DPDPE [Ligand Id: 1608] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| ABCB1/ATP-dependent translocase ABCB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ABCB1/ATP-dependent translocase ABCB1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447] | ||||||||
| ChEMBL | Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2003) 46: 1716-1725 [PMID:12699389] |
| δ receptor/Delta-type 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 | Binding affinity against Opioid receptor delta 1 in guinea pig brain homogenates, using [3H]DPDPE as radioligand. | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (1992) 35: 4498-4500 [PMID:1333014] |
| ChEMBL | Compound was tested for the inhibition of [3H]- [D-Pen2, D-Pen5]-enkephalin (DPDPE) binding to Opioid receptor delta 1 in guinea pig brain homogenates | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (1992) 35: 1535-1541 [PMID:1315870] |
| 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 delta opioid receptor expressed in HEK293 cells by scintillation counting | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (2014) 57: 6861-6866 [PMID:25051243] |
| ChEMBL | Displacement of [3H]diprenorphine from human DOR expressed in HEK293 cells after 90 mins by liquid scintillation counting | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (2012) 55: 10292-10296 [PMID:22995061] |
| 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 cloned delta opioid receptor | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 2656-2660 [PMID:17350835] |
| ChEMBL | Binding affinity towards Opioid receptor delta 1 | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
| 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 cell membranes measured after 2 hrs by microbeta scintillation counting method | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2021) 64: 9458-9483 [PMID:34152138] |
| ChEMBL | Inhibition of binding of [3H]diprenorphine to cloned human Opioid receptor delta 1 expressed in CHO cell membrane;Range is between (1-3.9) | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
| ChEMBL | In vitro potency was measured against human Opioid receptor delta 1 | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
| ChEMBL | Displacement of [125I]-IBNalA from DOR-1 expressed in CHO cells | B | 8.75 | pKi | 1.77 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| ChEMBL | Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes. | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| 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] |
| ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membrane | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
| 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 HEK cells after 60 mins | B | 8.85 | pKi | 1.41 | nM | Ki | Eur J Med Chem (2015) 90: 742-750 [PMID:25513968] |
| ChEMBL | Displacement of [125I]-IBNtxA from DOR-1 expressed in CHO cells | B | 8.86 | pKi | 1.39 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4001-4004 [PMID:21621410] |
| 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 | Displacement of [3H]Cl-DPDPE from human DOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 8.91 | pKi | 1.24 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
| ChEMBL | Compound was evaluated for its inhibitory potency against opioid receptor delta of Guinea pig ileum | B | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (1992) 35: 2384-2391 [PMID:1320122] |
| ChEMBL | Tested for the binding affinity against the Delta opioid receptor in guinea pig brain using [3H]DPDPE | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1994) 37: 4270-4277 [PMID:7996538] |
| ChEMBL | Inhibition of human delta opioid receptor | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Binding affinity towards Opioid receptor delta 1 was determined in guinea pig whole brain using [3H][4''-Cl-Phe4]-DPDPE as radioligand | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1996) 39: 4120-4124 [PMID:8831778] |
| ChEMBL | Binding activity against human Opioid receptor delta 1 using [3H]DPDPE as a radioligand | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2002) 45: 1395-1398 [PMID:11906279] |
| ChEMBL | Inhibitory concentration was determined against delta-opioid receptor using [3H]- DPDPE radioligand | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (1995) 38: 570-579 [PMID:7853350] |
| ChEMBL | Tested for inhibitory concentration against [3H]DPDPE binding at sites of delta-opioid receptor in guinea pig brain membrane | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (1994) 37: 2856-2864 [PMID:8071934] |
| 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 | Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cells | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Nat Prod (2007) 70: 1946-1950 [PMID:18039010] |
| ChEMBL | Displacement of [3H]deltorphin-2 from human delta opioid receptor expressed in HEK293 cell membrane | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Nat Prod (2010) 73: 988-991 [PMID:20426456] |
| ChEMBL | Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membrane | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Nat Prod (2007) 70: 866-868 [PMID:17388627] |
| ChEMBL | Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK293 cells | B | 8.95 | pIC50 | 1.12 | nM | IC50 | J Nat Prod (2006) 69: 1295-1299 [PMID:16989522] |
| ChEMBL | Displacement of [125I]deltorphin 2 from human recombinant delta opioid receptor expressed in HEK cell membranes | B | 8.95 | pIC50 | 1.12 | nM | IC50 | J Nat Prod (2007) 70: 872-875 [PMID:17451272] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay | F | 9.05 | pIC50 | 0.9 | nM | IC50 | Bioorg Med Chem (2014) 22: 4694-4703 [PMID:25087049] |
| 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 delta opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation | F | 9.85 | pIC50 | 0.14 | nM | IC50 | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| ChEMBL | Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay | F | 6.9 | pEC50 | 125.4 | nM | EC50 | J Med Chem (2023) 66: 17138-17154 [PMID:38095323] |
| ChEMBL | Agonist activity at human DOR expressed in CHO-K1 cells co-expressing G-alpha15 by calcium mobilization assay | F | 7.45 | pEC50 | 35.2 | nM | EC50 | J Med Chem (2024) 67: 272-288 [PMID:38118143] |
| 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 expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (2008) 51: 4404-4411 [PMID:18637671] |
| ChEMBL | Agonist activity at human recombinant delta opioid receptor expressed in CHO cells co-expressing Galphaq66Di5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay | F | 7.8 | pEC50 | 15.85 | nM | EC50 | ACS Med Chem Lett (2015) 6: 579-583 [PMID:26005537] |
| ChEMBL | Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.82 | pEC50 | 15 | nM | EC50 | Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449] |
| 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 | Agonist activity at human DOR expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.03 | pEC50 | 9.29 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
| 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 human delta opioid receptor transfected in CHOK1 cells after 60 mins by [35S]GTPgammaS binding assay | F | 8.2 | pEC50 | 6.34 | nM | EC50 | J Nat Prod (2013) 76: 824-828 [PMID:23659286] |
| 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 CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method | F | 8.36 | pEC50 | 4.32 | nM | EC50 | Bioorg Med Chem (2022) 53: 116552-116552 [PMID:34894610] |
| ChEMBL | Antagonist activity at human recombinant delta opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of DPDPE-induced intracellular calcium mobilization | F | 8.53 | pEC50 | 2.95 | nM | EC50 | J Med Chem (2009) 52: 4068-4071 [PMID:19473027] |
| 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 delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2008) 51: 6334-6347 [PMID:18821747] |
| ChEMBL | Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2008) 51: 1369-1376 [PMID:18266313] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
| ChEMBL | Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2006) 49: 2868-2875 [PMID:16686530] |
| ChEMBL | Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2006) 49: 1773-1780 [PMID:16509592] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2011) 54: 382-386 [PMID:21128594] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.8 | pEC50 | 1.58 | nM | EC50 | J Med Chem (2011) 54: 382-386 [PMID:21128594] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay | F | 8.8 | pEC50 | 1.58 | nM | EC50 | J Med Chem (2007) 50: 2779-2786 [PMID:17516639] |
| ChEMBL | Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells | F | 8.8 | pEC50 | 1.58 | nM | EC50 | J Med Chem (2006) 49: 2868-2875 [PMID:16686530] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay | F | 8.8 | pEC50 | 1.58 | nM | EC50 | J Med Chem (2008) 51: 6334-6347 [PMID:18821747] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay | F | 8.8 | pEC50 | 1.58 | nM | EC50 | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
| ChEMBL | Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells | F | 8.8 | pEC50 | 1.58 | nM | EC50 | J Med Chem (2006) 49: 1773-1780 [PMID:16509592] |
| ChEMBL | Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay | F | 8.8 | pEC50 | -8.8 | - | logEC50 | J Med Chem (2008) 51: 1369-1376 [PMID:18266313] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting analysis | F | 8.85 | pEC50 | 1.4 | nM | EC50 | Eur J Med Chem (2023) 258: 115589-115589 [PMID:37413884] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells. | F | 8.89 | pEC50 | 1.3 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology measured over 30 mins by label free binding assay | B | 9.1 | pEC50 | 0.8 | nM | EC50 | Eur J Med Chem (2015) 92: 270-281 [PMID:25559207] |
| ChEMBL | Agonist activity at Myc-tagged delta-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis | F | 9.25 | pEC50 | 0.56 | nM | EC50 | J Med Chem (2013) 56: 3102-3114 [PMID:23477419] |
| ChEMBL | Agonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting | F | 9.85 | pEC50 | 0.14 | nM | EC50 | J Med Chem (2011) 54: 7848-7859 [PMID:21978284] |
| 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] |
| ChEMBL | Agonist activity at DOR (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 60 mins by liquid scintillation counting analysis | B | 10 | pEC50 | 0.1 | nM | EC50 | J Med Chem (2021) 64: 9458-9483 [PMID:34152138] |
| δ receptor/Delta-type 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 | Displacement of [3H]DPDPE from mouse whole brain DOR | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4895-4898 [PMID:25248680] |
| ChEMBL | Binding affinity opioid receptor | B | 6.22 | pIC50 | 609 | nM | IC50 | J Med Chem (1994) 37: 1746-1757 [PMID:8021915] |
| ChEMBL | Inhibitory concentration required for 50 percent inhibition of opioid receptor delta 1 induced contractions in mouse vas deferens (MVD) smooth muscle contraction assays | F | 8.24 | pIC50 | 5.81 | nM | IC50 | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Tested for agonist activity against delta opioid receptor mouse vas deferens | F | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (1994) 37: 2125-2128 [PMID:8035418] |
| ChEMBL | Agonist activity was evaluated in guinea pig ileum (GPI) preparations at Opioid receptor delta 1 | F | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (1997) 40: 695-704 [PMID:9057856] |
| ChEMBL | Inhibitory activity measured against Opioid receptor delta 1 using mouse vas deference assay (MVD). | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1991) 34: 1823-1830 [PMID:1648137] |
| ChEMBL | Inhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferens | F | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1994) 37: 146-150 [PMID:8289188] |
| ChEMBL | Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deference (MVD, delta receptor) | F | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
| ChEMBL | Compound was evaluated for its inhibitory potency against opioid receptor delta of Mouse vas deferens | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1992) 35: 2384-2391 [PMID:1320122] |
| ChEMBL | Agonistic activity towards Opioid receptor delta 1 as inhibitory activity towards electrically stimulated mouse vas deferens | F | 8.39 | pIC50 | 4.1 | 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 | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
| ChEMBL | Inhibitory activity of the electrically induced smooth muscle contraction of mouse vas deferens | F | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (1994) 37: 1572-1577 [PMID:8201592] |
| ChEMBL | Compound is tested in vitro in mouse vas deferens (MVD) assay mediated by Opioid receptor delta 1 | B | 8.58 | pIC50 | 2.65 | nM | IC50 | J Med Chem (1991) 34: 1656-1661 [PMID:1851843] |
| ChEMBL | Inhibitory potency against Opioid receptor delta 1 was determined in electrically induced smooth muscle contractions of mouse vas deferens (MVD) | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (1997) 40: 3957-3962 [PMID:9397176] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens | F | 8.69 | pIC50 | 2.02 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1899-1902 [PMID:22325949] |
| ChEMBL | Binding affinity opioid receptor | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (1994) 37: 1746-1757 [PMID:8021915] |
| 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] |
| ChEMBL | Effective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitro | B | 8.39 | pEC50 | 4.1 | nM | EC50 | J Med Chem (1994) 37: 1746-1757 [PMID:8021915] |
| ChEMBL | In vitro bioassay data to determine the effective concentration required for antagonistic activity against Opioid receptor delta 1 in functional assay, MVD | F | 8.39 | pEC50 | 4.1 | nM | EC50 | J Med Chem (2003) 46: 4215-4231 [PMID:13678399] |
| ChEMBL | Agonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay | F | 8.69 | pEC50 | 2.05 | nM | EC50 | Eur J Med Chem (2013) 69: 786-789 [PMID:24103580] |
| δ receptor/Delta-type opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | In Vitro evaluation for the binding affinity in homogenates of rat brain at Opioid receptor delta 1 by displacing [3H]- DSLET | B | 7.75 | pKi | 17.7 | nM | Ki | J Med Chem (1992) 35: 684-687 [PMID:1311764] |
| ChEMBL | Tested for binding affinity against delta opioid receptor by displacing [3H]- DSLET radioligand from rat brain membrane preparations | B | 7.79 | pKi | 16.4 | nM | Ki | J Med Chem (1993) 36: 3182-3187 [PMID:8230106] |
| ChEMBL | Inhibition of [3H]DTLET binding torat brain membrane Opioid receptor delta 1 | B | 7.96 | pKi | 10.9 | nM | Ki | J Med Chem (1988) 31: 1891-1897 [PMID:2845081] |
| ChEMBL | Inhibition of [3H]DSLET binding to delta 1 opioid receptors in rat brain membranes | B | 7.96 | pKi | 10.9 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Displacement of [3H]DSLET from delta opioid receptor in rat brain membrane after 2 hrs | B | 8.08 | pKi | 8.39 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1899-1902 [PMID:22325949] |
| 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 Sprague-Dawley rat delta opioid receptor by liquid scintillation counting | B | 8.57 | pKi | 2.72 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| 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 | Displacement of [3H] DPDPE from rat delta-opioid receptor extracted from CHO cell membrane assessed as inhibition constant by liquid scintillation counting analysis | B | 8.64 | pKi | 2.3 | nM | Ki | Eur J Med Chem (2024) 276: 116643-116643 [PMID:38986343] |
| ChEMBL | Inhibition of binding of radioligand [3H][p-Cl-phe]-DPDPE to Opioid receptor delta 1 in rat brain | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1997) 40: 3957-3962 [PMID:9397176] |
| ChEMBL | Evaluation for the binding affinity by competitive inhibition of [3H]- p-chloro DPDPE binding | B | 8.07 | pIC50 | 8.5 | nM | IC50 | J Med Chem (1994) 37: 1572-1577 [PMID:8201592] |
| ChEMBL | Displacement of [3H]pCl-DPDP from delta opioid receptor in rat central nervous system membrane | B | 8.22 | pIC50 | 6 | nM | IC50 | J Nat Prod (1992) 55: 380-384 [PMID:1317407] |
| ChEMBL | Inhibitory activity measured against [3H]DPDPE (Opioid receptor delta 1 ligand) in rat brain using radioreceptor binding assays. | B | 8.23 | pIC50 | 5.83 | nM | IC50 | J Med Chem (1991) 34: 1823-1830 [PMID:1648137] |
| ChEMBL | Compound was evaluated for the binding affinity in comparison with [3H]- DPDPE (opioid receptor delta selective ligand) | B | 8.23 | pIC50 | 5.83 | nM | IC50 | J Med Chem (1992) 35: 2384-2391 [PMID:1320122] |
| ChEMBL | Binding affinity towards delta opioid receptor was determined in rat brain using [H]-[p-Cl-Phe4]-DPDPE as radioligand | B | 8.24 | pIC50 | 5.8 | nM | IC50 | J Med Chem (1994) 37: 146-150 [PMID:8289188] |
| ChEMBL | Opioid receptor binding affinity in rat brain membrane preparations by the displacement of [3H]DSLET (Opioid receptor delta 1-selective radioligand) | B | 8.24 | pIC50 | 5.8 | nM | IC50 | J Med Chem (1991) 34: 1656-1661 [PMID:1851843] |
| ChEMBL | Ability to displace [3H]DPDPE from Opioid receptor delta 1 in rat brain membranes, was determined from radioreceptor assay. | B | 8.28 | pIC50 | 5.25 | nM | IC50 | J Med Chem (1990) 33: 249-253 [PMID:2153205] |
| ChEMBL | Inhibitory activity against forskolin-stimulated cAMP production in chinese hamster ovary cells expressing Opioid receptor delta 1 | F | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2027-2032 [PMID:9873480] |
| ChEMBL | Binding potency of compound in competition with [3H]DPDPE for Opioid receptor delta 1 tested in rat brain membrane | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1989) 32: 638-643 [PMID:2537426] |
| ChEMBL | Binding affinity towards Opioid receptor delta 1 using [3H]- [p-CIPhe4] DPDPE as radioligand | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2003) 46: 4215-4231 [PMID:13678399] |
| ChEMBL | Compound was evaluated for the binding affinity in comparison with [3H][p-Cl-Phe4]-DPDPE (opioid receptor delta selective ligand) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (1992) 35: 2384-2391 [PMID:1320122] |
| ChEMBL | Binding affinity was measured against Opioid receptor delta 1 using [3H]p-Cl-DPDPE as radioligand. | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (1998) 41: 4767-4776 [PMID:9822547] |
| ChEMBL | Binding affinity against rat Opioid receptor delta 1 expressed in CHO cells determined by competitive inhibition of 1 nM [3H]DPDPE. | B | 9.2 | pIC50 | 0.63 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2027-2032 [PMID:9873480] |
| 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-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | In vitro potency was measured against human Opioid receptor kappa 1 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
| ChEMBL | Inhibition of binding of [3H]diprenorphine to cloned human Opioid receptor kappa 1 expressed in CHO cell membrane | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
| 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] |
| ChEMBL | Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| ChEMBL | Binding affinity towards opioid receptor kappa 2 | B | 6.46 | pKi | >350 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
| ChEMBL | Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells. | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| Kappa-type opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Compound was tested for the inhibition of [3H]- (U69,593) binding to Opioid receptor kappa 1 in guinea pig brain homogenates | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1535-1541 [PMID:1315870] |
| ChEMBL | Binding affinity against opioid receptor kappa from guinea pig brain homogenates, using [3H]U-69593 as radioligand. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 4498-4500 [PMID:1333014] |
| ChEMBL | Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig brain membrane after 2 hrs | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1899-1902 [PMID:22325949] |
| ChEMBL | Displacement of [3H]U69593 from Sprague-Dawley rat kappa opioid receptor in guinea pig cerebella by liquid scintillation counting | B | 5.3 | pKi | >5000 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| ChEMBL | Binding affinity towards opioid receptor kappa 1 | B | 6.46 | pKi | >350 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
| ChEMBL | Tested for inhibitory concentration against [3H]U-69593 binding at sites of kappa-opioid receptor in guinea pig brain membrane | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1994) 37: 2856-2864 [PMID:8071934] |
| ChEMBL | Inhibitory concentration against Opioid receptor kappa 1 using [3H]- U-69,593 radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1995) 38: 570-579 [PMID:7853350] |
| ChEMBL | Tested for the binding affinity against the Kappa opioid receptor in guinea pig brain using [3H]U-69593 | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (1994) 37: 4270-4277 [PMID:7996538] |
| μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | In vitro potency was measured against human Opioid receptor mu 1 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1998) 41: 2631-2635 [PMID:9651168] |
| ChEMBL | Inhibition of binding of [3H]diprenorphine to cloned human Opioid receptor mu 1 expressed in CHO cell membrane | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
| 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 | Displacement of [3H]DAMGO from human recombinant Opioid receptor mu 1 on CHO cell membranes. | B | 6.3 | pKi | 504 | nM | Ki | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| ChEMBL | Displacement of [3H]DAMGO from human MOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 6.3 | pKi | 504 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 using [3H]- CTOP as radioligand | B | 6.21 | pIC50 | 610 | nM | IC50 | J Med Chem (2003) 46: 4215-4231 [PMID:13678399] |
| 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 | Stimulation of [35S]GTP-gamma-S, binding to recombinant human Opioid receptor mu 1 expressed in CHO cells | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2003) 46: 1563-1566 [PMID:12672258] |
| Mu-type opioid receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3041] [UniProtKB: P79350] | ||||||||
| ChEMBL | Binding affinity towards opioid receptor mu 2 | B | 6.34 | pKi | 460 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
| ChEMBL | Binding affinity towards opioid receptor mu 1 | B | 7.09 | pKi | 82 | nM | Ki | J Med Chem (1992) 35: 1521-1525 [PMID:1315868] |
| μ receptor/Mu-type opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Binding affinity against opioid receptor by displacing radioligand [3H]DPDPE | B | 8.53 | pKi | 2.95 | nM | Ki | J Med Chem (1994) 37: 3408-3418 [PMID:7932569] |
| ChEMBL | Inhibitory potency against Opioid receptor mu 1 was determined in electrically induced strips of guinea pig ileum (GPI) | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1997) 40: 3957-3962 [PMID:9397176] |
| μ receptor/Mu-type opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane after 2 hrs | B | 5.55 | pKi | 2820 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1899-1902 [PMID:22325949] |
| ChEMBL | Displacement of [3H]DAMGO from Sprague-Dawley rat mu opioid receptor by liquid scintillation counting | B | 5.67 | pKi | 2120 | nM | Ki | Bioorg Med Chem (2010) 18: 4975-4982 [PMID:20599386] |
| ChEMBL | In Vitro evaluation for the binding affinity in homogenates of rat brain at opioid receptor mu by displacing [3H]- DAMGO | B | 5.7 | pKi | 2018 | nM | Ki | J Med Chem (1992) 35: 684-687 [PMID:1311764] |
| ChEMBL | Tested for binding affinity against mu opioid receptor fby displacing [3H]- DAMGO radioligand from rat brain membrane preparations | B | 6.03 | pKi | 943 | nM | Ki | J Med Chem (1993) 36: 3182-3187 [PMID:8230106] |
| ChEMBL | Inhibition of [3H]DAGO binding to mu 1 opioid receptor in rat brain membranes | B | 6.06 | pKi | 873 | nM | Ki | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 1 | B | 6.06 | pKi | 873 | nM | Ki | J Med Chem (1988) 31: 1891-1897 [PMID:2845081] |
| ChEMBL | Displacement of [3H]DPDPE from rat mu opioid receptor | B | 6.21 | pKi | 610 | nM | Ki | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
| ChEMBL | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membrane | B | 6.21 | pKi | 610 | nM | Ki | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
| ChEMBL | Inhibition of binding of radioligand [3H]CTOP to Opioid receptor mu 1 in rat brain | B | 5.43 | pIC50 | 3700 | nM | IC50 | J Med Chem (1997) 40: 3957-3962 [PMID:9397176] |
| ChEMBL | Opioid receptor mu 1 binding affinity in rat brain membrane preparations by the displacement of [3H]- DAGO | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (1991) 34: 1656-1661 [PMID:1851843] |
| ChEMBL | Binding affinity towards mu opioid receptor was determined in rat brain using [3H]CTOP as radioligand | B | 6.21 | pIC50 | 620 | nM | IC50 | J Med Chem (1994) 37: 146-150 [PMID:8289188] |
| ChEMBL | Evaluation for the binding affinity by competitive inhibition of [3H]- CTOP binding | B | 6.21 | pIC50 | 620 | nM | IC50 | J Med Chem (1994) 37: 1572-1577 [PMID:8201592] |
| ChEMBL | Inhibitory activity measured against [3H]CTOP (Opioid receptor mu 1) in rat brain using radioreceptor binding assays. | B | 6.21 | pIC50 | 619 | nM | IC50 | J Med Chem (1991) 34: 1823-1830 [PMID:1648137] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]- CTOP (opioid receptor mu selective ligand) | B | 6.22 | pIC50 | 609 | nM | IC50 | J Med Chem (1992) 35: 2384-2391 [PMID:1320122] |
| ChEMBL | Binding affinity was measured against Opioid receptor mu 1 using [3H]-DAMGO as radioligand. | B | 6.22 | pIC50 | 609 | nM | IC50 | J Med Chem (1998) 41: 4767-4776 [PMID:9822547] |
| ChEMBL | Ability to displace [3H]CTOP from Opioid receptor mu 1 in rat brain membranes, was determined from radioreceptor assay | B | 6.22 | pIC50 | 609 | nM | IC50 | J Med Chem (1990) 33: 249-253 [PMID:2153205] |
| ChEMBL | The ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from rat brain membrane. | B | 6.41 | pIC50 | 385 | nM | IC50 | J Med Chem (1989) 32: 638-643 [PMID:2537426] |
| Mu-type opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | F | 6.24 | pKd | 577 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3053-3056 [PMID:10571174] |
| ChEMBL | Binding affinity against Mu opioid receptor using [35S]GTP-gamma-S, binding assay in guinea pig caudate membranes in unblocked condition | F | 6.24 | pKd | 577 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 3347-3350 [PMID:10612597] |
| ChEMBL | Compound was tested for the inhibition of [3H]- [D-Ala2, N-MePhe4, Gly5-ol]-enkephalin (DAMGO) binding to mOpioid receptor mu 1 in guinea pig brain homogenates | B | 6.09 | pKi | 810 | nM | Ki | J Med Chem (1992) 35: 1535-1541 [PMID:1315870] |
| ChEMBL | Binding affinity against opioid receptor mu in guinea pig brain homogenates, using [3H]DAMGO as radioligand. | B | 6.09 | pKi | 810 | nM | Ki | J Med Chem (1992) 35: 4498-4500 [PMID:1333014] |
| ChEMBL | Inhibitory concentration for inhibition of Opioid receptor mu 1 induced contractions in guinea pig ileum (GPI) smooth muscle assays | F | 4.94 | pIC50 | 11600 | nM | IC50 | J Med Chem (2004) 47: 1400-1412 [PMID:14998329] |
| ChEMBL | Inhibition of electrically evoked contraction of guinea pig ileum (myenteric plexus:longitudinal muscle preparation) by antagonist action at mu 1 opioid receptors | F | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (1988) 31: 374-383 [PMID:2828622] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 was determined in guinea pig whole brain using [3H]CTOP radioligand | B | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (1996) 39: 4120-4124 [PMID:8831778] |
| ChEMBL | Agonistic activity for Opioid receptor mu 1 as inhibitory activity towards electrically stimulated guinea pig ileum | F | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (1996) 39: 2081-2086 [PMID:8642567] |
| ChEMBL | Tested for agonist activity against mu opioid receptor in guinea pig ileum | F | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (1994) 37: 2125-2128 [PMID:8035418] |
| ChEMBL | The opioid activity against the mu-receptor in the isolated guinea pig ileum(GPI) | B | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (1995) 38: 1523-1537 [PMID:7739011] |
| ChEMBL | Inhibitory concentration against electrically evoked contractions of guinea pig ileum longitudinal muscle-myenteric plexus | F | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (1994) 37: 146-150 [PMID:8289188] |
| ChEMBL | Agonist activity was evaluated in guinea pig ileum (GPI) preparations at Opioid receptor mu 1 | F | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (1997) 40: 695-704 [PMID:9057856] |
| ChEMBL | Inhibitory activity of the electrically induced guinea pig ileum longitudinal muscle-myenteric plexus | F | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (1994) 37: 1572-1577 [PMID:8201592] |
| ChEMBL | Ability to inhibit electrically evoked contractions of isolated muscle preparations of guinea pig ileum (GPI, mu receptor) | F | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (2002) 45: 3746-3754 [PMID:12166947] |
| ChEMBL | Inhibitory activity measured against Opioid receptor mu 1 using guinea pig ileum assay (GPI). | B | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (1991) 34: 1823-1830 [PMID:1648137] |
| ChEMBL | Compound is tested in vitro in guinea pig ileum (GPI) assay mediated by Opioid receptor mu 1 | B | 5.26 | pIC50 | 5500 | nM | IC50 | J Med Chem (1991) 34: 1656-1661 [PMID:1851843] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 5.57 | pIC50 | 2720 | nM | IC50 | J Med Chem (2010) 53: 5491-5501 [PMID:20617791] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 5.57 | pIC50 | 2720 | nM | IC50 | J Med Chem (2009) 52: 5164-5175 [PMID:20560643] |
| ChEMBL | Tested for the binding affinity against the Mu opioid receptor in guinea pig brain using [3H]-DAMGO | B | 5.75 | pIC50 | 1760 | nM | IC50 | J Med Chem (1994) 37: 4270-4277 [PMID:7996538] |
| ChEMBL | Tested for inhibitory concentration against [3H]DAMGO binding at sites of mu-opioid receptor in guinea pig brain membrane | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1994) 37: 2856-2864 [PMID:8071934] |
| ChEMBL | Inhibitory concentration was determined against Opioid receptor mu 1 using [3H]- DAMGO radioligand | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1995) 38: 570-579 [PMID:7853350] |
| ChEMBL | Effective concentration was measured towards mu opioid receptor using guinea pig ileum (GPI, mu) bioassay in vitro | B | 5.14 | pEC50 | 7300 | nM | EC50 | J Med Chem (1994) 37: 1746-1757 [PMID:8021915] |
| ChEMBL | In vitro bioassay data to determine the effective concentration required for antagonistic activity against Opioid receptor mu 1 in functional assay, GPI | F | 5.14 | pEC50 | 7300 | nM | EC50 | J Med Chem (2003) 46: 4215-4231 [PMID:13678399] |
| NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
| ChEMBL | Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2011) 54: 6531-6537 [PMID:21866885] |
ChEMBL data shown on this page come from version 36:
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]
