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]
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 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]