nalfurafine [Ligand Id: 1651] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267495 (MT-9938, Nalfurafine) |
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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 | 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 | 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 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 | 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 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]
