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ChEMBL ligand: CHEMBL634 (Afentanyl, Alfentanil, Alfentanyl, IDS-NA-014, R-39209, R-39209-) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
ChEMBL | In vitro binding activity against opioid receptor kappa using [3H]EKC) as radioligand | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1991) 34: 827-841 [PMID:1847432] |
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
ChEMBL | Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes. | B | 8.09 | pKi | 8.21 | nM | Ki | J Med Chem (1990) 33: 2876-2882 [PMID:2170652] |
ChEMBL | Displacement of [3H]DAMGO from rat brain mu opioid receptor incubated for 60 mins by microbeta scintillation counting method | B | 7.41 | pIC50 | 38.9 | nM | IC50 | Medchemcomm (2019) 10: 1187-1191 [PMID:31391893] |
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
ChEMBL | In vitro binding activity against opioid receptor mu using [3H]DAGO) as radioligand | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (1991) 34: 827-841 [PMID:1847432] |
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] | ||||||||
ChEMBL | Displacement of [3H]pentazocine from LAL/HA/BR guinea pig brain sigma1 receptor incubated for 90 mins by liquid scintillation counting method | B | 5 | pIC50 | >10000 | nM | IC50 | Medchemcomm (2019) 10: 1187-1191 [PMID:31391893] |
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]