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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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GPCRdb ID #Vendors UniProt IUPHAR Species p-value
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Activity
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Activity
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Assay Type Assay Description Source Mol
weight
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H don H acc LogP Smiles DOI
1640 2564 4 OPRD δ receptor Human - None Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 415 2 2 5 3.8 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1oc1c2cccc1)CC1CC1 9696425
3828 2564 4 OPRD δ receptor Human - None Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 415 2 2 5 3.8 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1oc1c2cccc1)CC1CC1 9696425
5486827 2564 4 OPRD δ receptor Human - None Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 415 2 2 5 3.8 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1oc1c2cccc1)CC1CC1 9696425
CHEMBL100940 2564 4 OPRD δ receptor Human - None Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 415 2 2 5 3.8 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1oc1c2cccc1)CC1CC1 9696425
54669894 80119 0 OPRD δ receptor Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
ChEMBL 509 8 4 6 0.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(C)[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/jm200894e
CHEMBL2151735 80119 0 OPRD δ receptor Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
ChEMBL 509 8 4 6 0.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(C)[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/jm200894e
46227362 196167 0 OPRD δ receptor Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 1210 16 10 12 4.7 CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)NC(=O)[C@@H]2CCCN2C1=O 10.1016/j.bmc.2009.08.035
CHEMBL611926 196167 0 OPRD δ receptor Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 1210 16 10 12 4.7 CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)NC(=O)[C@@H]2CCCN2C1=O 10.1016/j.bmc.2009.08.035
23642304 189540 0 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 396 2 1 3 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1cc2ccccc2nc1C3 10.1016/j.bmcl.2009.03.099
CHEMBL559518 189540 0 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 396 2 1 3 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1cc2ccccc2nc1C3 10.1016/j.bmcl.2009.03.099
23642304 189540 0 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 396 2 1 3 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2011.11.047
CHEMBL559518 189540 0 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 396 2 1 3 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2011.11.047
127029284 136851 0 OPRD δ receptor Mouse 10.7 pEC50 = 10.7 Binding
Agonist activity at delta-opioid receptor in mouse vas deferensAgonist activity at delta-opioid receptor in mouse vas deferens
ChEMBL 497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)NCc1nc2ccccc2[nH]1 10.1016/j.ejmech.2015.11.028
CHEMBL3758292 136851 0 OPRD δ receptor Mouse 10.7 pEC50 = 10.7 Binding
Agonist activity at delta-opioid receptor in mouse vas deferensAgonist activity at delta-opioid receptor in mouse vas deferens
ChEMBL 497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)NCc1nc2ccccc2[nH]1 10.1016/j.ejmech.2015.11.028
1607 1225 27 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL None None None None 10.1039/d0md00104j
6917707 1225 27 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL None None None None 10.1039/d0md00104j
CHEMBL340032 1225 27 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL None None None None 10.1039/d0md00104j
DB08856 1225 27 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human DOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL None None None None 10.1039/d0md00104j
46227362 196167 0 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 1210 16 10 12 4.7 CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)NC(=O)[C@@H]2CCCN2C1=O 10.1016/j.bmc.2009.08.035
CHEMBL611926 196167 0 OPRD δ receptor Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 1210 16 10 12 4.7 CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)NC(=O)[C@@H]2CCCN2C1=O 10.1016/j.bmc.2009.08.035
44467662 189030 0 OPRD δ receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 356 0 1 3 3.9 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2009.03.099
CHEMBL552308 189030 0 OPRD δ receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 356 0 1 3 3.9 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2009.03.099
44467662 189030 0 OPRD δ receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 356 0 1 3 3.9 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2011.11.047
CHEMBL552308 189030 0 OPRD δ receptor Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 356 0 1 3 3.9 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2011.11.047
45270599 190264 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 398 2 1 3 4.9 CC(C)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2009.03.099
CHEMBL564538 190264 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 398 2 1 3 4.9 CC(C)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2009.03.099
45270599 190264 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 398 2 1 3 4.9 CC(C)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2011.11.047
CHEMBL564538 190264 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 398 2 1 3 4.9 CC(C)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2011.11.047
50994459 56700 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 774 17 5 7 4.5 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649941 56700 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 774 17 5 7 4.5 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
50994459 56700 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 774 17 5 7 4.5 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649941 56700 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 774 17 5 7 4.5 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
50994460 56701 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 758 17 5 7 4.0 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649942 56701 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 758 17 5 7 4.0 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
50994460 56701 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 758 17 5 7 4.0 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649942 56701 0 OPRD δ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 758 17 5 7 4.0 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
1613 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Binding
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cellsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2019.07.033
3903 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Binding
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cellsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2019.07.033
461776 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Binding
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cellsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2019.07.033
CHEMBL15038 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Binding
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cellsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2019.07.033
CHEMBL8234 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Binding
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cellsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2019.07.033
1613 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530
3903 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530
461776 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530
CHEMBL15038 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530
CHEMBL8234 2159 34 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530
127029284 136851 0 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human delta-opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)NCc1nc2ccccc2[nH]1 10.1016/j.ejmech.2015.11.028
CHEMBL3758292 136851 0 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human delta-opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)NCc1nc2ccccc2[nH]1 10.1016/j.ejmech.2015.11.028
50994531 56706 0 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 804 13 4 7 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649947 56706 0 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 804 13 4 7 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
50994531 56706 0 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 804 13 4 7 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649947 56706 0 OPRD δ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 804 13 4 7 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
50994380 56697 0 OPRD δ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 740 17 5 7 3.8 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649938 56697 0 OPRD δ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 740 17 5 7 3.8 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
44177570 60710 0 OPRD δ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1219 27 10 10 6.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766204 60710 0 OPRD δ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1219 27 10 10 6.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL26575 204177 0 OPRD δ receptor Rat 10.0 pEC50 = 10 Functional
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)NCC(=O)O)C(C)C 10.1016/j.bmcl.2018.05.015
71456262 78811 0 OPRD δ receptor Human 10.0 pEC50 = 10 Functional
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 448 3 1 4 3.5 CN1CC[C@]23c4c5cccc4O[C@H]2C(=O)CC[C@@]3(NC(=O)/C=C/c2ccccc2Cl)[C@H]1C5 10.1021/jm0604777
CHEMBL2113666 78811 0 OPRD δ receptor Human 10.0 pEC50 = 10 Functional
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 448 3 1 4 3.5 CN1CC[C@]23c4c5cccc4O[C@H]2C(=O)CC[C@@]3(NC(=O)/C=C/c2ccccc2Cl)[C@H]1C5 10.1021/jm0604777
1641 2565 3 OPRD δ receptor Human 10.0 pEC50 = 10.0 Functional
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm030801n
3829 2565 3 OPRD δ receptor Human 10.0 pEC50 = 10.0 Functional
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm030801n
5497186 2565 3 OPRD δ receptor Human 10.0 pEC50 = 10.0 Functional
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm030801n
CHEMBL567175 2565 3 OPRD δ receptor Human 10.0 pEC50 = 10.0 Functional
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm030801n
104787 1376 16 OPRD δ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1021/acsmedchemlett.5b00423
1608 1376 16 OPRD δ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1021/acsmedchemlett.5b00423
CHEMBL31421 1376 16 OPRD δ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1021/acsmedchemlett.5b00423
DB08861 1376 16 OPRD δ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1021/acsmedchemlett.5b00423
50994530 56705 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 716 14 5 7 2.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649946 56705 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 716 14 5 7 2.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
119029 711 21 OPRD δ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
ChEMBL 435 8 1 4 4.5 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)O)c1ccc(cc1)C(=O)N(CC)CC 10.1021/jm000228x
9002 711 21 OPRD δ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
ChEMBL 435 8 1 4 4.5 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)O)c1ccc(cc1)C(=O)N(CC)CC 10.1021/jm000228x
CHEMBL25230 711 21 OPRD δ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
ChEMBL 435 8 1 4 4.5 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)O)c1ccc(cc1)C(=O)N(CC)CC 10.1021/jm000228x
50994530 56705 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 716 14 5 7 2.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649946 56705 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 716 14 5 7 2.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
44177570 60710 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1219 27 10 10 6.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766204 60710 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1219 27 10 10 6.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
10345770 8211 0 OPRD δ receptor Mouse 9.9 pEC50 = 9.9 Functional
Negative logarithm of the molar concentration required to produce 50% of the maximum effect in mu receptor from mouse vas deferens (MVD)Negative logarithm of the molar concentration required to produce 50% of the maximum effect in mu receptor from mouse vas deferens (MVD)
ChEMBL 497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCc1nc2ccccc2[nH]1 10.1021/jm010449i
CHEMBL109390 8211 0 OPRD δ receptor Mouse 9.9 pEC50 = 9.9 Functional
Negative logarithm of the molar concentration required to produce 50% of the maximum effect in mu receptor from mouse vas deferens (MVD)Negative logarithm of the molar concentration required to produce 50% of the maximum effect in mu receptor from mouse vas deferens (MVD)
ChEMBL 497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCc1nc2ccccc2[nH]1 10.1021/jm010449i
46227961 13822 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198015 13822 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL593214 13822 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL294616 204409 0 OPRD δ receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm200894e
71456106 83520 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 494 7 2 3 6.0 CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5O)cc4)cc3C1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
CHEMBL2208349 83520 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 494 7 2 3 6.0 CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5O)cc4)cc3C1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
50925450 56702 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 732 14 5 7 3.3 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649943 56702 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 732 14 5 7 3.3 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
16720745 84698 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 384 2 2 2 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3 10.1021/jm0701674
CHEMBL226166 84698 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 384 2 2 2 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3 10.1021/jm0701674
50925450 56702 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 732 14 5 7 3.3 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649943 56702 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 732 14 5 7 3.3 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
54757387 65100 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
ChEMBL 495 8 5 6 -0.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/jm200894e
CHEMBL1834247 65100 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human DOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
ChEMBL 495 8 5 6 -0.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/jm200894e
16720749 84714 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 367 2 2 5 3.1 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm0701674
CHEMBL226217 84714 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 367 2 2 5 3.1 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm0701674
CHEMBL3086304 84714 0 OPRD δ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 367 2 2 5 3.1 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm0701674
57394219 68761 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 396 2 1 3 4.6 Oc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2011.11.047
CHEMBL1929365 68761 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 396 2 1 3 4.6 Oc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2011.11.047
44596170 13879 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 524 4 3 5 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Br)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198702 13879 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 524 4 3 5 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Br)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611930 13879 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 524 4 3 5 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Br)cc1 10.1016/j.bmc.2009.07.069
50994602 56707 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 820 13 4 7 4.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649948 56707 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 820 13 4 7 4.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
44177670 60712 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1151 27 10 10 5.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766206 60712 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1151 27 10 10 5.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1 10.1021/jm101023r
10142188 197213 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 508 7 0 4 6.5 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL67192 197213 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 508 7 0 4 6.5 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
50994602 56707 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 820 13 4 7 4.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649948 56707 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 820 13 4 7 4.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
45486042 190910 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 461 9 1 5 5.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccoc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL568818 190910 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 461 9 1 5 5.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccoc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
45486046 192542 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 477 9 1 5 5.8 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccsc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL584941 192542 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 477 9 1 5 5.8 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccsc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL2387214 203918 0 OPRD δ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)O 10.1016/j.bmcl.2013.03.065
137657032 158764 0 OPRD δ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 444 3 1 4 4.2 O=C(c1ccoc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
CHEMBL4103044 158764 0 OPRD δ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 444 3 1 4 4.2 O=C(c1ccoc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
45486018 190977 0 OPRD δ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 472 9 1 5 5.1 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccn3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL569316 190977 0 OPRD δ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 472 9 1 5 5.1 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccn3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL2419538 203954 0 OPRD δ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human DOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NC1(C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)OCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCCC1 10.1016/j.bmcl.2013.06.065
11694 3452 0 OPRD δ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysis
ChEMBL 564 6 1 5 6.7 CN1CC[C@]23[C@H]4Oc5c(O)ccc(C[C@@H]1[C@@]2(Cc1c4ncc(c1)c1ccc(Cl)cc1)OCCCc1ccccc1)c35 10.1021/jm300686p
71460944 3452 0 OPRD δ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysis
ChEMBL 564 6 1 5 6.7 CN1CC[C@]23[C@H]4Oc5c(O)ccc(C[C@@H]1[C@@]2(Cc1c4ncc(c1)c1ccc(Cl)cc1)OCCCc1ccccc1)c35 10.1021/jm300686p
CHEMBL2179656 3452 0 OPRD δ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysis
ChEMBL 564 6 1 5 6.7 CN1CC[C@]23[C@H]4Oc5c(O)ccc(C[C@@H]1[C@@]2(Cc1c4ncc(c1)c1ccc(Cl)cc1)OCCCc1ccccc1)c35 10.1021/jm300686p
10206319 192072 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
ChEMBL 484 9 1 4 5.1 CCN(CC)C(=O)c1ccc(N(c2cccc(C(N)=O)c2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.068
CHEMBL577615 192072 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
ChEMBL 484 9 1 4 5.1 CCN(CC)C(=O)c1ccc(N(c2cccc(C(N)=O)c2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.068
44279699 98591 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
GTPgammaS binding in cloned human Opioid receptor delta 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor delta 1 transfected into hamster ovary cells
ChEMBL 435 3 2 5 3.3 CO[C@]12C=CC3(CC14CCC[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1CC1CC1)[C@@H]2O5 10.1021/jm991165p
CHEMBL281986 98591 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
GTPgammaS binding in cloned human Opioid receptor delta 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor delta 1 transfected into hamster ovary cells
ChEMBL 435 3 2 5 3.3 CO[C@]12C=CC3(CC14CCC[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1CC1CC1)[C@@H]2O5 10.1021/jm991165p
46227966 13881 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Inverse agonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198704 13881 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Inverse agonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611932 13881 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Inverse agonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at delta opioid receptor expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
71454361 83518 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 494 7 2 3 6.0 C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(O)cc5)cc4)cc3[C@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
CHEMBL2208347 83518 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 494 7 2 3 6.0 C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(O)cc5)cc4)cc3[C@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
90397724 157055 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 454 3 1 3 4.6 O=C(c1ccccc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
CHEMBL4083940 157055 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 454 3 1 3 4.6 O=C(c1ccccc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
11016127 163732 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 468 5 4 4 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C/N=C(/S)NC(C)(C)C 10.1021/jm015532k
CHEMBL421520 163732 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 468 5 4 4 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C/N=C(/S)NC(C)(C)C 10.1021/jm015532k
71452746 78535 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 401 2 3 4 3.4 CCN[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm021073r
CHEMBL2113383 78535 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 401 2 3 4 3.4 CCN[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm021073r
4060 1227 0 OPRD δ receptor Mouse 9.5 pEC50 = 9.5 Functional
Negative logarithm of the molar concentration of delta receptor was determined in mouse vas deferensNegative logarithm of the molar concentration of delta receptor was determined in mouse vas deferens
ChEMBL None None None None 10.1016/s0960-894x(00)00569-2
CHEMBL296603 1227 0 OPRD δ receptor Mouse 9.5 pEC50 = 9.5 Functional
Negative logarithm of the molar concentration of delta receptor was determined in mouse vas deferensNegative logarithm of the molar concentration of delta receptor was determined in mouse vas deferens
ChEMBL None None None None 10.1016/s0960-894x(00)00569-2
CHEMBL2387215 203919 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)O 10.1016/j.bmcl.2013.03.065
CHEMBL4797394 182451 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human delta-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assayAgonist activity at human delta-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assay
ChEMBL 897 23 13 10 -1.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O 10.1021/acs.jmedchem.0c00643
89435126 155779 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 455 3 1 4 4.0 O=C(c1ccccn1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
CHEMBL4068691 155779 0 OPRD δ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 455 3 1 4 4.0 O=C(c1ccccn1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
CHEMBL49581 207504 0 OPRD δ receptor Mouse 9.4 pEC50 = 9.4 Binding
Effective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitroEffective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitro
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)N)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1021/jm00038a004
122187205 122227 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL 981 22 8 9 5.3 CCCCC(NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2015.06.030
CHEMBL3608938 122227 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL 981 22 8 9 5.3 CCCCC(NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2015.06.030
12038832 179764 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 464 6 3 6 2.5 CO[C@@]12CC[C@H](N[C@@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4754944 179764 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 464 6 3 6 2.5 CO[C@@]12CC[C@H](N[C@@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
90655828 110482 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 486 3 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1c1ccccc1 10.1021/ml400491k
CHEMBL3264747 110482 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 486 3 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1c1ccccc1 10.1021/ml400491k
119029 711 21 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 435 8 1 4 4.5 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)O)c1ccc(cc1)C(=O)N(CC)CC 10.1021/jm8008986
9002 711 21 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 435 8 1 4 4.5 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)O)c1ccc(cc1)C(=O)N(CC)CC 10.1021/jm8008986
CHEMBL25230 711 21 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 435 8 1 4 4.5 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)O)c1ccc(cc1)C(=O)N(CC)CC 10.1021/jm8008986
11849285 195434 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 444 3 2 5 2.9 Cc1ccccc1/C=C/C(=O)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/jm0604777
CHEMBL607125 195434 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 444 3 2 5 2.9 Cc1ccccc1/C=C/C(=O)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/jm0604777
90655829 110483 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 514 5 1 6 3.4 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1CCc1ccccc1 10.1021/ml400491k
CHEMBL3264748 110483 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 514 5 1 6 3.4 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1CCc1ccccc1 10.1021/ml400491k
90392376 155150 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 440 4 1 3 5.0 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1Cc1ccccc1)C2 10.1016/j.bmcl.2017.05.072
CHEMBL4061334 155150 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 440 4 1 3 5.0 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1Cc1ccccc1)C2 10.1016/j.bmcl.2017.05.072
71509871 156350 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 442 3 1 4 3.5 C=CCN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1 10.1016/j.bmcl.2017.04.059
CHEMBL4075409 156350 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 442 3 1 4 3.5 C=CCN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1 10.1016/j.bmcl.2017.04.059
71509717 156411 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 416 1 1 4 3.0 CN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1 10.1016/j.bmcl.2017.04.059
CHEMBL4076303 156411 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 416 1 1 4 3.0 CN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1 10.1016/j.bmcl.2017.04.059
89435196 158026 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 428 3 1 5 3.8 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1c1cnccn1)C2 10.1016/j.bmcl.2017.05.072
CHEMBL4094845 158026 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 428 3 1 5 3.8 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1c1cnccn1)C2 10.1016/j.bmcl.2017.05.072
44177670 60712 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1151 27 10 10 5.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766206 60712 0 OPRD δ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1151 27 10 10 5.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1 10.1021/jm101023r
16720553 84663 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 344 0 2 2 3.8 CN1CC[C@]23Cc4[nH]c5ccccc5c4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1021/jm0701674
CHEMBL226114 84663 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 344 0 2 2 3.8 CN1CC[C@]23Cc4[nH]c5ccccc5c4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1021/jm0701674
12038831 182279 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 464 6 3 6 2.5 CO[C@@]12CC[C@@H](N[C@@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4795312 182279 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 464 6 3 6 2.5 CO[C@@]12CC[C@@H](N[C@@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
73353599 90954 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis
ChEMBL 763 11 3 6 5.6 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
CHEMBL2408013 90954 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis
ChEMBL 763 11 3 6 5.6 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
CHEMBL63732 196650 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 414 7 0 2 5.8 C=CCN1[C@H]2CC[C@@H]1C/C(=C(/c1ccccc1)c1ccc(C(=O)N(CC)CC)cc1)C2 10.1016/j.bmcl.2004.02.051
44408417 157458 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 1089 30 11 14 1.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL408889 157458 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 1089 30 11 14 1.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O 10.1021/jm050851n
52942137 17881 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 372 0 2 4 3.0 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL1270282 17881 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 372 0 2 4 3.0 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL4296720 17881 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 372 0 2 4 3.0 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
44408417 157458 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 1089 30 11 14 1.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL408889 157458 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 1089 30 11 14 1.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O 10.1021/jm050851n
90392373 155609 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 456 3 1 4 3.7 O=C(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.04.059
CHEMBL4066752 155609 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 456 3 1 4 3.7 O=C(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.04.059
CHEMBL294616 204409 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
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 analysisAgonist 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
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm400195y
9911987 190689 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
ChEMBL 457 8 1 4 5.7 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.068
CHEMBL567604 190689 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
ChEMBL 457 8 1 4 5.7 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.068
45486055 191047 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 471 9 1 4 5.7 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL569755 191047 0 OPRD δ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 471 9 1 4 5.7 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
54581461 60713 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1143 29 10 12 4.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1 10.1021/jm101023r
CHEMBL1766207 60713 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1143 29 10 12 4.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1 10.1021/jm101023r
71455506 82063 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysis
ChEMBL 562 5 1 5 6.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2ncc(-c4ccc(Cl)cc4)cc2C[C@@]3(OC/C=C/c2ccccc2)[C@H]1C5 10.1021/jm300686p
CHEMBL2179655 82063 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysis
ChEMBL 562 5 1 5 6.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2ncc(-c4ccc(Cl)cc4)cc2C[C@@]3(OC/C=C/c2ccccc2)[C@H]1C5 10.1021/jm300686p
54581461 60713 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1143 29 10 12 4.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1 10.1021/jm101023r
CHEMBL1766207 60713 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1143 29 10 12 4.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1 10.1021/jm101023r
117705988 158161 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 506 4 1 4 4.6 O=C(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CCc2ccccc2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.04.059
CHEMBL4096314 158161 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 506 4 1 4 4.6 O=C(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CCc2ccccc2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.04.059
90655829 110483 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 514 5 1 6 3.4 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1CCc1ccccc1 10.1021/ml400491k
CHEMBL3264748 110483 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 514 5 1 6 3.4 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1CCc1ccccc1 10.1021/ml400491k
90306849 110228 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 473 5 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL3262092 110228 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 473 5 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
10874095 104056 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 452 5 4 4 2.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNC(=O)NC(C)(C)C 10.1021/jm015532k
CHEMBL310842 104056 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 452 5 4 4 2.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNC(=O)NC(C)(C)C 10.1021/jm015532k
CHEMBL49507 207503 0 OPRD δ receptor Mouse 9.2 pEC50 = 9.2 Binding
Effective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitroEffective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitro
ChEMBL None None None Cc1cc(O)cc(C)c1[C@H](C)[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C)C(C)C 10.1021/jm00038a004
117706010 158595 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 442 4 1 4 4.1 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1Cc1ccccc1)O2 10.1016/j.bmcl.2017.04.059
CHEMBL4100943 158595 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 442 4 1 4 4.1 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1Cc1ccccc1)O2 10.1016/j.bmcl.2017.04.059
44444601 93555 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 508 8 1 3 6.3 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)[C@@]3(C)CCN(CC5CC5)C(C4)[C@@H]3C)cc2)cc1 10.1016/j.bmcl.2007.09.082
CHEMBL249985 93555 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 508 8 1 3 6.3 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)[C@@]3(C)CCN(CC5CC5)C(C4)[C@@H]3C)cc2)cc1 10.1016/j.bmcl.2007.09.082
51003219 59576 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins
ChEMBL 518 10 3 6 3.7 O=C(O)CN[C@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm101211p
CHEMBL1739441 59576 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins
ChEMBL 518 10 3 6 3.7 O=C(O)CN[C@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm101211p
CHEMBL3216476 59576 0 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins
ChEMBL 518 10 3 6 3.7 O=C(O)CN[C@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm101211p
9567 3522 4 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmcl.2009.03.099
9950038 3522 4 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmcl.2009.03.099
CHEMBL327745 3522 4 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmcl.2009.03.099
9567 3522 4 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmc.2011.11.047
9950038 3522 4 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmc.2011.11.047
CHEMBL327745 3522 4 OPRD δ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmc.2011.11.047
155538529 175677 0 OPRD δ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 548 7 3 5 5.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4476818 175677 0 OPRD δ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 548 7 3 5 5.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597054 175677 0 OPRD δ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 548 7 3 5 5.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
9890982 199027 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 472 6 4 4 3.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNC(=O)Nc1ccccc1 10.1021/jm015532k
CHEMBL80463 199027 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 472 6 4 4 3.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNC(=O)Nc1ccccc1 10.1021/jm015532k
24768397 145617 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 698 14 5 7 2.7 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL392185 145617 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 698 14 5 7 2.7 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
44436084 87840 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 845 18 6 8 3.4 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm061465o
CHEMBL235109 87840 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 845 18 6 8 3.4 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm061465o
24768397 145617 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 698 14 5 7 2.7 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL392185 145617 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 698 14 5 7 2.7 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
44436084 87840 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 845 18 6 8 3.4 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm061465o
CHEMBL235109 87840 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 845 18 6 8 3.4 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm061465o
72735565 105584 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 444 5 2 5 3.8 CCOCCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL3139076 105584 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 444 5 2 5 3.8 CCOCCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL4296728 105584 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 444 5 2 5 3.8 CCOCCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
155461914 181945 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assayAgonist activity at human delta-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assay
ChEMBL 1014 25 10 10 2.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCN2CCC(Cc3ccccc3)CC2)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O 10.1021/acs.jmedchem.0c00643
CHEMBL4790994 181945 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assayAgonist activity at human delta-opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition in presence of IBMX by Glo-sensor cAMP assay
ChEMBL 1014 25 10 10 2.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCN2CCC(Cc3ccccc3)CC2)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O 10.1021/acs.jmedchem.0c00643
CHEMBL294616 204409 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Binding
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 assayAgonist 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
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1016/j.ejmech.2014.12.049
58443234 83522 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 522 7 1 4 6.0 CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc6c(c5)OCO6)cc4)cc3C1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
CHEMBL2208351 83522 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 522 7 1 4 6.0 CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc6c(c5)OCO6)cc4)cc3C1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
16720646 136797 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 398 2 2 2 5.0 Oc1ccc2c(c1)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3 10.1021/jm0701674
CHEMBL375504 136797 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 398 2 2 2 5.0 Oc1ccc2c(c1)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3 10.1021/jm0701674
CHEMBL3787263 138367 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 412 2 2 4 3.7 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2016.03.040
89978664 160076 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Functional Assay: Functional [35S]GTPgammaS binding assays were conducted as follows. Delta opioid receptor membrane solution was prepared by sequentially adding final concentrations of 0.026 ug/ul delta membrane protein (Perkin Elmer, Shelton, Conn.), 10 ug/mL saponin, 3 uM GDP and 0.20 nM [35S]GTPgammaS to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice. The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of agonist prepared in DMSO. Plates were incubated for 30 min at a temperature of about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Packard) and followed by three filtration washes with 200 ul ice-cold binding buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50° C. for 1-2 hours.Functional Assay: Functional [35S]GTPgammaS binding assays were conducted as follows. Delta opioid receptor membrane solution was prepared by sequentially adding final concentrations of 0.026 ug/ul delta membrane protein (Perkin Elmer, Shelton, Conn.), 10 ug/mL saponin, 3 uM GDP and 0.20 nM [35S]GTPgammaS to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice. The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of agonist prepared in DMSO. Plates were incubated for 30 min at a temperature of about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Packard) and followed by three filtration washes with 200 ul ice-cold binding buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50° C. for 1-2 hours.
ChEMBL 544 8 2 7 3.7 CO[C@]12CC[C@@]3(C[C@@H]1COC(=O)[C@@H](N)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL4115222 160076 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Functional Assay: Functional [35S]GTPgammaS binding assays were conducted as follows. Delta opioid receptor membrane solution was prepared by sequentially adding final concentrations of 0.026 ug/ul delta membrane protein (Perkin Elmer, Shelton, Conn.), 10 ug/mL saponin, 3 uM GDP and 0.20 nM [35S]GTPgammaS to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice. The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of agonist prepared in DMSO. Plates were incubated for 30 min at a temperature of about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Packard) and followed by three filtration washes with 200 ul ice-cold binding buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50° C. for 1-2 hours.Functional Assay: Functional [35S]GTPgammaS binding assays were conducted as follows. Delta opioid receptor membrane solution was prepared by sequentially adding final concentrations of 0.026 ug/ul delta membrane protein (Perkin Elmer, Shelton, Conn.), 10 ug/mL saponin, 3 uM GDP and 0.20 nM [35S]GTPgammaS to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice. The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of agonist prepared in DMSO. Plates were incubated for 30 min at a temperature of about 25° C. with shaking. Reactions were terminated by rapid filtration onto 96-well Unifilter GF/B filter plates (Perkin Elmer, Shelton, Conn.) using a 96-well tissue harvester (Packard) and followed by three filtration washes with 200 ul ice-cold binding buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50° C. for 1-2 hours.
ChEMBL 544 8 2 7 3.7 CO[C@]12CC[C@@]3(C[C@@H]1COC(=O)[C@@H](N)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
16733485 136425 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay
ChEMBL 551 7 7 7 -0.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C\C[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1021/jm061048b
CHEMBL375025 136425 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay
ChEMBL 551 7 7 7 -0.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C\C[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1021/jm061048b
155526934 170293 0 OPRD δ receptor Mouse 9.1 pEC50 = 9.1 Functional
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 analysisAgonist 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
ChEMBL 460 5 1 6 4.5 CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.6b00748
CHEMBL4458337 170293 0 OPRD δ receptor Mouse 9.1 pEC50 = 9.1 Functional
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 analysisAgonist 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
ChEMBL 460 5 1 6 4.5 CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.6b00748
11123816 136989 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Partial agonist activity at delta opioid receptor (unknown origin) assessed as [35S]GTPgammaS binding by cell based assayPartial agonist activity at delta opioid receptor (unknown origin) assessed as [35S]GTPgammaS binding by cell based assay
ChEMBL 490 4 2 3 6.2 CN1CC[C@]23c4c5ccc(O)c4O[C@@]2(C)c2[nH]c4ccccc4c2C[C@@]3(CCCc2ccccc2)[C@H]1C5 10.1016/j.ejmech.2015.11.028
CHEMBL3759489 136989 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Partial agonist activity at delta opioid receptor (unknown origin) assessed as [35S]GTPgammaS binding by cell based assayPartial agonist activity at delta opioid receptor (unknown origin) assessed as [35S]GTPgammaS binding by cell based assay
ChEMBL 490 4 2 3 6.2 CN1CC[C@]23c4c5ccc(O)c4O[C@@]2(C)c2[nH]c4ccccc4c2C[C@@]3(CCCc2ccccc2)[C@H]1C5 10.1016/j.ejmech.2015.11.028
71456257 78530 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 491 5 3 4 5.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NCCCc2ccccc2)C1C5 10.1021/jm021073r
CHEMBL2113378 78530 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 491 5 3 4 5.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NCCCc2ccccc2)C1C5 10.1021/jm021073r
16733487 85125 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay
ChEMBL 551 7 7 7 -0.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1021/jm061048b
CHEMBL229440 85125 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay
ChEMBL 551 7 7 7 -0.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1021/jm061048b
CHEMBL382051 205806 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
CHEMBL382051 205806 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
10479670 76757 0 OPRD δ receptor Mouse 9.1 pEC50 = 9.1 Functional
Activity against delta opioid receptor by stimulation of [35S]GTP-gamma-S binding in CHO-hgamma cellsActivity against delta opioid receptor by stimulation of [35S]GTP-gamma-S binding in CHO-hgamma cells
ChEMBL 466 5 3 4 4.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
CHEMBL208454 76757 0 OPRD δ receptor Mouse 9.1 pEC50 = 9.1 Functional
Activity against delta opioid receptor by stimulation of [35S]GTP-gamma-S binding in CHO-hgamma cellsActivity against delta opioid receptor by stimulation of [35S]GTP-gamma-S binding in CHO-hgamma cells
ChEMBL 466 5 3 4 4.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
10479670 76757 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 466 5 3 4 4.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL208454 76757 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 466 5 3 4 4.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
10620902 18896 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.
ChEMBL 398 5 1 2 5.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc3ccccc23)cc1 10.1021/jm000229p
CHEMBL129034 18896 0 OPRD δ receptor Human 9.1 pEC50 = 9.1 Functional
Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.
ChEMBL 398 5 1 2 5.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc3ccccc23)cc1 10.1021/jm000229p
11729952 198592 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 443 7 3 4 3.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNCc1ccccc1 10.1021/jm015532k
CHEMBL77001 198592 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 443 7 3 4 3.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNCc1ccccc1 10.1021/jm015532k
10435156 78534 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 477 4 3 4 4.6 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NCCc2ccccc2)C1C5 10.1021/jm021073r
CHEMBL2113382 78534 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 477 4 3 4 4.6 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NCCc2ccccc2)C1C5 10.1021/jm021073r
11091522 198471 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 444 7 2 4 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1COCc1ccccc1 10.1021/jm015532k
CHEMBL76089 198471 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 444 7 2 4 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1COCc1ccccc1 10.1021/jm015532k
44178113 60714 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1237 27 10 11 5.6 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766208 60714 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1237 27 10 11 5.6 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
90655828 110482 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 486 3 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1c1ccccc1 10.1021/ml400491k
CHEMBL3264747 110482 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 486 3 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1c1ccccc1 10.1021/ml400491k
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm800389v
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm800389v
44178113 60714 0 OPRD δ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1237 27 10 11 5.6 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766208 60714 0 OPRD δ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1237 27 10 11 5.6 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9 Binding
Binding affinity to DOR (unknown origin)Binding affinity to DOR (unknown origin)
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/acsmedchemlett.7b00210
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9 Binding
Binding affinity to DOR (unknown origin)Binding affinity to DOR (unknown origin)
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/acsmedchemlett.7b00210
1614 2344 32 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmcl.2009.03.099
443363 2344 32 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmcl.2009.03.099
CHEMBL13786 2344 32 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmcl.2009.03.099
DB12668 2344 32 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmcl.2009.03.099
1614 2344 32 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2011.11.047
443363 2344 32 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2011.11.047
CHEMBL13786 2344 32 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2011.11.047
DB12668 2344 32 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2011.11.047
52942140 17909 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 412 2 2 4 3.7 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL1270475 17909 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 412 2 2 4 3.7 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL4296721 17909 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 412 2 2 4 3.7 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL3787016 138342 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 414 2 3 3 4.1 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)CCc1c([nH]c2ccccc12)C3 10.1016/j.bmc.2016.03.040
51003217 59577 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins
ChEMBL 518 10 3 6 3.7 O=C(O)CN[C@@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm101211p
CHEMBL1739442 59577 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins
ChEMBL 518 10 3 6 3.7 O=C(O)CN[C@@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm101211p
CHEMBL3216936 59577 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins
ChEMBL 518 10 3 6 3.7 O=C(O)CN[C@@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm101211p
45483664 191721 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
ChEMBL 514 9 1 5 6.2 CCN(CC)C(=O)c1ccc(N(c2cccc(NC(=O)OC)c2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.068
CHEMBL574640 191721 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
ChEMBL 514 9 1 5 6.2 CCN(CC)C(=O)c1ccc(N(c2cccc(NC(=O)OC)c2)C2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.068
72735204 105592 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 386 1 2 4 3.4 CCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL3139097 105592 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 386 1 2 4 3.4 CCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL4296733 105592 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 386 1 2 4 3.4 CCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL2419542 203958 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human DOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2013.06.065
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm070332f
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm070332f
56589659 110477 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 500 4 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1Cc1ccccc1 10.1021/ml400491k
CHEMBL3264742 110477 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 500 4 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1Cc1ccccc1 10.1021/ml400491k
CHEMBL2387328 203922 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCC(=O)NCCCCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](Cc1c(F)c(F)c(F)c(F)c1F)C(N)=O 10.1016/j.bmcl.2013.03.065
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1016/j.bmc.2009.08.035
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1016/j.bmc.2009.08.035
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061369n
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061369n
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm900473p
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm900473p
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm800389v
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm800389v
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm100157m
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm101023r
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm100157m
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm101023r
71459962 78815 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
ChEMBL 459 5 1 5 4.2 CO[C@]12C=C[C@@]3(C[C@H]1[C@@H](C)OCc1ccccc1)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm990951r
CHEMBL2113671 78815 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
ChEMBL 459 5 1 5 4.2 CO[C@]12C=C[C@@]3(C[C@H]1[C@@H](C)OCc1ccccc1)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm990951r
44279686 103687 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
GTPgammaS binding in cloned human Opioid receptor delta 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor delta 1 transfected into hamster ovary cells
ChEMBL 463 3 2 5 3.9 CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1CC1CC1)[C@@H]2O5 10.1021/jm991165p
CHEMBL31030 103687 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
GTPgammaS binding in cloned human Opioid receptor delta 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor delta 1 transfected into hamster ovary cells
ChEMBL 463 3 2 5 3.9 CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1CC1CC1)[C@@H]2O5 10.1021/jm991165p
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050851n
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050851n
69272251 178646 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 416 5 3 6 1.9 CO[C@@]12CC[C@H](N[C@@H](C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4741203 178646 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 416 5 3 6 1.9 CO[C@@]12CC[C@H](N[C@@H](C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1016/j.bmc.2009.08.035
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1016/j.bmc.2009.08.035
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061369n
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061369n
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm900473p
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm900473p
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm100157m
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm101023r
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm100157m
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm101023r
5487663 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050851n
CHEMBL200199 72260 7 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050851n
45486011 191922 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 489 9 1 4 5.9 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccc3F)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL576267 191922 0 OPRD δ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 489 9 1 4 5.9 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccc3F)CC2)cc1 10.1016/j.bmcl.2009.09.072
145961376 160785 0 OPRD δ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 569 15 9 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
CHEMBL4129679 160785 0 OPRD δ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 569 15 9 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
45486101 191039 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 485 9 1 4 6.0 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccc(C)cc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL569728 191039 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 485 9 1 4 6.0 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccc(C)cc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL4789014 181788 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 579 9 5 8 2.3 CO[C@@]12CC[C@H](N[C@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
45486102 191081 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 461 9 2 5 4.4 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ncc[nH]3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL569956 191081 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 461 9 2 5 4.4 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ncc[nH]3)CC2)cc1 10.1016/j.bmcl.2009.09.072
24873473 83528 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 508 8 1 3 6.3 COc1cccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)c1 10.1016/j.bmcl.2012.10.081
CHEMBL2208358 83528 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 508 8 1 3 6.3 COc1cccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)c1 10.1016/j.bmcl.2012.10.081
117706009 156879 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 492 4 1 5 3.3 O=S(=O)(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.04.059
CHEMBL4081856 156879 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 492 4 1 5 3.3 O=S(=O)(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.04.059
10323346 78531 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 491 3 3 4 4.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NC(=O)Cc2ccccc2)C1C5 10.1021/jm021073r
CHEMBL2113379 78531 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 491 3 3 4 4.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NC(=O)Cc2ccccc2)C1C5 10.1021/jm021073r
72735205 105624 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 400 2 2 4 3.7 CCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL3139191 105624 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 400 2 2 4 3.7 CCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL4296730 105624 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 400 2 2 4 3.7 CCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
118731120 117428 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human DOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assayAgonist activity at human DOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay
ChEMBL 594 13 8 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL3408737 117428 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human DOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assayAgonist activity at human DOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay
ChEMBL 594 13 8 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O 10.1021/acs.jmedchem.0c01376
45486070 191092 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 461 9 1 5 5.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccco3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL570000 191092 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 461 9 1 5 5.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccco3)CC2)cc1 10.1016/j.bmcl.2009.09.072
69122359 182294 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 416 5 3 6 1.9 CO[C@@]12CC[C@@H](N[C@@H](C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4795517 182294 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 416 5 3 6 1.9 CO[C@@]12CC[C@@H](N[C@@H](C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
89435280 156449 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 470 3 1 4 5.0 O=C(Oc1ccccc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
CHEMBL4076681 156449 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 470 3 1 4 5.0 O=C(Oc1ccccc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
44408411 160485 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL412331 160485 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL294616 204409 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm021073r
44408411 160485 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL412331 160485 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
72735758 105612 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 442 2 2 5 3.5 Oc1ccc2c(c1)[C@]13CCN(C[C@@H]4CCCO4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL3139163 105612 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 442 2 2 5 3.5 Oc1ccc2c(c1)[C@]13CCN(C[C@@H]4CCCO4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL4296737 105612 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 442 2 2 5 3.5 Oc1ccc2c(c1)[C@]13CCN(C[C@@H]4CCCO4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
24822630 97174 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
CHEMBL272215 97174 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
CHEMBL593215 97174 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Activity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at delta opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
CHEMBL3785854 138232 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 400 2 3 3 3.7 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@@H](C2)[C@]1(O)Cc1c([nH]c2ccccc12)C3 10.1016/j.bmc.2016.03.040
117860306 156447 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 474 5 1 5 3.4 COCCCN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1 10.1016/j.bmcl.2017.04.059
CHEMBL4076673 156447 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 474 5 1 5 3.4 COCCCN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1 10.1016/j.bmcl.2017.04.059
11474838 184865 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 392 4 2 4 3.8 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccc(O)cc32)cc1 10.1021/jm8008986
CHEMBL494479 184865 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 392 4 2 4 3.8 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccc(O)cc32)cc1 10.1021/jm8008986
9567 3522 4 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmcl.2009.03.099
9950038 3522 4 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmcl.2009.03.099
CHEMBL327745 3522 4 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmcl.2009.03.099
155526934 170293 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of delta opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assay
ChEMBL 460 5 1 6 4.5 CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1016/j.ejmech.2019.111701
CHEMBL4458337 170293 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of delta opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assay
ChEMBL 460 5 1 6 4.5 CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1016/j.ejmech.2019.111701
155526934 170293 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of delta opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assay
ChEMBL 460 5 1 6 4.5 CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1016/j.ejmech.2019.111701
CHEMBL4458337 170293 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of delta opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assay
ChEMBL 460 5 1 6 4.5 CC[C@@H]1CN2CC[C@]3(Nc4cccc(-c5ccccc5)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1016/j.ejmech.2019.111701
11213149 122324 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 452 5 3 4 4.3 Cc1[nH]c([C@@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1-c1ccccc1 10.1021/jm030548r
CHEMBL361033 122324 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 452 5 3 4 4.3 Cc1[nH]c([C@@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1-c1ccccc1 10.1021/jm030548r
71458065 78527 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 505 4 3 4 4.5 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NC(=O)CCc2ccccc2)C1C5 10.1021/jm021073r
CHEMBL2113373 78527 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
ChEMBL 505 4 3 4 4.5 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NC(=O)CCc2ccccc2)C1C5 10.1021/jm021073r
72735386 105649 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 404 2 2 4 3.3 Oc1ccc2c(c1)[C@]13CCN(CCF)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL3139248 105649 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 404 2 2 4 3.3 Oc1ccc2c(c1)[C@]13CCN(CCF)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL4296731 105649 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 404 2 2 4 3.3 Oc1ccc2c(c1)[C@]13CCN(CCF)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
45486096 190907 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 477 9 1 5 5.8 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3cccs3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL568803 190907 0 OPRD δ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 477 9 1 5 5.8 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3cccs3)CC2)cc1 10.1016/j.bmcl.2009.09.072
104787 1376 16 OPRD δ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL None None None None 10.1016/j.ejmech.2020.112070
1608 1376 16 OPRD δ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL None None None None 10.1016/j.ejmech.2020.112070
CHEMBL31421 1376 16 OPRD δ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL None None None None 10.1016/j.ejmech.2020.112070
DB08861 1376 16 OPRD δ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL None None None None 10.1016/j.ejmech.2020.112070
145961844 160828 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay
ChEMBL 1146 12 12 16 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NCCSSCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1016/j.bmc.2018.05.045
CHEMBL4130303 160828 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay
ChEMBL 1146 12 12 16 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NCCSSCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1016/j.bmc.2018.05.045
145961844 160828 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay
ChEMBL 1146 12 12 16 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NCCSSCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1016/j.bmc.2018.05.045
CHEMBL4130303 160828 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay
ChEMBL 1146 12 12 16 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NCCSSCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1016/j.bmc.2018.05.045
16720551 84662 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 398 3 1 2 4.9 COc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3 10.1021/jm0701674
CHEMBL226113 84662 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 398 3 1 2 4.9 COc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3 10.1021/jm0701674
117706054 156443 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 469 3 2 3 5.0 O=C(Nc1ccccc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
CHEMBL4076632 156443 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 469 3 2 3 5.0 O=C(Nc1ccccc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21 10.1016/j.bmcl.2017.05.072
10872951 199076 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 395 5 3 4 2.0 CC(=O)NC[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/jm015532k
CHEMBL80823 199076 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 395 5 3 4 2.0 CC(=O)NC[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/jm015532k
49799969 10274 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
ChEMBL 411 4 2 5 3.2 CCC[C@@](C)(O)[C@@H]1CC23C=C[C@]1(OC)[C@H]1Oc4c(O)ccc5c4C12CCN(C)C3C5 10.1021/jm990951r
CHEMBL1169585 10274 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
ChEMBL 411 4 2 5 3.2 CCC[C@@](C)(O)[C@@H]1CC23C=C[C@]1(OC)[C@H]1Oc4c(O)ccc5c4C12CCN(C)C3C5 10.1021/jm990951r
56589659 110477 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 500 4 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1Cc1ccccc1 10.1021/ml400491k
CHEMBL3264742 110477 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 500 4 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1Cc1ccccc1 10.1021/ml400491k
CHEMBL4792012 182009 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 579 9 5 8 2.3 CO[C@@]12CC[C@@H](N[C@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm050921q
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm100982d
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm061369n
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm900473p
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm800389v
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm050851n
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm050921q
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm070332f
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm100982d
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm061369n
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cell membrane by [35S]GTPgamma binding assay
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm900473p
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm800389v
155522549 175387 0 OPRD δ receptor Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 511 6 3 5 4.8 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL4453526 175387 0 OPRD δ receptor Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 511 6 3 5 4.8 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL4594713 175387 0 OPRD δ receptor Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 511 6 3 5 4.8 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL294616 204409 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm050851n
72735567 105617 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 416 2 3 5 2.7 C[C@H](O)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL3139175 105617 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 416 2 3 5 2.7 C[C@H](O)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL4296732 105617 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 416 2 3 5 2.7 C[C@H](O)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL2387211 203915 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](NC(=O)C(C)(C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](CCC(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(N)=O 10.1016/j.bmcl.2013.03.065
118716009 114041 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 485 5 3 6 2.5 O=C(NCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5 10.1016/j.bmcl.2014.09.029
CHEMBL3339378 114041 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 485 5 3 6 2.5 O=C(NCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5 10.1016/j.bmcl.2014.09.029
123924 3413 31 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
1611 3413 31 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
CHEMBL13470 3413 31 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
117706085 158382 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 446 4 1 3 5.4 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1CC1CCCCC1)C2 10.1016/j.bmcl.2017.05.072
CHEMBL4098662 158382 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant DOR expressed in CHO cells assessed as cAMP accumulation
ChEMBL 446 4 1 3 5.4 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1CC1CCCCC1)C2 10.1016/j.bmcl.2017.05.072
11827053 198439 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 488 6 4 4 4.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C/N=C(/S)Nc1ccccc1 10.1021/jm015532k
CHEMBL75802 198439 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
ChEMBL 488 6 4 4 4.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C/N=C(/S)Nc1ccccc1 10.1021/jm015532k
44301701 192415 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Inhibition of delta opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assay
ChEMBL 414 5 1 7 2.9 CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1016/j.ejmech.2019.111701
CHEMBL58362 192415 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Inhibition of delta opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) in presence of DAMGO by [35S]-GTPgammaS binding assay
ChEMBL 414 5 1 7 2.9 CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1016/j.ejmech.2019.111701
44301701 192415 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Inhibition of delta opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assay
ChEMBL 414 5 1 7 2.9 CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1016/j.ejmech.2019.111701
CHEMBL58362 192415 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Inhibition of delta opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) in presence of DPDPE by [35S]-GTPgammaS binding assay
ChEMBL 414 5 1 7 2.9 CC[C@@H]1CN2CC[C@]3(Nc4cccc(OC)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1016/j.ejmech.2019.111701
CHEMBL4783612 181376 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 464 6 3 6 2.5 CO[C@@]12CC[C@@H](N[C@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
69122388 179688 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 480 6 4 7 2.2 CO[C@@]12CC[C@H](N[C@@H](Cc3ccc(O)cc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4753934 179688 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 480 6 4 7 2.2 CO[C@@]12CC[C@H](N[C@@H](Cc3ccc(O)cc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
90656665 110229 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 471 5 2 5 4.1 CO[C@]12C=C[C@@]3(C[C@@H]1[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL3262093 110229 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 471 5 2 5 4.1 CO[C@]12C=C[C@@]3(C[C@@H]1[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
57394218 68760 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 356 0 1 3 3.9 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1cccc(O)c13 10.1016/j.bmc.2011.11.047
CHEMBL1929364 68760 0 OPRD δ receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 356 0 1 3 3.9 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1cccc(O)c13 10.1016/j.bmc.2011.11.047
10651 3250 3 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 370 3 3 5 1.3 O=C1CC[C@@]2([C@@]3(C1)CCN([C@@H]2Cc1c3c(O)c(cc1)C(=O)N)CC1CC1)O 10.1016/j.bmcl.2009.02.078
11667832 3250 3 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 370 3 3 5 1.3 O=C1CC[C@@]2([C@@]3(C1)CCN([C@@H]2Cc1c3c(O)c(cc1)C(=O)N)CC1CC1)O 10.1016/j.bmcl.2009.02.078
CHEMBL426084 3250 3 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 370 3 3 5 1.3 O=C1CC[C@@]2([C@@]3(C1)CCN([C@@H]2Cc1c3c(O)c(cc1)C(=O)N)CC1CC1)O 10.1016/j.bmcl.2009.02.078
DB12543 3250 3 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 370 3 3 5 1.3 O=C1CC[C@@]2([C@@]3(C1)CCN([C@@H]2Cc1c3c(O)c(cc1)C(=O)N)CC1CC1)O 10.1016/j.bmcl.2009.02.078
CHEMBL229280 202981 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC[S+](C)[O-])NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm061369n
CHEMBL67846 197322 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 374 5 1 2 4.9 CCN(CC)C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL334369 204911 0 OPRD δ receptor Mouse 8.7 pEC50 = 8.7 Functional
In vitro bioassay data to determine the effective concentration required for antagonistic activity against Opioid receptor delta 1 in functional assay, MVDIn vitro bioassay data to determine the effective concentration required for antagonistic activity against Opioid receptor delta 1 in functional assay, MVD
ChEMBL None None None Cc1cc(O)cc(C)c1[C@@H](C)[C@H](N)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)O)C(C)(C)S)C(C)(C)S 10.1021/jm0303103
CHEMBL150625 202316 0 OPRD δ receptor Mouse 8.7 pEC50 = 8.7 Functional
Tested for electrically induced smooth muscle contractions from mouse vas deferens expressed in delta opioid receptorsTested for electrically induced smooth muscle contractions from mouse vas deferens expressed in delta opioid receptors
ChEMBL None None None Cc1cc(O)cc(C)c1[C@@H](C)[C@H](N)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(=O)O)C(C)(C)SSC1(C)C 10.1021/jm980374r
CHEMBL3786083 138253 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 429 3 2 4 4.2 O=C1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]3(O)CC/C1=C/c1ccccc1 10.1016/j.bmc.2016.03.040
CHEMBL229280 202981 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assayAgonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC[S+](C)[O-])NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm061369n
123924 3413 31 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
1611 3413 31 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
CHEMBL13470 3413 31 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
134338859 175548 0 OPRD δ receptor Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 4 5.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4446945 175548 0 OPRD δ receptor Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 4 5.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4595985 175548 0 OPRD δ receptor Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 4 5.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
11375776 157291 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 516 5 3 4 4.7 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(Br)c(-c2ccccc2)[nH]1 10.1021/jm030548r
CHEMBL408680 157291 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 516 5 3 4 4.7 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(Br)c(-c2ccccc2)[nH]1 10.1021/jm030548r
72735760 105595 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 438 2 2 5 4.1 Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL3139108 105595 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 438 2 2 5 4.1 Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL4296726 105595 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 438 2 2 5 4.1 Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL1627325 202336 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human recombinant delta opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of DPDPE-induced intracellular calcium mobilizationAntagonist activity at human recombinant delta opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of DPDPE-induced intracellular calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(C)(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)O 10.1021/jm900604g
72735387 105602 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 422 2 2 4 3.6 Oc1ccc2c(c1)[C@]13CCN(CC(F)F)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL3139134 105602 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 422 2 2 4 3.6 Oc1ccc2c(c1)[C@]13CCN(CC(F)F)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL4296727 105602 0 OPRD δ receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 422 2 2 4 3.6 Oc1ccc2c(c1)[C@]13CCN(CC(F)F)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
44439866 93020 0 OPRD δ receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 599 17 7 8 -1.7 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(C(N)=O)cc1)C(N)=O 10.1016/j.bmcl.2007.01.092
CHEMBL246956 93020 0 OPRD δ receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 599 17 7 8 -1.7 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(C(N)=O)cc1)C(N)=O 10.1016/j.bmcl.2007.01.092
44235490 189923 0 OPRD δ receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by scintillation counting
ChEMBL 384 2 2 2 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)C[C@@]1(C2)Cc1c([nH]c2ccccc12)C3 10.1016/j.bmcl.2009.06.093
CHEMBL562340 189923 0 OPRD δ receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by scintillation countingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by scintillation counting
ChEMBL 384 2 2 2 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)C[C@@]1(C2)Cc1c([nH]c2ccccc12)C3 10.1016/j.bmcl.2009.06.093
123924 3413 31 OPRD δ receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/jm8008986
1611 3413 31 OPRD δ receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/jm8008986
CHEMBL13470 3413 31 OPRD δ receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/jm8008986
104787 1376 16 OPRD δ receptor Mouse 8.0 pEC50 = 8 Functional
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 analysisAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.6b00748
1608 1376 16 OPRD δ receptor Mouse 8.0 pEC50 = 8 Functional
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 analysisAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.6b00748
CHEMBL31421 1376 16 OPRD δ receptor Mouse 8.0 pEC50 = 8 Functional
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 analysisAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.6b00748
DB08861 1376 16 OPRD δ receptor Mouse 8.0 pEC50 = 8 Functional
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 analysisAgonist 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
ChEMBL None None None None 10.1021/acs.jmedchem.6b00748
127049272 140171 0 OPRD δ receptor Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 497 7 3 4 4.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
CHEMBL3823231 140171 0 OPRD δ receptor Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 497 7 3 4 4.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
24768353 97059 0 OPRD δ receptor Human 8.0 pEC50 = 8 Binding
Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cellsDisplacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cells
ChEMBL 941 22 9 9 2.7 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm070332f
CHEMBL271619 97059 0 OPRD δ receptor Human 8.0 pEC50 = 8 Binding
Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cellsDisplacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cells
ChEMBL 941 22 9 9 2.7 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm070332f
69122130 178565 0 OPRD δ receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 432 6 4 7 0.7 CO[C@@]12CC[C@H](N[C@@H](CC(=O)O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4740360 178565 0 OPRD δ receptor Human 8.0 pEC50 = 8 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 432 6 4 7 0.7 CO[C@@]12CC[C@H](N[C@@H](CC(=O)O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
90656664 110234 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 499 6 2 5 4.7 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
CHEMBL3262361 110234 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysisAgonist activity at human delta opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 499 6 2 5 4.7 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
44421408 84045 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 406 1 2 5 3.0 CCn1c2c(c3c1[C@@H]1Oc4c(O)ccc5c4[C@@]14CCN(C)C(C5)[C@]4(O)C3)CCCC2 10.1021/jm040817t
CHEMBL222704 84045 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 406 1 2 5 3.0 CCn1c2c(c3c1[C@@H]1Oc4c(O)ccc5c4[C@@]14CCN(C)C(C5)[C@]4(O)C3)CCCC2 10.1021/jm040817t
72713097 105688 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 8 1 3 5.5 C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N(C)CC3CC3)C[C@]1(c1cccc(O)c1)C2 10.1021/jm401250s
CHEMBL3139482 105688 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 8 1 3 5.5 C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N(C)CC3CC3)C[C@]1(c1cccc(O)c1)C2 10.1021/jm401250s
CHEMBL3217271 105688 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 8 1 3 5.5 C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N(C)CC3CC3)C[C@]1(c1cccc(O)c1)C2 10.1021/jm401250s
CHEMBL4649733 177363 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 490 3 2 4 4.5 O=C(CCc1ccccc1)N1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2020.127176
10598391 18154 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Binding
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
ChEMBL 423 7 1 4 4.3 CCN(CC)C(=O)c1ccc(C(c2cccc(OC)c2)N2CC(C)(C)NCC2C)cc1 10.1021/jm000228x
CHEMBL127434 18154 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Binding
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
ChEMBL 423 7 1 4 4.3 CCN(CC)C(=O)c1ccc(C(c2cccc(OC)c2)N2CC(C)(C)NCC2C)cc1 10.1021/jm000228x
102270004 112123 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 488 4 3 6 2.5 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2C2=C(C[C@H](CCO)C(=O)N2Cc2ccccc2)C[C@@]3(O)[C@H]1C5 10.1016/j.bmc.2014.05.065
CHEMBL3309510 112123 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 488 4 3 6 2.5 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2C2=C(C[C@H](CCO)C(=O)N2Cc2ccccc2)C[C@@]3(O)[C@H]1C5 10.1016/j.bmc.2014.05.065
10596575 19011 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.
ChEMBL 390 6 1 3 4.6 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(C(C)=O)c2)cc1 10.1021/jm000229p
CHEMBL129300 19011 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.
ChEMBL 390 6 1 3 4.6 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(C(C)=O)c2)cc1 10.1021/jm000229p
16219954 59372 5 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@@H](C)N(C(c2ccc(C(=O)N(CC)CC)cc2)c2cccc(OC)c2)C[C@@H]1C nan
CHEMBL1730890 59372 5 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@@H](C)N(C(c2ccc(C(=O)N(CC)CC)cc2)c2cccc(OC)c2)C[C@@H]1C nan
69121986 180334 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 446 7 4 7 1.1 CO[C@@]12CC[C@H](N[C@@H](CCC(=O)O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4761211 180334 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 446 7 4 7 1.1 CO[C@@]12CC[C@H](N[C@@H](CCC(=O)O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
44254955 188750 0 OPRD δ receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 388 2 1 3 4.3 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1CCCCC1 10.1021/jm900773n
CHEMBL550261 188750 0 OPRD δ receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 388 2 1 3 4.3 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1CCCCC1 10.1021/jm900773n
44254585 188915 0 OPRD δ receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 424 4 1 3 4.9 CN(Cc1ccccc1)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL551536 188915 0 OPRD δ receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 424 4 1 3 4.9 CN(Cc1ccccc1)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
1044308 118321 11 OPRD δ receptor Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 474 4 0 4 6.8 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccccc2F)cc1 10.1021/acs.jmedchem.5b00007
CHEMBL3426792 118321 11 OPRD δ receptor Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 474 4 0 4 6.8 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccccc2F)cc1 10.1021/acs.jmedchem.5b00007
1009511 118323 10 OPRD δ receptor Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 474 4 0 4 6.8 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.5b00007
CHEMBL3426794 118323 10 OPRD δ receptor Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 474 4 0 4 6.8 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.5b00007
118737393 118325 0 OPRD δ receptor Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 524 4 0 4 8.0 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2cccc(Cl)c2Cl)cc1 10.1021/acs.jmedchem.5b00007
CHEMBL3426796 118325 0 OPRD δ receptor Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 524 4 0 4 8.0 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2cccc(Cl)c2Cl)cc1 10.1021/acs.jmedchem.5b00007
127043614 139652 0 OPRD δ receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
ChEMBL 457 5 2 4 5.3 CN(C)C[C@H]1CCc2cc(-c3ccccc3OC(F)(F)F)ccc2[C@]1(O)c1cccc(O)c1 10.1021/acsmedchemlett.5b00423
CHEMBL3809323 139652 0 OPRD δ receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
ChEMBL 457 5 2 4 5.3 CN(C)C[C@H]1CCc2cc(-c3ccccc3OC(F)(F)F)ccc2[C@]1(O)c1cccc(O)c1 10.1021/acsmedchemlett.5b00423
118737392 118322 0 OPRD δ receptor Human 6.0 pEC50 = 6 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 474 4 0 4 6.8 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2cccc(F)c2)cc1 10.1021/acs.jmedchem.5b00007
CHEMBL3426793 118322 0 OPRD δ receptor Human 6.0 pEC50 = 6 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 474 4 0 4 6.8 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2cccc(F)c2)cc1 10.1021/acs.jmedchem.5b00007
118737398 118330 0 OPRD δ receptor Human 6.0 pEC50 = 6 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 486 5 1 5 6.2 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccccc2CO)cc1 10.1021/acs.jmedchem.5b00007
CHEMBL3426801 118330 0 OPRD δ receptor Human 6.0 pEC50 = 6 Binding
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
ChEMBL 486 5 1 5 6.2 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccccc2CO)cc1 10.1021/acs.jmedchem.5b00007
CHEMBL2112214 77933 0 OPRD δ receptor Human 5.0 pEC50 = 5 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 518 6 0 2 7.8 CC1CCCC(C)N1C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
71819403 91380 0 OPRD δ receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay
ChEMBL 317 1 2 5 0.7 COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](O)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
CHEMBL2418741 91380 0 OPRD δ receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assayAgonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay
ChEMBL 317 1 2 5 0.7 COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](O)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
118725843 116421 0 OPRD δ receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assay
ChEMBL 349 5 1 5 3.1 Cc1ccc(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)nc1 10.1016/j.bmcl.2014.12.064
CHEMBL3393993 116421 0 OPRD δ receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assay
ChEMBL 349 5 1 5 3.1 Cc1ccc(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)nc1 10.1016/j.bmcl.2014.12.064
118725849 116426 0 OPRD δ receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assay
ChEMBL 391 5 1 6 4.0 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1nc2ccccc2s1 10.1016/j.bmcl.2014.12.064
CHEMBL3393999 116426 0 OPRD δ receptor Human 4.0 pEC50 = 4 Functional
Agonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assay
ChEMBL 391 5 1 6 4.0 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1nc2ccccc2s1 10.1016/j.bmcl.2014.12.064
CHEMBL4755700 179848 0 OPRD δ receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting methodAgonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting method
ChEMBL 549 11 1 3 5.7 CCC(=O)N(Cc1cccc(Cl)c1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
57978865 80685 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 420 7 3 4 4.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(C(C)C)[C@@H](C)c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL2159117 80685 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 420 7 3 4 4.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(C(C)C)[C@@H](C)c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
9888152 195597 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Compound was evaluated in 3 determinations for the agonistic activity in the Opioid receptor delta 1 of mouse vas deferensCompound was evaluated in 3 determinations for the agonistic activity in the Opioid receptor delta 1 of mouse vas deferens
ChEMBL 416 2 2 4 4.0 CCO[C@@]12Cc3c([nH]c4ccccc34)[C@]3(C)Oc4c(O)ccc5c4[C@]13CCN(C)[C@@H]2C5 10.1016/S0960-894X(96)00599-9
CHEMBL608246 195597 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Compound was evaluated in 3 determinations for the agonistic activity in the Opioid receptor delta 1 of mouse vas deferensCompound was evaluated in 3 determinations for the agonistic activity in the Opioid receptor delta 1 of mouse vas deferens
ChEMBL 416 2 2 4 4.0 CCO[C@@]12Cc3c([nH]c4ccccc34)[C@]3(C)Oc4c(O)ccc5c4[C@]13CCN(C)[C@@H]2C5 10.1016/S0960-894X(96)00599-9
CHEMBL407057 206148 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O 10.1021/jm050921q
3432723 29518 1 OPRD δ receptor Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 337 5 1 3 3.4 CN(C)C(CNC(=O)c1cnc(Cl)c(Cl)c1)c1ccccc1 nan
CHEMBL1388222 29518 1 OPRD δ receptor Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 337 5 1 3 3.4 CN(C)C(CNC(=O)c1cnc(Cl)c(Cl)c1)c1ccccc1 nan
44573444 184751 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by ALPHAscreen assayAgonist activity at delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by ALPHAscreen assay
ChEMBL 337 4 1 5 2.5 Nc1ccnc(N2CCC(N(C(=O)C3CC3)c3ccccn3)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL493781 184751 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by ALPHAscreen assayAgonist activity at delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by ALPHAscreen assay
ChEMBL 337 4 1 5 2.5 Nc1ccnc(N2CCC(N(C(=O)C3CC3)c3ccccn3)CC2)c1 10.1016/j.bmcl.2009.01.106
117738965 116981 0 OPRD δ receptor Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayAgonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 542 5 3 8 3.2 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2cc([N+](=O)[O-])ccc2cn1 10.1016/j.bmc.2015.02.055
CHEMBL3401554 116981 0 OPRD δ receptor Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayAgonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 542 5 3 8 3.2 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2cc([N+](=O)[O-])ccc2cn1 10.1016/j.bmc.2015.02.055
CHEMBL2112215 77934 0 OPRD δ receptor Human 6.0 pEC50 = 6.0 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 504 9 0 2 7.4 C=C(C)CN(CC)C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
16756840 141560 0 OPRD δ receptor Rat 6.0 pEC50 = 6.0 Functional
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 methodAgonist 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
ChEMBL 337 4 2 3 3.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1 10.1016/j.bmc.2017.02.064
CHEMBL388873 141560 0 OPRD δ receptor Rat 6.0 pEC50 = 6.0 Functional
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 methodAgonist 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
ChEMBL 337 4 2 3 3.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1 10.1016/j.bmc.2017.02.064
10033203 202655 29 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting methodAgonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1021/acs.jmedchem.0c00901
CHEMBL20226 202655 29 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting methodAgonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1021/acs.jmedchem.0c00901
71460943 82062 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysis
ChEMBL 536 4 1 5 6.3 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2ncc(-c4ccc(Cl)cc4)cc2C[C@@]3(OCc2ccccc2)[C@H]1C5 10.1021/jm300686p
CHEMBL2179654 82062 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysisAgonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysis
ChEMBL 536 4 1 5 6.3 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2ncc(-c4ccc(Cl)cc4)cc2C[C@@]3(OCc2ccccc2)[C@H]1C5 10.1021/jm300686p
56589680 110478 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 460 2 1 6 2.5 CN1CC[C@@]23c4c5ccc(O)c4OCO[C@]46CC[C@@]2(O[C@H](C(=O)N4Cc2ccccc2)[C@H]63)[C@H]1C5 10.1021/ml400491k
CHEMBL3264743 110478 0 OPRD δ receptor Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 460 2 1 6 2.5 CN1CC[C@@]23c4c5ccc(O)c4OCO[C@]46CC[C@@]2(O[C@H](C(=O)N4Cc2ccccc2)[C@H]63)[C@H]1C5 10.1021/ml400491k
145963594 160589 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay
ChEMBL 1080 12 10 14 0.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1016/j.bmc.2018.05.045
CHEMBL4126803 160589 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay
ChEMBL 1080 12 10 14 0.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1016/j.bmc.2018.05.045
69122691 179143 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 432 6 4 7 0.7 CO[C@@]12CC[C@@H](N[C@@H](CC(=O)O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4747179 179143 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 432 6 4 7 0.7 CO[C@@]12CC[C@@H](N[C@@H](CC(=O)O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
102270007 112121 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 412 2 3 6 0.9 CN1C(=O)[C@H](CCO)CC2=C1[C@@H]1Oc3c(O)ccc4c3[C@@]13CCN(C)[C@H](C4)[C@]3(O)C2 10.1016/j.bmc.2014.05.065
CHEMBL3309508 112121 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 412 2 3 6 0.9 CN1C(=O)[C@H](CCO)CC2=C1[C@@H]1Oc3c(O)ccc4c3[C@@]13CCN(C)[C@H](C4)[C@]3(O)C2 10.1016/j.bmc.2014.05.065
CHEMBL407057 206148 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O 10.1021/jm050921q
44421406 84053 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 522 5 2 5 5.0 Oc1ccc2c3c1O[C@H]1c4c(c5c(n4CCc4ccccc4)CCCC5)C[C@@]4(O)C(C2)N(CC2CC2)CC[C@]314 10.1021/jm040817t
CHEMBL222762 84053 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 522 5 2 5 5.0 Oc1ccc2c3c1O[C@H]1c4c(c5c(n4CCc4ccccc4)CCCC5)C[C@@]4(O)C(C2)N(CC2CC2)CC[C@]314 10.1021/jm040817t
44254503 188722 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 320 2 2 3 2.7 NC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL550063 188722 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 320 2 2 3 2.7 NC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
44254859 188897 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 334 2 2 3 3.0 CNC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL551413 188897 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 334 2 2 3 3.0 CNC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
23634921 145647 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 832 19 7 9 2.3 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
CHEMBL392206 145647 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 832 19 7 9 2.3 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
10320450 86183 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/jm400050y
CHEMBL2322568 86183 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/jm400050y
CHEMBL4444479 86183 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/jm400050y
10320450 86183 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL2322568 86183 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4444479 86183 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
10320450 86183 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.5b01270
CHEMBL2322568 86183 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.5b01270
CHEMBL4444479 86183 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.5b01270
5748293 108970 11 OPRD δ receptor Human 6.0 pEC50 = 6.0 Functional
Concentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human opioid receptor delta 1 expressed in CHO cellsConcentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human opioid receptor delta 1 expressed in CHO cells
ChEMBL 355 4 0 4 3.1 COc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3 10.1021/jm031126k
CHEMBL1628270 108970 11 OPRD δ receptor Human 6.0 pEC50 = 6.0 Functional
Concentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human opioid receptor delta 1 expressed in CHO cellsConcentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human opioid receptor delta 1 expressed in CHO cells
ChEMBL 355 4 0 4 3.1 COc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3 10.1021/jm031126k
CHEMBL322796 108970 11 OPRD δ receptor Human 6.0 pEC50 = 6.0 Functional
Concentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human opioid receptor delta 1 expressed in CHO cellsConcentration necessary to produce 50% of the Emax value, i.e. to stimulate [35S]GTP-gamma-S, binding to recombinant human opioid receptor delta 1 expressed in CHO cells
ChEMBL 355 4 0 4 3.1 COc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3 10.1021/jm031126k
16746145 50431 0 OPRD δ receptor Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 659 7 3 6 6.9 CCN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(NC(=O)c4cnc5cc(C(F)(F)F)ccc5c4O)c3)cc2C(F)(F)F)CC1 nan
CHEMBL1577639 50431 0 OPRD δ receptor Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 659 7 3 6 6.9 CCN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(NC(=O)c4cnc5cc(C(F)(F)F)ccc5c4O)c3)cc2C(F)(F)F)CC1 nan
10278214 196651 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 492 9 0 2 7.2 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL63750 196651 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 492 9 0 2 7.2 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
23634921 145647 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 832 19 7 9 2.3 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
CHEMBL392206 145647 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 832 19 7 9 2.3 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
CHEMBL4786173 182859 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 369 4 3 4 2.7 CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1 10.1016/j.ejmech.2020.112070
CHEMBL4803577 182859 0 OPRD δ receptor Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 369 4 3 4 2.7 CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1 10.1016/j.ejmech.2020.112070
10786358 18456 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Binding
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
ChEMBL 385 6 1 3 3.8 CCN(CC)C(=O)c1ccc(C(c2ccc(Cl)cc2)N2CCNCC2)cc1 10.1021/jm000228x
CHEMBL128006 18456 0 OPRD δ receptor Human 7.0 pEC50 = 7.0 Binding
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
ChEMBL 385 6 1 3 3.8 CCN(CC)C(=O)c1ccc(C(c2ccc(Cl)cc2)N2CCNCC2)cc1 10.1021/jm000228x
CHEMBL4759079 180139 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1172 35 15 15 -3.2 CSCC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL382349 205815 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Activity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to human delta opioid receptor expressed in HN9.10 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
CHEMBL4759079 180139 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1172 35 15 15 -3.2 CSCC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
49863732 14974 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1266 18 10 12 6.1 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC1(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm100157m
CHEMBL1214025 14974 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1266 18 10 12 6.1 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC1(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm100157m
4391932 32629 7 OPRD δ receptor Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 333 5 2 2 4.3 CN(C)C(CN=C(S)Nc1cccc(Cl)c1)c1ccccc1 nan
CHEMBL1416425 32629 7 OPRD δ receptor Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 333 5 2 2 4.3 CN(C)C(CN=C(S)Nc1cccc(Cl)c1)c1ccccc1 nan
118725858 116436 0 OPRD δ receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assay
ChEMBL 402 6 2 7 1.5 CS(=O)(=O)c1c[nH]c(C(=O)Nc2nc3cccnc3n2CCN2CCCC2)c1 10.1016/j.bmcl.2014.12.064
CHEMBL3394008 116436 0 OPRD δ receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assay
ChEMBL 402 6 2 7 1.5 CS(=O)(=O)c1c[nH]c(C(=O)Nc2nc3cccnc3n2CCN2CCCC2)c1 10.1016/j.bmcl.2014.12.064
CHEMBL47545 207497 12 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assayInverse agonist activity at human DOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL None None None C=CCN(CC=C)[C@@H](Cc1ccc(O)cc1)C(=O)NC(C)(C)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)O 10.1016/j.bmcl.2015.05.038
3863202 43118 14 OPRD δ receptor Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 484 3 1 7 5.4 COc1ccc(C2C(C#N)=C(N)N(c3sc4c(c3C#N)CCCC4)C3=C2C(=O)CC(C)(C)C3)cc1 nan
CHEMBL1509052 43118 14 OPRD δ receptor Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 484 3 1 7 5.4 COc1ccc(C2C(C#N)=C(N)N(c3sc4c(c3C#N)CCCC4)C3=C2C(=O)CC(C)(C)C3)cc1 nan
145963594 160589 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay
ChEMBL 1080 12 10 14 0.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1016/j.bmc.2018.05.045
CHEMBL4126803 160589 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assayAgonist activity at DOR (unknown origin) expressed in HEK cells assessed as reduction in cAMP accumulation by split luciferase assay
ChEMBL 1080 12 10 14 0.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1016/j.bmc.2018.05.045
44406109 71687 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist potency assessed by [35S]GTP-gammaS binding assay in C6 Glioma cells expressing cloned human delta opioid receptorAgonist potency assessed by [35S]GTP-gammaS binding assay in C6 Glioma cells expressing cloned human delta opioid receptor
ChEMBL 388 5 1 3 4.0 CCNC(=O)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1 10.1016/j.bmcl.2005.09.025
CHEMBL198238 71687 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist potency assessed by [35S]GTP-gammaS binding assay in C6 Glioma cells expressing cloned human delta opioid receptorAgonist potency assessed by [35S]GTP-gammaS binding assay in C6 Glioma cells expressing cloned human delta opioid receptor
ChEMBL 388 5 1 3 4.0 CCNC(=O)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1 10.1016/j.bmcl.2005.09.025
44406224 72028 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist potency assessed by [35S]GTP-gammaS binding assay in C6 Glioma cells expressing cloned human delta opioid receptorAgonist potency assessed by [35S]GTP-gammaS binding assay in C6 Glioma cells expressing cloned human delta opioid receptor
ChEMBL 466 6 1 4 5.6 COc1ccccc1NC(=O)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1 10.1016/j.bmcl.2005.09.025
CHEMBL199378 72028 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist potency assessed by [35S]GTP-gammaS binding assay in C6 Glioma cells expressing cloned human delta opioid receptorAgonist potency assessed by [35S]GTP-gammaS binding assay in C6 Glioma cells expressing cloned human delta opioid receptor
ChEMBL 466 6 1 4 5.6 COc1ccccc1NC(=O)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1 10.1016/j.bmcl.2005.09.025
CHEMBL4785222 181512 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1128 33 16 15 -5.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4785222 181512 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1128 33 16 15 -5.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
5461578 66921 1 OPRD δ receptor Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 533 10 2 9 2.7 COC(=O)C1=C(C)N(CCCC(=O)O)C(=O)NC1c1ccccc1OS(=O)(=O)c1ccc([N+](=O)[O-])cc1 nan
CHEMBL1893806 66921 1 OPRD δ receptor Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 533 10 2 9 2.7 COC(=O)C1=C(C)N(CCCC(=O)O)C(=O)NC1c1ccccc1OS(=O)(=O)c1ccc([N+](=O)[O-])cc1 nan
CHEMBL4749564 179334 0 OPRD δ receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1115 32 14 14 -2.5 CSCC[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
2447421 59396 6 OPRD δ receptor Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 471 3 1 3 3.1 O=S(=O)(c1c(Cl)cc(Br)cc1Cl)N1CCN(C(=S)NC2CC2)CC1 nan
CHEMBL1731939 59396 6 OPRD δ receptor Human 4.9 pEC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high throughput dose response assay to identify agonists of OPRD1 homodimerization. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 471 3 1 3 3.1 O=S(=O)(c1c(Cl)cc(Br)cc1Cl)N1CCN(C(=S)NC2CC2)CC1 nan
44421422 84065 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 482 3 2 5 4.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CCc2ccccc2)CCCC4)C[C@@]3(O)C1C5 10.1021/jm040817t
CHEMBL222814 84065 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 482 3 2 5 4.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CCc2ccccc2)CCCC4)C[C@@]3(O)C1C5 10.1021/jm040817t
16730815 184551 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by ALPHAscreen assayAgonist activity at delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by ALPHAscreen assay
ChEMBL 380 4 1 5 3.1 CCN(CC)C(=O)[C@H]1OC2(CCN(c3cc(N)ccn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.01.106
CHEMBL492552 184551 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by ALPHAscreen assayAgonist activity at delta opioid receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by ALPHAscreen assay
ChEMBL 380 4 1 5 3.1 CCN(CC)C(=O)[C@H]1OC2(CCN(c3cc(N)ccn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.01.106
118725853 116431 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assay
ChEMBL 369 6 2 5 3.4 CSc1c[nH]c(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)c1 10.1016/j.bmcl.2014.12.064
CHEMBL3394003 116431 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assayAgonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assay
ChEMBL 369 6 2 5 3.4 CSc1c[nH]c(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)c1 10.1016/j.bmcl.2014.12.064
122187724 122290 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL 692 11 5 6 5.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2015.06.030
CHEMBL3609620 122290 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL 692 11 5 6 5.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2015.06.030
155542413 175445 0 OPRD δ receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 507 7 3 5 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4521319 175445 0 OPRD δ receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 507 7 3 5 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4595172 175445 0 OPRD δ receptor Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 507 7 3 5 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
9951665 101904 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 377 6 1 3 4.6 CCN(CC)C(=O)c1ccc(N(c2ccccc2)C2C[C@@H]3CC[C@H](C2)N3)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL304196 101904 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 377 6 1 3 4.6 CCN(CC)C(=O)c1ccc(N(c2ccccc2)C2C[C@@H]3CC[C@H](C2)N3)cc1 10.1016/j.bmcl.2004.02.051
9888235 197274 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 417 8 0 3 5.5 C=CCN1[C@H]2CC[C@@H]1CC(N(c1ccccc1)c1ccc(C(=O)N(CC)CC)cc1)C2 10.1016/j.bmcl.2004.02.051
CHEMBL67545 197274 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 417 8 0 3 5.5 C=CCN1[C@H]2CC[C@@H]1CC(N(c1ccccc1)c1ccc(C(=O)N(CC)CC)cc1)C2 10.1016/j.bmcl.2004.02.051
10833535 116722 0 OPRD δ receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay.
ChEMBL 378 6 1 3 4.4 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(OC)cc2)cc1 10.1021/jm000229p