oliceridine [Ligand Id: 7334] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2443262 (Oliceridine, Olinvyk, Olynvik, TRV-130, TRV130) |
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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 HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 5 | pEC50 | >10000 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | F | 5.55 | pEC50 | 2800 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG channel expressed in HEK293 cells by whole-cell patch clamp technique | B | 5.21 | pIC50 | 6200 | nM | IC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 5 | pEC50 | >10000 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | F | 5.85 | pEC50 | 1400 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Binding affinity to human mu opioid receptor by radio-ligand binding assay | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Displacement of [3H]-Diprenorphine from human mu opiod receptor expressed in CHO cells incubated for 1 hr by competition binding assay | B | 8.84 | pKi | 1.46 | nM | Ki | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as beta-arrestin recruitment by chemiluminescence assay | B | 7.3 | pEC50 | 50.12 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay | F | 7.92 | pEC50 | 12 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | F | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | F | 8.1 | pEC50 | 7.94 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 8.17 | pEC50 | 6.7 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry | F | 8.74 | pEC50 | 1.8 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of human Nav 1.5 tonic ion channel expressed in HEK293 cells by whole-cell patch clamp technique | B | 4.78 | pIC50 | 16500 | nM | IC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Inhibition of human Nav 1.5 phasic ion channel expressed in HEK293 cells by whole-cell patch clamp technique | B | 5.33 | pIC50 | 4700 | nM | IC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
| ChEMBL | Inhibition of human Cav 1.2 ion channel expressed in HEK293 cells by whole-cell patch clamp technique | B | 4.44 | pIC50 | 36000 | nM | IC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
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]
