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ChEMBL ligand: CHEMBL31421 |
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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]-Diprenorphine from human DOP receptor expressed in HEK293 cells by scintillation counting method | B | 7.24 | pKi | 57.1 | nM | Ki | J Med Chem (2021) 64: 7555-7564 [PMID:34008968] |
ChEMBL | Displacement of [3H]diprenorphine from human delta opioid receptor expressed in HEK293 cell membranes after 2 hrs by liquid scintillation spectrometry | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (2018) 61: 5751-5757 [PMID:29901392] |
ChEMBL | Displacement of [3H]diprenorphine from human DOR expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (2016) 59: 9255-9261 [PMID:27607020] |
ChEMBL | Displacement of [3H]diprenorphine from human cloned delta opioid receptor | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835] |
ChEMBL | Displacement of [3H]DPDPE from human DOR expressed in CHO cells | B | 8.62 | pKi | 2.4 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 666-669 [PMID:28011222] |
ChEMBL | Displacement of [3H]DPDPE from human DOR expressed in CHO cells | B | 8.77 | pKi | 1.7 | nM | Ki | Bioorg Med Chem (2016) 24: 5280-5290 [PMID:27624520] |
GtoPdb | - | - | 8.8 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Proc Natl Acad Sci USA (1983) 80: 5871-4 [PMID:6310598] |
ChEMBL | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in rat Chem-1 (RBL) cell membranes incubated for 60 mins | B | 8.88 | pKi | 1.32 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
ChEMBL | Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method | F | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2016) 59: 9255-9261 [PMID:27607020] |
ChEMBL | Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cells measured after 120 mins by scintillation counting method | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
ChEMBL | Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay | F | 9.52 | pIC50 | 0.3 | nM | IC50 | Eur J Med Chem (2017) 126: 202-217 [PMID:27776274] |
ChEMBL | Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis | F | 7.57 | pEC50 | 26.92 | nM | EC50 | Eur J Med Chem (2016) 109: 276-286 [PMID:26785295] |
ChEMBL | Agonist activity at human cloned delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding | F | 7.68 | pEC50 | 21 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835] |
ChEMBL | Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay | F | 7.77 | pEC50 | 16.98 | nM | EC50 | Bioorg Med Chem (2016) 24: 1582-1588 [PMID:26944625] |
ChEMBL | Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay | F | 7.88 | pEC50 | 13.2 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 5532-5535 [PMID:26525865] |
ChEMBL | Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay | F | 8.1 | pEC50 | 8.01 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 2927-2930 [PMID:26048798] |
ChEMBL | Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay | F | 8.19 | pEC50 | 6.4 | nM | EC50 | J Med Chem (2021) 64: 13394-13409 [PMID:34465090] |
ChEMBL | Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay | F | 8.34 | pEC50 | 4.57 | nM | EC50 | J Med Chem (2021) 64: 13394-13409 [PMID:34465090] |
ChEMBL | Agonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 8.6 | pEC50 | 2.49 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
ChEMBL | Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay | B | 9.92 | pEC50 | 0.12 | nM | EC50 | ACS Med Chem Lett (2016) 7: 391-396 [PMID:27096047] |
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
GtoPdb | - | - | 7.9 | pKi | - | - | - | Mol Pharmacol (1994) 45: 330-4 [PMID:8114680] |
ChEMBL | Agonist activity at DOR in CD1 mouse vas deferens assessed as inhibition of EFS-induced contractions incubated for 60 mins | B | 6.9 | pEC50 | 125.89 | nM | EC50 | Bioorg Med Chem (2016) 24: 2832-2842 [PMID:27234885] |
ChEMBL | Agonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2016) 59: 8381-8397 [PMID:27556704] |
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
ChEMBL | Displacement of [3H]lleDelt2 from delta opioid receptor in Wistar rat brain membranes after 45 mins by liquid scintillation counting method | B | 8.35 | pKi | 4.5 | nM | Ki | ACS Med Chem Lett (2017) 8: 449-454 [PMID:28435535] |
ChEMBL | Displacement of [3H]-DPDPE from rat delta opioid receptor expressed in CHO cells incubated for 30 mins by liquid scintillation counting method | B | 8.64 | pKi | 2.3 | nM | Ki | Eur J Med Chem (2020) 189: 112070-112070 [PMID:31982651] |
ChEMBL | Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method | F | 6.43 | pEC50 | 368 | nM | EC50 | Bioorg Med Chem (2017) 25: 2406-2422 [PMID:28314512] |
ChEMBL | Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method | F | 8.84 | pEC50 | 1.43 | nM | EC50 | Eur J Med Chem (2020) 189: 112070-112070 [PMID:31982651] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Displacement of [3H]diprenorphine from human cloned mu opioid receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835] |
ChEMBL | Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method | F | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2016) 59: 9255-9261 [PMID:27607020] |
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]