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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 |
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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]