nalfurafine [Ligand Id: 1651] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267495 (MT-9938, Nalfurafina, Nalfurafine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CX3CR1/C-X3-C chemokine receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4843] [GtoPdb: 74] [UniProtKB: P49238] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Displacement of [3H]U-69-593 from human DOR expressed in HEK293 cell membrane | B | 7.44 | pKi | 36.5 | nM | Ki | Bioorg Med Chem Lett (2022) 59: 128527-128527 [PMID:35007722] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 7.13 | pEC50 | 74.1 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4980-4983 [PMID:25283554] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in mouse brain membranes without cerebellum | B | 7.29 | pKi | 51.3 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4980-4983 [PMID:25283554] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting | B | 9.43 | pKi | 0.37 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| GtoPdb | - | - | 10.1 | pKd | - | - | - | J Pharmacol Exp Ther (2005) 312: 220-30 [PMID:15383632] |
| ChEMBL | Binding affinity to kappa opioid receptor (unknown origin) | B | 6.77 | pKi | 170 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
| ChEMBL | Binding affinity to kappa opioid receptor | B | 9.64 | pKi | 0.23 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 2689-2692 [PMID:22445285] |
| ChEMBL | Binding affinity to kappa opioid receptor (unknown origin) | B | 9.64 | pKi | 0.23 | nM | Ki | Bioorg Med Chem (2013) 21: 3032-3050 [PMID:23623711] |
| ChEMBL | Displacement of [3H]DPDPE from human KOR expressed in HEK293 cell membrane | B | 10.72 | pKi | 0.02 | nM | Ki | Bioorg Med Chem Lett (2022) 59: 128527-128527 [PMID:35007722] |
| ChEMBL | Agonist activity at FLAG-tagged human kappa opioid receptor expressed in HEK293 cells assessed as increase in beta-arrestin mediated p38 phosphorylation after 5 mins by Western blot analysis | B | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at FLAG-tagged human kappa opioid receptor expressed in HEK293 cells assessed as increase in ERK1/2 phosphorylation after 5 mins by Western blot analysis | B | 8.85 | pEC50 | 1.4 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 10.3 | pEC50 | 0.05 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4980-4983 [PMID:25283554] |
| ChEMBL | Agonist activity at kappa opioid receptor in human HEK293 cells after 30 mins by [35S]GTPgammaS binding assay | F | 10.47 | pEC50 | 0.03 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 10.6 | pEC50 | 0.03 | nM | EC50 | Bioorg Med Chem (2008) 16: 1279-1286 [PMID:17981041] |
| κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Agonist activity at KOR receptor in mouse vas deferens assessed as inhibition of electrically evoked vas deferens contraction | F | 10.44 | pIC50 | 0.04 | nM | IC50 | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Agonist activity at GFP-tagged rat kappa opioid receptor expressed in HEK293 cells assessed as increase in beta-arrestin mediated p38 phosphorylation after 5 mins by Western blot analysis | B | 8.28 | pEC50 | 5.2 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at GFP-tagged rat kappa opioid receptor expressed in HEK293 cells assessed as increase in ERK1/2 phosphorylation after 5 mins by Western blot analysis | B | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | B | 9.65 | pKi | 0.23 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5035-5038 [PMID:20685120] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum | B | 9.65 | pKi | 0.23 | nM | Ki | Bioorg Med Chem (2011) 19: 1205-1221 [PMID:21256034] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig cerebellum | B | 9.74 | pKi | 0.18 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4980-4983 [PMID:25283554] |
| ChEMBL | Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting | B | 9.77 | pKi | 0.17 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
| mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Inhibition of ERK1 phosphorylation (unknown origin) | B | 9.26 | pEC50 | 0.55 | nM | EC50 | Eur J Med Chem (2019) 183: 111701-111701 [PMID:31550662] |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Inhibition of ERK2 phosphorylation (unknown origin) | B | 9.26 | pEC50 | 0.55 | nM | EC50 | Eur J Med Chem (2019) 183: 111701-111701 [PMID:31550662] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cell membrane | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem Lett (2022) 59: 128527-128527 [PMID:35007722] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 9.14 | pEC50 | 0.72 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4980-4983 [PMID:25283554] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in mouse brain membranes without cerebellum | B | 9.37 | pKi | 0.43 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4980-4983 [PMID:25283554] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain | B | 9.24 | pKi | 0.58 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5035-5038 [PMID:20685120] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain | B | 9.24 | pKi | 0.58 | nM | Ki | Bioorg Med Chem (2011) 19: 1205-1221 [PMID:21256034] |
| ChEMBL | Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting | B | 9.41 | pKi | 0.39 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
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]
