pethidine [Ligand Id: 7221] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL607 (IDS-NP-001, Isonipecaine, Meperidine, Meperidol, Pethanol, Pethidine, Pethidine dbl, Pethidineter, Renaudin) |
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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] | ||||||||
| GtoPdb | - | - | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2001) 44: 3378-90 [PMID:11585443] |
| ChEMBL | Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2001) 44: 3378-3390 [PMID:11585443] |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Displacement of [3H]WIN-35428 from dopamine transporter (DAT) | B | 4.75 | pKi | 17800 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3273-3276 [PMID:10612583] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG channel in HEK293 cells by voltage-clamp method | B | 4.12 | pIC50 | 75857.76 | nM | IC50 | Eur J Med Chem (2008) 43: 2479-2488 [PMID:18262683] |
| ChEMBL | Inhibition of human ERG | B | 4.13 | pIC50 | 74131.02 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 6.49 | pIC50 | 323.59 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand | B | 5.63 | pIC50 | 2370 | nM | IC50 | J Med Chem (2001) 44: 3378-3390 [PMID:11585443] |
| GtoPdb | - | - | 5.63 | pIC50 | 2370 | nM | IC50 | J Med Chem (2001) 44: 3378-90 [PMID:11585443] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor kappa 1 was determined in brain membrane preparations from male Hartley guinea-pigs | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1813-1818 [PMID:9873439] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 6.5 | pIC50 | 315 | nM | IC50 | J Med Chem (2001) 44: 3378-90 [PMID:11585443] |
| ChEMBL | Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand | B | 6.5 | pIC50 | 315 | nM | IC50 | J Med Chem (2001) 44: 3378-3390 [PMID:11585443] |
| ChEMBL | Agonist activity at human cloned mu opioid receptor by [35S]GTPgammaS binding assay | F | 5.03 | pEC50 | 9400 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1228-1232 [PMID:19168350] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity against mu opioid receptor was determined in brain membrane preparations from male Hartley guinea-pigs | B | 6.35 | pKi | 451 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1813-1818 [PMID:9873439] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Displacement of [3H]paroxetine from serotonin transporter (SERT) | B | 6.39 | pKi | 412 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3273-3276 [PMID:10612583] |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | B | 4.65 | pIC50 | 22250 | nM | IC50 | J Med Chem (2019) 62: 9890-9905 [PMID:31597043] |
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]
