DADLE [Ligand Id: 1607] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL340032 (DADLE)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]