diprenorphine [Ligand Id: 1617] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL281786 (Diprenorfin, Diprenorphine, M-5050, M. 5050, M5050, M50-50 injection, Revivon) |
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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] | ||||||||
| GtoPdb | - | - | 9.3 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Binding affinity to human cloned delta opioid receptor expressed in CHO cells by radioligand displacement assay | B | 9.64 | pKi | 0.23 | nM | Ki | J Med Chem (2014) 57: 5464-5469 [PMID:24933507] |
| ChEMBL | Inhibition of Opioid receptor delta 1 by displacing 1 nM [3H]DPDPE in guinea pig brain membrane | B | 9.17 | pIC50 | 0.68 | nM | IC50 | J Med Chem (1992) 35: 4589-4594 [PMID:1335078] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Displacement of [3H]diprenorphine from human KOR expressed in HEK293T cell membranes after 120 mins by scintillation counting method | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (2019) 62: 893-907 [PMID:30543421] |
| ChEMBL | Binding affinity using [3H]diprenorphine as the radioligand against E297A mutant Opioid receptor kappa 1 in COS-7 cells | B | 9.42 | pKi | 0.38 | nM | Ki | J Med Chem (2000) 43: 1573-1576 [PMID:10780914] |
| ChEMBL | Binding affinity using [3H]diprenorphine as the radioligand against E297K mutant Opioid receptor kappa 1 in COS-7 cells | B | 9.43 | pKi | 0.37 | nM | Ki | J Med Chem (2000) 43: 1573-1576 [PMID:10780914] |
| ChEMBL | Binding affinity using [3H]diprenorphine as the radioligand against wild-type Opioid receptor kappa 1 in COS-7 cells | B | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (2000) 43: 1573-1576 [PMID:10780914] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.. The Delta Receptor (2003); Life Sci (1995) 56: PL201-PL207 [PMID:7869844]; J Pharmacol Exp Ther (1997) 282: 676-84 [PMID:9262330] |
| ChEMBL | Binding affinity to human cloned kappa opioid receptor expressed in HEK293 cells by radioligand displacement assay | B | 10.7 | pKi | 0.02 | nM | Ki | J Med Chem (2014) 57: 5464-5469 [PMID:24933507] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Dissociation constant against E203Q,D204N,D206N EL-2 Opioid receptor kappa 1 expressed in HEK cells | B | 10.3 | pKd | 0.05 | nM | Kd | J Med Chem (2000) 43: 1251-1252 [PMID:10753461] |
| ChEMBL | Dissociation constant against D216N,D217N,E218Q EL-2 Opioid receptor kappa 1 expressed in HEK cells | B | 10.3 | pKd | 0.05 | nM | Kd | J Med Chem (2000) 43: 1251-1252 [PMID:10753461] |
| ChEMBL | Dissociation constant against E203Q,D204N,D206N,E209Q EL-2 Opioid receptor kappa 1 expressed in HEK cells | B | 10.42 | pKd | 0.04 | nM | Kd | J Med Chem (2000) 43: 1251-1252 [PMID:10753461] |
| ChEMBL | Dissociation constant against wild type EL-2 Opioid receptor kappa 1 expressed in HEK cells | B | 10.54 | pKd | 0.03 | nM | Kd | J Med Chem (2000) 43: 1251-1252 [PMID:10753461] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Inhibition of opioid receptor kappa by displacing 0.5 nM [3H]bremazocine in guinea pig brain membrane | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (1992) 35: 4589-4594 [PMID:1335078] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 9.1 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Binding affinity using [3H]diprenorphine as the radioligand against K303E Opioid receptor mu 1 in COS-7 cells | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2000) 43: 1573-1576 [PMID:10780914] |
| ChEMBL | Binding affinity using [3H]diprenorphine as the radioligand against wild-type Opioid receptor mu 1 in COS-7 cells | B | 9.57 | pKi | 0.27 | nM | Ki | J Med Chem (2000) 43: 1573-1576 [PMID:10780914] |
| ChEMBL | Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
| ChEMBL | Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamido)hexyl)-amino)-6-oxohexyl)-3,3-dimethyl-3H-indol-1-ium-5-sulfonate,2,2,2-Trifluoroacetate Salt from human MOR expressed in HEK293 cells by Cheng-Prusoff analysis | B | 9.91 | pKi | 0.12 | nM | Ki | J Med Chem (2015) 58: 9754-9767 [PMID:26632862] |
| ChEMBL | Binding affinity to human cloned mu opioid receptor expressed in CHO cells by radioligand displacement assay | B | 10.15 | pKi | 0.07 | nM | Ki | J Med Chem (2014) 57: 5464-5469 [PMID:24933507] |
| Mu opioid receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3041] [UniProtKB: P79350] | ||||||||
| ChEMBL | Inhibition of 0.5 nM [3H]- Bremazocine binding to Opioid receptor mu 1 of bovine striatum membrane | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (1990) 33: 2286-2296 [PMID:2165166] |
| μ receptor in Mouse [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| GtoPdb | - | - | 10.1 | pKi | - | - | - | Mol Pharmacol (1994) 45: 330-4 [PMID:8114680] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Inhibition of opioid receptor mu by displacing 1 nM [3H]DAGO in guinea pig brain membrane | B | 9.15 | pIC50 | 0.71 | nM | IC50 | J Med Chem (1992) 35: 4589-4594 [PMID:1335078] |
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]
