Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
54669894 80355 0 None 60 2 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 80355 0 None 60 2 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 200897 0 None 1 5 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 200897 0 None 1 5 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 194272 0 None - 1 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 194272 0 None - 1 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 194272 0 None - 1 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 194272 0 None - 1 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
1607 1279 31 None -3 5 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 1279 31 None -3 5 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 1279 31 None -3 5 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 1279 31 None -3 5 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 200897 0 None 1 5 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 200897 0 None 1 5 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 193762 0 None - 1 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 193762 0 None - 1 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 193762 0 None - 1 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 193762 0 None - 1 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 194996 0 None - 1 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 194996 0 None - 1 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 194996 0 None - 1 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 194996 0 None - 1 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 56920 0 None 1 3 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 56920 0 None 1 3 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 56920 0 None 1 3 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 56920 0 None 1 3 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 56921 0 None -1 3 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 56921 0 None -1 3 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 56921 0 None -1 3 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 56921 0 None -1 3 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 2265 40 None -1 6 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 2265 40 None -1 6 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 2265 40 None -1 6 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 2265 40 None -1 6 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 2265 40 None -1 6 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 137116 0 None -4 2 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 137116 0 None -4 2 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 56926 0 None -6 3 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 56926 0 None -6 3 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 56926 0 None -6 3 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 56926 0 None -6 3 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 56917 0 None 1 3 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 56917 0 None 1 3 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 60931 0 None -4 5 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 60931 0 None -4 5 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
71456262 79047 0 None -2 3 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 79047 0 None -2 3 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 2688 6 None 2 7 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 2688 6 None 2 7 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 2688 6 None 2 7 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 2688 6 None 2 7 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
50994530 56925 0 None 1 3 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 56925 0 None 1 3 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
50994530 56925 0 None 1 3 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 56925 0 None 1 3 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 60931 0 None -4 5 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 60931 0 None -4 5 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 8393 0 None - 1 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 8393 0 None - 1 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 14005 0 None 16 4 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 14005 0 None 16 4 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 14005 0 None 16 4 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 209149 0 None -2 6 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 83757 0 None -1 3 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 83757 0 None -1 3 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 56922 0 None 1 3 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 56922 0 None 1 3 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 84936 0 None 74 3 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 84936 0 None 74 3 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 56922 0 None 1 3 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 56922 0 None 1 3 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 65326 0 None -2 3 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 65326 0 None -2 3 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 84952 0 None 2 3 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 84952 0 None 2 3 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 84952 0 None 2 3 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
168290357 191310 0 None 9 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting methodAgonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method
ChEMBL 458 4 1 4 4.1 CN(C(=O)c1ccccc1)[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
CHEMBL5200050 191310 0 None 9 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting methodAgonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method
ChEMBL 458 4 1 4 4.1 CN(C(=O)c1ccccc1)[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
57394219 68992 0 None - 1 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 68992 0 None - 1 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 14062 0 None -36 4 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 14062 0 None -36 4 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 14062 0 None -36 4 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 56927 0 None -2 3 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 56927 0 None -2 3 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 60933 0 None 1 5 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 60933 0 None 1 5 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 201942 0 None - 1 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 201942 0 None - 1 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 56927 0 None -2 3 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 56927 0 None -2 3 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 195643 0 None - 1 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 195643 0 None - 1 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 197273 0 None - 1 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 197273 0 None - 1 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 208658 0 None 6 3 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 159043 0 None 6 3 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 159043 0 None 6 3 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 195710 0 None - 1 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 195710 0 None - 1 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 208694 0 None 19 3 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 3616 0 None 1 2 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 3616 0 None 1 2 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 3616 0 None 1 2 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
44279699 98834 0 None -7 3 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 98834 0 None -7 3 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 14064 0 None 1 4 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 14064 0 None 1 4 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 14064 0 None 1 4 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 83755 0 None -1 3 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 83755 0 None -1 3 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 157331 0 None - 1 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 157331 0 None - 1 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
71452746 78771 0 None 549 2 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 78771 0 None 549 2 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 1281 0 None 18620 2 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 1281 0 None 18620 2 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 208659 0 None -1 3 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
162676940 182746 0 None 32 5 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
CHEMBL4797394 182746 0 None 32 5 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 156049 0 None - 1 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 156049 0 None - 1 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
122187205 122487 0 None 15 3 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 122487 0 None 15 3 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
119029 742 29 None 1 5 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 742 29 None 1 5 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 742 29 None 1 5 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 200165 0 None -10 3 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 200165 0 None -10 3 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 110721 0 None 6 3 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 110721 0 None 6 3 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 155418 0 None 10 2 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 155418 0 None 10 2 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 156623 0 None - 1 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 156623 0 None - 1 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 156685 0 None 13 3 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 156685 0 None 13 3 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 158304 0 None -2 2 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 158304 0 None -2 2 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 60933 0 None 1 5 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 60933 0 None 1 5 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 84901 0 None - 1 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 84901 0 None - 1 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
73353599 91195 0 None 12 3 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 91195 0 None 12 3 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
10093250 201380 0 None - 1 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
CHEMBL63732 201380 0 None - 1 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 157735 0 None 2 3 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 157735 0 None 2 3 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 18067 4 None 446 3 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 18067 4 None 446 3 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 18067 4 None 446 3 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 157735 0 None 2 3 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 157735 0 None 2 3 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 155879 0 None - 1 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 155879 0 None - 1 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 209149 0 None -2 6 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
45486055 195780 0 None - 1 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 195780 0 None - 1 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 60934 0 None 1 5 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 60934 0 None 1 5 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 82299 0 None 7 2 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 82299 0 None 7 2 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 60934 0 None 1 5 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 60934 0 None 1 5 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 158439 0 None 8 3 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 158439 0 None 8 3 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
90306849 110466 0 None -1 3 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 110466 0 None -1 3 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
117706010 158873 0 None - 1 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 158873 0 None - 1 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 93795 0 None 1 3 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 93795 0 None 1 3 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 59798 0 None 1 3 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 59798 0 None 1 3 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 59798 0 None 1 3 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 3693 6 None 3 3 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 3693 6 None 3 3 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 3693 6 None 3 3 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 3693 6 None 3 3 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 3693 6 None 3 3 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 3693 6 None 3 3 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
24768397 145885 0 None -7 3 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 145885 0 None -7 3 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 88080 0 None 1 3 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 88080 0 None 1 3 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 145885 0 None -7 3 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 145885 0 None -7 3 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 88080 0 None 1 3 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 88080 0 None 1 3 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 105824 0 None - 1 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 105824 0 None - 1 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 105824 0 None - 1 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 182239 0 None 22 5 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 182239 0 None 22 5 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
58443234 83759 0 None -2 3 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 83759 0 None -2 3 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 137062 0 None 158 3 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 137062 0 None 158 3 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
127032209 138632 0 None - 1 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
CHEMBL3787263 138632 0 None - 1 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 160354 0 None 2 2 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 160354 0 None 2 2 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 136689 0 None -1 3 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 136689 0 None -1 3 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 170566 0 None 1 6 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 170566 0 None 1 6 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 137254 0 None 51 2 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 137254 0 None 51 2 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 78766 0 None 30 3 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 78766 0 None 30 3 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 85363 0 None -1 3 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 85363 0 None -1 3 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 210546 0 None 8 5 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 210546 0 None 8 5 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 76995 0 None -1 3 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 76995 0 None -1 3 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 76995 0 None 1 3 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 76995 0 None 1 3 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 19083 0 None 776 3 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 19083 0 None 776 3 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
10435156 78770 0 None 5 3 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 78770 0 None 5 3 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
44178113 60935 0 None -39 5 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 60935 0 None -39 5 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 110720 0 None 4 3 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 110720 0 None 4 3 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
1613 2265 40 None -1 6 Human 9.0 pEC50 = 9 Functional
Agonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation levelAgonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation level
ChEMBL None None None None 10.1021/acs.jmedchem.2c01061
3903 2265 40 None -1 6 Human 9.0 pEC50 = 9 Functional
Agonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation levelAgonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation level
ChEMBL None None None None 10.1021/acs.jmedchem.2c01061
461776 2265 40 None -1 6 Human 9.0 pEC50 = 9 Functional
Agonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation levelAgonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation level
ChEMBL None None None None 10.1021/acs.jmedchem.2c01061
CHEMBL15038 2265 40 None -1 6 Human 9.0 pEC50 = 9 Functional
Agonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation levelAgonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation level
ChEMBL None None None None 10.1021/acs.jmedchem.2c01061
CHEMBL8234 2265 40 None -1 6 Human 9.0 pEC50 = 9 Functional
Agonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation levelAgonist activity at human DOR expressed in CHO cells assessed as reduction in ERK1/2 phosphorylation level
ChEMBL None None None None 10.1021/acs.jmedchem.2c01061
5487663 72494 11 None -1 4 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 72494 11 None -1 4 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 60935 0 None -39 5 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 60935 0 None -39 5 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
1614 2459 37 None 3 4 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 2459 37 None 3 4 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 2459 37 None 3 4 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 2459 37 None 3 4 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 2459 37 None 3 4 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 2459 37 None 3 4 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 2459 37 None 3 4 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 2459 37 None 3 4 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 18095 0 None - 1 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 18095 0 None - 1 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 18095 0 None - 1 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
127032208 138607 0 None 2 3 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
CHEMBL3787016 138607 0 None 2 3 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 59799 0 None 3 3 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 59799 0 None 3 3 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 59799 0 None 3 3 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
72735204 105832 0 None 97 2 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 105832 0 None 97 2 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 105832 0 None 97 2 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 72494 11 None -1 4 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 72494 11 None -1 4 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 208698 0 None -1 3 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 72494 11 None -1 4 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 72494 11 None -1 4 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 110715 0 None 1 3 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 110715 0 None 1 3 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 208662 0 None 1 3 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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
44279686 103925 0 None -10 3 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 103925 0 None -10 3 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 72494 11 None -1 4 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 72494 11 None -1 4 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
5487663 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 72494 11 None -1 4 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 196655 0 None - 1 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 196655 0 None - 1 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
45486101 195772 0 None - 1 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 195772 0 None - 1 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
45486102 195814 0 None - 1 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 195814 0 None - 1 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 83765 0 None 1 3 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 83765 0 None 1 3 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 157155 0 None 2 2 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 157155 0 None 2 2 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 78767 0 None 79 3 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 78767 0 None 79 3 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 105863 0 None - 1 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 105863 0 None - 1 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 105863 0 None - 1 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 117673 0 None -5 3 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 117673 0 None -5 3 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 195825 0 None - 1 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 195825 0 None - 1 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
89435280 156723 0 None 1 2 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 156723 0 None 1 2 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 160763 0 None 6 5 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 160763 0 None 6 5 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 209149 0 None -2 6 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 160763 0 None 6 5 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 160763 0 None 6 5 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 105852 0 None 11 3 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 105852 0 None 11 3 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 105852 0 None 11 3 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 97414 0 None -14 4 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 97414 0 None -14 4 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 97414 0 None -14 4 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
127033399 138497 0 None 2 2 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
CHEMBL3785854 138497 0 None 2 2 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 156721 0 None 15 2 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 156721 0 None 15 2 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 186959 0 None - 1 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 186959 0 None - 1 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 3693 6 None 3 3 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 3693 6 None 3 3 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 3693 6 None 3 3 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 170566 0 None -1 6 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 170566 0 None -1 6 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 170566 0 None -1 6 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 170566 0 None -1 6 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 122584 0 None - 1 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 122584 0 None - 1 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 78763 0 None 3 2 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 78763 0 None 3 2 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 105888 0 None 81 2 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 105888 0 None 81 2 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 105888 0 None 81 2 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 195640 0 None - 1 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 195640 0 None - 1 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
145961844 161105 0 None 2 3 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 161105 0 None 2 3 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 161105 0 None 2 3 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 161105 0 None 2 3 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 84900 0 None 15 3 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 84900 0 None 15 3 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 156717 0 None -5 2 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 156717 0 None -5 2 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
CHEMBL294616 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 209149 0 None -2 6 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 105857 0 None 10 2 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 105857 0 None 10 2 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 105857 0 None 10 2 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 208655 0 None 3 3 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 114283 0 None -51 3 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 114283 0 None -51 3 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
117706085 158660 0 None 3 3 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 158660 0 None 3 3 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
44301701 197147 2 None 1 6 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 197147 2 None 1 6 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 197147 2 None 1 6 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 197147 2 None 1 6 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
90656665 110467 0 None 1 3 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 110467 0 None 1 3 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 68991 0 None - 1 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 68991 0 None - 1 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 3409 6 None -4 3 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 3409 6 None -4 3 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 3409 6 None -4 3 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 3409 6 None -4 3 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 207713 0 None -4 4 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
9820950 202051 0 None - 1 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
CHEMBL67846 202051 0 None - 1 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 209651 0 None 2344 2 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 207048 0 None 2344 2 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
127033967 138518 0 None 10 3 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
CHEMBL3786083 138518 0 None 10 3 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 207713 0 None -4 4 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 3576 38 None 1 8 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 3576 38 None 1 8 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 3576 38 None 1 8 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
11375776 157568 0 None - 1 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 157568 0 None - 1 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 105835 0 None -1 2 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 105835 0 None -1 2 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 105835 0 None -1 2 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 207068 0 None -57 8 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 105842 0 None - 1 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 105842 0 None - 1 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 105842 0 None - 1 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 93259 0 None 26 2 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 93259 0 None 26 2 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 194655 0 None 3 3 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 194655 0 None 3 3 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 3576 38 None 1 8 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 3576 38 None 1 8 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 3576 38 None 1 8 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 1445 19 None -22 3 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 1445 19 None -22 3 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 1445 19 None -22 3 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 1445 19 None -22 3 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
1613 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
3903 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
461776 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
CHEMBL15038 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
CHEMBL8234 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
90656664 110472 0 None 3 3 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 110472 0 None 3 3 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
1613 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
3903 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
461776 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
CHEMBL15038 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
CHEMBL8234 2265 40 None -1 6 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment measured after 90 mins by PathHunter assay
ChEMBL None None None None 10.1039/D1MD00025J
44421408 84282 0 None 9 3 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 84282 0 None 9 3 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 105927 0 None -3 3 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 105927 0 None -3 3 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 105927 0 None -3 3 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
156021880 177640 0 None - 1 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
CHEMBL4649733 177640 0 None - 1 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
102270004 112363 0 None 8 2 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 112363 0 None 8 2 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 19198 0 None 1096 2 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 19198 0 None 1096 2 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 59595 6 None - 1 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 59595 6 None - 1 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
44254955 193482 0 None - 1 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 193482 0 None - 1 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 193647 0 None - 1 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 193647 0 None - 1 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
71459902 78170 0 None - 1 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
CHEMBL2112214 78170 0 None - 1 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 91620 0 None -15 3 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 91620 0 None -15 3 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 116666 0 None -1445 3 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 116666 0 None -1445 3 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 116671 0 None -812 3 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 116671 0 None -812 3 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
162655722 180136 0 None -2 2 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
CHEMBL4755700 180136 0 None -2 2 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 80921 0 None - 1 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 80921 0 None - 1 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
CHEMBL407057 210888 0 None -3 5 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 29708 1 None 4 2 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 29708 1 None 4 2 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 186845 0 None - 1 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 186845 0 None - 1 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 117226 0 None -3 4 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 117226 0 None -3 4 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
71450851 78171 0 None - 1 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
CHEMBL2112215 78171 0 None - 1 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
10033203 207387 33 None -25 3 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 207387 33 None -25 3 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 82298 0 None 19 3 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 82298 0 None 19 3 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 110716 0 None 9 3 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 110716 0 None 9 3 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 160867 0 None 1 3 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 160867 0 None 1 3 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
102270007 112361 0 None 13 2 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 112361 0 None 13 2 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 210888 0 None -3 5 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 84290 0 None -7 2 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 84290 0 None -7 2 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 193454 0 None - 1 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 193454 0 None - 1 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 193629 0 None - 1 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 193629 0 None - 1 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 145915 0 None -10 3 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 145915 0 None -10 3 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
5748293 109209 14 None -53 3 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 109209 14 None -53 3 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 109209 14 None -53 3 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 50639 0 None 1 2 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 50639 0 None 1 2 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
168291520 191323 0 None -21 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting methodAgonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method
ChEMBL 472 6 2 4 4.1 O=C(CCc1ccccc1)N[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
CHEMBL5200218 191323 0 None -21 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting methodAgonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method
ChEMBL 472 6 2 4 4.1 O=C(CCc1ccccc1)N[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
10278214 201381 0 None - 1 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 201381 0 None - 1 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 145915 0 None -10 3 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 145915 0 None -10 3 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
162658841 180430 0 None -2 5 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
CHEMBL4759079 180430 0 None -2 5 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 210555 0 None -15 5 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
162658841 180430 0 None -2 5 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
CHEMBL4759079 180430 0 None -2 5 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 15158 0 None -239 5 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 15158 0 None -239 5 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 32821 8 None -2 2 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 32821 8 None -2 2 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 116681 0 None -2 3 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 116681 0 None -2 3 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 212281 18 None 7 2 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 43320 15 None -1 2 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 43320 15 None -1 2 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 160867 0 None 1 3 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 160867 0 None 1 3 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 71921 0 None - 1 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 71921 0 None - 1 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 72262 0 None - 1 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 72262 0 None - 1 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
162666603 181804 0 None 2 5 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 181804 0 None 2 5 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
162666603 181804 0 None 2 5 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 181804 0 None 2 5 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 67150 1 None - 1 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 67150 1 None - 1 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
162651571 179620 0 None 2 4 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
CHEMBL4749564 179620 0 None 2 4 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 59619 6 None - 1 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 59619 6 None - 1 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 84302 0 None 10 3 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 84302 0 None 10 3 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 186645 0 None - 1 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 186645 0 None - 1 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 116676 0 None -12 3 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 116676 0 None -12 3 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 122550 0 None -7 3 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 122550 0 None -7 3 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
9951665 102143 0 None - 1 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 102143 0 None - 1 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 202003 0 None - 1 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 202003 0 None - 1 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 116967 0 None 1096 2 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
CHEMBL339922 116967 0 None 1096 2 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
127032211 138602 0 None -1 2 Human 7.9 pEC50 = 7.9 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 415 3 2 4 3.8 O=C1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]3(O)C/C1=C\c1ccccc1 10.1016/j.bmc.2016.03.040
CHEMBL3786970 138602 0 None -1 2 Human 7.9 pEC50 = 7.9 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 415 3 2 4 3.8 O=C1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]3(O)C/C1=C\c1ccccc1 10.1016/j.bmc.2016.03.040
1613 2265 40 None -1 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL None None None None 10.1021/acs.jnatprod.0c01036
3903 2265 40 None -1 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL None None None None 10.1021/acs.jnatprod.0c01036
461776 2265 40 None -1 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL None None None None 10.1021/acs.jnatprod.0c01036
CHEMBL15038 2265 40 None -1 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL None None None None 10.1021/acs.jnatprod.0c01036
CHEMBL8234 2265 40 None -1 6 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human delta opioid receptor expressed in CHO-K1 cells assessed as beta-arrestin2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL None None None None 10.1021/acs.jnatprod.0c01036
CHEMBL317956 209460 35 None -1 6 Mouse 7.9 pEC50 = 7.9 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 None None None CC(C)[C@H](NC(=O)[C@H](CC(=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/jm010449i
CHEMBL382349 210555 0 None -15 5 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
132082412 182221 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assayAgonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay
ChEMBL 522 5 0 9 4.4 COC(=O)[C@@H]1C=C(OC(=O)c2ccc(OC)cc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C 10.1021/acs.jmedchem.6b01235
CHEMBL4790712 182221 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assayAgonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay
ChEMBL 522 5 0 9 4.4 COC(=O)[C@@H]1C=C(OC(=O)c2ccc(OC)cc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C 10.1021/acs.jmedchem.6b01235
24768356 155321 0 None 1 3 Human 6.9 pEC50 = 6.9 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 1091 22 8 9 5.0 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)N(C)Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm070332f
CHEMBL406030 155321 0 None 1 3 Human 6.9 pEC50 = 6.9 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 1091 22 8 9 5.0 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)N(C)Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm070332f
49863732 15158 0 None -239 5 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 15158 0 None -239 5 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
49863734 15160 0 None -64 5 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 1477 21 11 14 6.8 CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC(C)(C)[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)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 10.1021/jm100157m
CHEMBL1214027 15160 0 None -64 5 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 1477 21 11 14 6.8 CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC(C)(C)[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)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 10.1021/jm100157m
162651571 179620 0 None 2 4 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
CHEMBL4749564 179620 0 None 2 4 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
10760345 17838 0 None - 1 Human 6.9 pEC50 = 6.9 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 350 6 1 2 4.3 CCN(CC)C(=O)c1ccc(C(c2ccccc2)C2CCNCC2)cc1 10.1021/jm000229p
CHEMBL126382 17838 0 None - 1 Human 6.9 pEC50 = 6.9 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 350 6 1 2 4.3 CCN(CC)C(=O)c1ccc(C(c2ccccc2)C2CCNCC2)cc1 10.1021/jm000229p
49863734 15160 0 None -64 5 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 1477 21 11 14 6.8 CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC(C)(C)[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)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 10.1021/jm100157m
CHEMBL1214027 15160 0 None -64 5 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 1477 21 11 14 6.8 CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(C)(C)SSC(C)(C)[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)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 10.1021/jm100157m
45485986 195854 0 None - 1 Human 6.9 pEC50 = 6.9 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 475 10 1 5 4.7 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3ncc[nH]3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL570181 195854 0 None - 1 Human 6.9 pEC50 = 6.9 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 475 10 1 5 4.7 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3ncc[nH]3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL3580743 210023 0 None -301 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells co-expressing Galphaq66Di5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assayAgonist activity at human recombinant delta opioid receptor expressed in CHO cells co-expressing Galphaq66Di5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay
ChEMBL None None None NC(=O)[C@@H]1CC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(F)cc2F)C(=O)N1 10.1021/acsmedchemlett.5b00056
122633395 176735 0 None - 1 Human 6.9 pEC50 = 6.9 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 492 3 3 4 4.3 O=C(CCc1ccccc1)N1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2020.127176
CHEMBL4636799 176735 0 None - 1 Human 6.9 pEC50 = 6.9 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 492 3 3 4 4.3 O=C(CCc1ccccc1)N1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2020.127176
11213149 122584 0 None - 1 Human 6.9 pEC50 = 6.9 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 122584 0 None - 1 Human 6.9 pEC50 = 6.9 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
86711653 160041 0 None -15 3 Human 6.9 pEC50 = 6.9 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 542 8 0 5 5.0 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CN(Cc1ccccc1)C(C)=O)C2 nan
CHEMBL4112771 160041 0 None -15 3 Human 6.9 pEC50 = 6.9 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 542 8 0 5 5.0 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CN(Cc1ccccc1)C(C)=O)C2 nan
CHEMBL379405 210518 0 None -2 5 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](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
CHEMBL383458 210566 0 None 1 5 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](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](C)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
89978581 159453 0 None -3 3 Human 6.9 pEC50 = 6.9 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 524 9 1 7 3.8 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COC(=O)[C@@H](N)CC(C)C)C2 nan
CHEMBL4107821 159453 0 None -3 3 Human 6.9 pEC50 = 6.9 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 524 9 1 7 3.8 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COC(=O)[C@@H](N)CC(C)C)C2 nan
155539727 175868 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human DOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay
ChEMBL 439 9 3 5 3.6 CCOc1ccc(CN2CCCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4482942 175868 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human DOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay
ChEMBL 439 9 3 5 3.6 CCOc1ccc(CN2CCCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4596318 175868 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human DOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay
ChEMBL 439 9 3 5 3.6 CCOc1ccc(CN2CCCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
16100406 82811 0 None 1 5 Human 7.9 pEC50 = 7.9 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 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)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
CHEMBL218600 82811 0 None 1 5 Human