nalorphine [Ligand Id: 1629] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL415284 (Nalorfina, Nalorphine, Nalorphine serb) |
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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]Naltrindole form human delta opioid receptor expressed in CHO cells | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| GtoPdb | - | - | 7.4 | 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 | Binding affinity to human kappa opioid receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2016) 59: 810-840 [PMID:26390077] |
| GtoPdb | - | - | 9.1 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; J Pharmacol Exp Ther (1997) 282: 676-84 [PMID:9262330] |
| ChEMBL | Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells | B | 9.42 | pKi | 0.38 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity to Opioid receptor kappa 1 in guinea pig cortex using [3H]EKC as radioligand | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1988) 31: 555-560 [PMID:2831363] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 8.9 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Binding affinity to human mu opioid receptor | B | 9.44 | pKi | 0.36 | nM | Ki | J Med Chem (2016) 59: 810-840 [PMID:26390077] |
| ChEMBL | Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells | B | 9.72 | pKi | 0.19 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Binding affinity to Opioid receptor mu 1 in rat brain using [3H]-NAL as radioligand | B | 8.19 | pKi | 6.5 | nM | Ki | J Med Chem (1988) 31: 555-560 [PMID:2831363] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| ChEMBL | Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| ChEMBL | Inhibition of specific binding of [3H]3-PPP to sigma binding site in Guinea pig brain membranes | B | 5.55 | pIC50 | 2850 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| ChEMBL | Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| ChEMBL | Inhibition of specific binding of [125I]PIPAG to sigma receptor in Guinea pig brain membranes | B | 6.13 | pIC50 | 735 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| ChEMBL | Inhibition of specific binding of [3H]DTG to sigma receptor in Guinea pig brain membranes | B | 6.2 | pIC50 | 625 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| ChEMBL | Inhibition of specific binding of [3H]3-PPP to sigma receptor in Guinea pig brain membranes | B | 7.03 | pIC50 | 93 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
| ChEMBL | Inhibition of specific binding of [3H]NANM of sigma receptor in Guinea pig brain membranes | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (1992) 35: 4683-4689 [PMID:1469697] |
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]
