DADLE [Ligand Id: 1607] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL340032 (DADLE) |
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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 | Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
| GtoPdb | - | - | 9.2 | pKi | 0.63 | nM | Ki | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in DOR/G beta1 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assay | B | 5.86 | pEC50 | 1380.38 | nM | EC50 | Eur J Med Chem (2019) 168: 189-198 [PMID:30822708] |
| ChEMBL | Agonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay | F | 10.7 | pEC50 | 0.02 | nM | EC50 | RSC Med Chem (2020) 11: 896-904 [PMID:33479684] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| GtoPdb | - | - | 9.1 | pKi | - | - | - | Mol Pharmacol (1994) 45: 330-4 [PMID:8114680] |
| ChEMBL | Agonistic activity towards Opioid receptor delta 1 as inhibitory activity towards electrically stimulated mouse vas deferens | F | 6.35 | pIC50 | 447 | nM | IC50 | J Med Chem (1996) 39: 2081-2086 [PMID:8642567] |
| ChEMBL | Opioid activity against delta-receptor of isolated mouse vas deferens(MVD) at 30 uM | B | 6.35 | pIC50 | 447 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem (2014) 22: 2208-2219 [PMID:24613457] |
| ChEMBL | Inhibitory potency against delta Opioid receptor delta 1 in longitudinal muscle preparation of mouse vas deferens | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (1981) 24: 1119-1124 [PMID:6276540] |
| ChEMBL | Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 9.57 | pIC50 | 0.27 | nM | IC50 | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Affinity against the Opioid receptor delta 1 | B | 8.68 | pKd | 2.1 | nM | Kd | J Med Chem (1986) 29: 531-537 [PMID:3007760] |
| ChEMBL | Inhibition of [3H]DSLET binding to delta 1 opioid receptors in rat brain membranes | B | 8.11 | pKi | 7.7 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Binding affinity against Opioid receptor delta 1 in P2 membrane preparation of rat brain by [3H]DADLE displacement. | B | 9.59 | pKi | 0.26 | nM | Ki | J Med Chem (1991) 34: 1350-1355 [PMID:1849997] |
| ChEMBL | Inhibition of [3H]- DADLE binding to Rat brain Opioid receptor delta 1 | B | 8.77 | pIC50 | 1.71 | nM | IC50 | J Med Chem (1996) 39: 2081-2086 [PMID:8642567] |
| ChEMBL | Inhibition of [3H]DADLE radioligand binding to rat brain opioid receptor delta 1. | B | 8.77 | pIC50 | 1.71 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Compound was evaluated for Opioid receptor kappa 1 affinity against the receptor site model site 4(kappa) | B | 6.2 | pKd | 625 | nM | Kd | J Med Chem (1986) 29: 531-537 [PMID:3007760] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Inhibition of [3H]- U69,593 binding to Guinea pig Opioid receptor kappa 1 | B | 5.36 | pIC50 | 4404 | nM | IC50 | J Med Chem (1996) 39: 2081-2086 [PMID:8642567] |
| ChEMBL | Inhibition of [3H]-U-69,593 radioligand binding to Guinea pig Opioid receptor kappa 1; not determined | B | 8.77 | pIC50 | 1.71 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 8.7 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to MOR/beta-arrestin-2 assessed as increase in MOR/beta-arrestin-2 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assay | B | 5.86 | pEC50 | 1380.38 | nM | EC50 | Eur J Med Chem (2019) 168: 189-198 [PMID:30822708] |
| ChEMBL | Agonist activity at Rluc-tagged MOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in MOR/G beta1 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assay | B | 6.89 | pEC50 | 128.82 | nM | EC50 | Eur J Med Chem (2019) 168: 189-198 [PMID:30822708] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Opioid receptor mu 2 affinity against the receptor site model site 2(mu2) | B | 7.66 | pKd | 22 | nM | Kd | J Med Chem (1986) 29: 531-537 [PMID:3007760] |
| ChEMBL | Opioid receptor mu 1 affinity against the receptor site model site 1 (mu1) | B | 9.05 | pKd | 0.9 | nM | Kd | J Med Chem (1986) 29: 531-537 [PMID:3007760] |
| ChEMBL | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
| ChEMBL | Ability to inhibit the binding of [3H]-DAGO to Opioid receptor mu 1 in rat brain membranes | B | 8.08 | pKi | 8.4 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Binding affinity against Opioid receptor mu 1 in P2 membrane preparation of rat brain by [3H]DAGO displacement. | B | 8.09 | pKi | 8.16 | nM | Ki | J Med Chem (1991) 34: 1350-1355 [PMID:1849997] |
| ChEMBL | Inhibition of [3H]- DAMGO binding to Rat brain Opioid receptor mu 1 | B | 7.38 | pIC50 | 41.9 | nM | IC50 | J Med Chem (1996) 39: 2081-2086 [PMID:8642567] |
| 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 brain membranes after 1 hr | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem (2014) 22: 2208-2219 [PMID:24613457] |
| ChEMBL | Inhibitory potency against Opioid receptor mu 1 in longitudinal muscle preparation of guinea pig ileum | B | 7.32 | pIC50 | 47.8 | nM | IC50 | J Med Chem (1981) 24: 1119-1124 [PMID:6276540] |
| ChEMBL | Agonistic activity for Opioid receptor mu 1 as inhibitory activity towards electrically stimulated guinea pig ileum | F | 7.54 | pIC50 | 28.8 | nM | IC50 | J Med Chem (1996) 39: 2081-2086 [PMID:8642567] |
| ChEMBL | The opioid activity against the mu-receptor in the isolated guinea pig ileum(GPI) | B | 7.54 | pIC50 | 28.8 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
| ChEMBL | Agonist activity at mu opioid receptor in Hartley guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | B | 7.87 | pIC50 | 13.39 | nM | IC50 | Bioorg Med Chem (2014) 22: 2208-2219 [PMID:24613457] |
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]
