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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 |
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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 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]