β-FNA [Ligand Id: 1631] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL473136 (Beta-Funaltrexamine) |
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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 33:
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]
