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ChEMBL ligand: CHEMBL281786 (Diprenorfin, Diprenorphine, M-5050, M. 5050, M5050, Revivon) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]