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 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]
