996) 6: 167-172
ChEMBL Displacement of [3H]U69593 from KOR in guinea pig brain membrane B 9.05 pKi 0.9 nM Ki J Med Chem (2012) 55: 9868-9874 [PMID:23043264]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]naloxone from monocloned mu opioid receptor expressed in CHO cells B 9.39 pKi 0.41 nM Ki J Med Chem (2009) 52: 1416-1427 [PMID:19199782]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells B 9.39 pKi 0.41 nM Ki Bioorg Med Chem Lett (2009) 19: 1825-1829 [PMID:19217280]
GtoPdb - - 9.5 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
GtoPdb - - 9.5 pKi - - - Mol Pharmacol (1994) 45: 330-4 [PMID:8114680]
ChEMBL Inhibitory concentration against mu-opioid receptor in mouse vas deferens B 7.09 pIC50 82 nM IC50 J Med Chem (1993) 36: 3669-3673 [PMID:8246236]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Compound was evaluated for binding affinity against [3H]- DAMGO labeled mu opioid receptor in guinea-pig brain homogenate. B 9.4 pKi 0.4 nM Ki Bioorg Med Chem Lett (1996) 6: 167-172
ChEMBL Displacement of [3H]DAMGO from MOR in guinea pig brain membrane B 9.4 pKi 0.4 nM Ki J Med Chem (2012) 55: 9868-9874 [PMID:23043264]
ChEMBL Inhibitory concentration against mu-opioid receptor in guinea pig ileum B 8.32 pIC50 4.8 nM IC50 J Med Chem (1993) 36: 3669-3673 [PMID:8246236]
ChEMBL Displacement of beta-[3H]FNA from mu opioid receptor in guinea pig brain membrane B 8.66 pIC50 2.2 nM IC50 J Med Chem (2009) 52: 7372-7375 [PMID:19621878]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]