Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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name		 GPCRdb
ID		 Reference
ligand		 Vendors

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 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
54669894 80798 None 0 Human Functional pEC50 = 10.8 10.8 60 3
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 80798 None 0 Human Functional pEC50 = 10.8 10.8 60 3
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 205041 None 0 Human Functional pEC50 = 10.8 10.8 1 5
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 205041 None 0 Human Functional pEC50 = 10.8 10.8 1 5
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 198402 None 0 Human Functional pEC50 = 10.7 10.7 - 1
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 198402 None 0 Human Functional pEC50 = 10.7 10.7 - 1
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 198402 None 0 Human Functional pEC50 = 10.7 10.7 - 1
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 198402 None 0 Human Functional pEC50 = 10.7 10.7 - 1
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 1306 None 30 Human Functional pEC50 = 10.7 10.7 -22 6
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 1306 None 30 Human Functional pEC50 = 10.7 10.7 -22 6
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 1306 None 30 Human Functional pEC50 = 10.7 10.7 -22 6
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 1306 None 30 Human Functional pEC50 = 10.7 10.7 -22 6
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 205041 None 0 Human Functional pEC50 = 10.7 10.7 1 5
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 205041 None 0 Human Functional pEC50 = 10.7 10.7 1 5
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 197889 None 0 Human Functional pEC50 = 10.3 10.3 - 1
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 197889 None 0 Human Functional pEC50 = 10.3 10.3 - 1
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 197889 None 0 Human Functional pEC50 = 10.3 10.3 - 1
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 197889 None 0 Human Functional pEC50 = 10.3 10.3 - 1
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 199127 None 0 Human Functional pEC50 = 10.2 10.2 - 1
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 199127 None 0 Human Functional pEC50 = 10.2 10.2 - 1
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 199127 None 0 Human Functional pEC50 = 10.2 10.2 - 1
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 199127 None 0 Human Functional pEC50 = 10.2 10.2 - 1
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 57232 None 0 Human Functional pEC50 = 10.2 10.2 1 3
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 57232 None 0 Human Functional pEC50 = 10.2 10.2 1 3
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 57232 None 0 Human Functional pEC50 = 10.2 10.2 1 3
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 57232 None 0 Human Functional pEC50 = 10.2 10.2 1 3
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 57233 None 0 Human Functional pEC50 = 10.2 10.2 -1 3
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 57233 None 0 Human Functional pEC50 = 10.2 10.2 -1 3
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 57233 None 0 Human Functional pEC50 = 10.2 10.2 -1 3
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 57233 None 0 Human Functional pEC50 = 10.2 10.2 -1 3
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 2297 None 29 Human Functional pEC50 = 10.1 10.1 -1 7
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 2297 None 29 Human Functional pEC50 = 10.1 10.1 -1 7
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 2297 None 29 Human Functional pEC50 = 10.1 10.1 -1 7
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 2297 None 29 Human Functional pEC50 = 10.1 10.1 -1 7
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 2297 None 29 Human Functional pEC50 = 10.1 10.1 -1 7
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 137728 None 0 Human Functional pEC50 = 10.1 10.1 -4 2
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 137728 None 0 Human Functional pEC50 = 10.1 10.1 -4 2
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 57238 None 0 Human Functional pEC50 = 10.1 10.1 -6 3
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 57238 None 0 Human Functional pEC50 = 10.1 10.1 -6 3
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 57238 None 0 Human Functional pEC50 = 10.1 10.1 -6 3
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 57238 None 0 Human Functional pEC50 = 10.1 10.1 -6 3
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 57229 None 0 Human Functional pEC50 = 10 10.0 1 3
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 57229 None 0 Human Functional pEC50 = 10 10.0 1 3
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 61280 None 0 Human Functional pEC50 = 10 10.0 -4 5
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 61280 None 0 Human Functional pEC50 = 10 10.0 -4 5
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1219 27 10 10 6.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL26575 213121 None 0 Rat Functional pEC50 = 10 10.0 5 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)NCC(=O)O)C(C)C 10.1016/j.bmcl.2018.05.015
71456262 79488 None 0 Human Functional pEC50 = 10 10.0 -2 3
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 79488 None 0 Human Functional pEC50 = 10 10.0 -2 3
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 2728 None 8 Human Functional pEC50 = 10.0 10.0 2 7
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 2728 None 8 Human Functional pEC50 = 10.0 10.0 2 7
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 2728 None 8 Human Functional pEC50 = 10.0 10.0 2 7
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 2728 None 8 Human Functional pEC50 = 10.0 10.0 2 7
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 57237 None 0 Human Functional pEC50 = 9.9 9.9 1 3
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 57237 None 0 Human Functional pEC50 = 9.9 9.9 1 3
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 57237 None 0 Human Functional pEC50 = 9.9 9.9 1 3
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 57237 None 0 Human Functional pEC50 = 9.9 9.9 1 3
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 61280 None 0 Human Functional pEC50 = 9.9 9.9 -4 5
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 61280 None 0 Human Functional pEC50 = 9.9 9.9 -4 5
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 8480 None 0 Mouse Functional pEC50 = 9.9 9.9 - 1
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 8480 None 0 Mouse Functional pEC50 = 9.9 9.9 - 1
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 14125 None 0 Human Functional pEC50 = 9.9 9.9 16 4
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 14125 None 0 Human Functional pEC50 = 9.9 9.9 16 4
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 14125 None 0 Human Functional pEC50 = 9.9 9.9 16 4
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 213353 None 0 Human Functional pEC50 = 9.9 9.9 -2 7
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 84206 None 0 Human Functional pEC50 = 9.8 9.8 -1 3
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 84206 None 0 Human Functional pEC50 = 9.8 9.8 -1 3
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 57234 None 0 Human Functional pEC50 = 9.8 9.8 1 3
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 57234 None 0 Human Functional pEC50 = 9.8 9.8 1 3
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 85394 None 0 Human Functional pEC50 = 9.8 9.8 74 3
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 85394 None 0 Human Functional pEC50 = 9.8 9.8 74 3
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 57234 None 0 Human Functional pEC50 = 9.8 9.8 1 3
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 57234 None 0 Human Functional pEC50 = 9.8 9.8 1 3
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 65678 None 0 Human Functional pEC50 = 9.8 9.8 -2 3
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 65678 None 0 Human Functional pEC50 = 9.8 9.8 -2 3
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 85410 None 0 Human Functional pEC50 = 9.8 9.8 2 3
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 85410 None 0 Human Functional pEC50 = 9.8 9.8 2 3
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 85410 None 0 Human Functional pEC50 = 9.8 9.8 2 3
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 192016 None 0 Human Functional pEC50 = 9.8 9.8 9 3
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 192016 None 0 Human Functional pEC50 = 9.8 9.8 9 3
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 69356 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 69356 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 14182 None 0 Human Functional pEC50 = 9.7 9.7 -36 4
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 14182 None 0 Human Functional pEC50 = 9.7 9.7 -36 4
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 14182 None 0 Human Functional pEC50 = 9.7 9.7 -36 4
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 57239 None 0 Human Functional pEC50 = 9.7 9.7 -2 3
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 57239 None 0 Human Functional pEC50 = 9.7 9.7 -2 3
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 61282 None 0 Human Functional pEC50 = 9.7 9.7 1 5
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 61282 None 0 Human Functional pEC50 = 9.7 9.7 1 5
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 206095 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 206095 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 57239 None 0 Human Functional pEC50 = 9.7 9.7 -2 3
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 57239 None 0 Human Functional pEC50 = 9.7 9.7 -2 3
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 199775 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 199775 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 201407 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 201407 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 212862 None 0 Human Functional pEC50 = 9.7 9.7 6 3
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 159684 None 0 Human Functional pEC50 = 9.6 9.6 6 3
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 159684 None 0 Human Functional pEC50 = 9.6 9.6 6 3
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 199842 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 199842 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 212898 None 0 Human Functional pEC50 = 9.6 9.6 19 3
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 3673 None 0 Human Functional pEC50 = 9.6 9.6 1 2
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 3673 None 0 Human Functional pEC50 = 9.6 9.6 1 2
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 3673 None 0 Human Functional pEC50 = 9.6 9.6 1 2
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 99345 None 0 Human Functional pEC50 = 9.5 9.5 -7 3
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 99345 None 0 Human Functional pEC50 = 9.5 9.5 -7 3
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 14184 None 0 Human Functional pEC50 = 9.5 9.5 1 4
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 14184 None 0 Human Functional pEC50 = 9.5 9.5 1 4
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 14184 None 0 Human Functional pEC50 = 9.5 9.5 1 4
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 84204 None 0 Human Functional pEC50 = 9.5 9.5 -1 3
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 84204 None 0 Human Functional pEC50 = 9.5 9.5 -1 3
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 157965 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 157965 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 79212 None 0 Human Functional pEC50 = 9.5 9.5 549 2
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 79212 None 0 Human Functional pEC50 = 9.5 9.5 549 2
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 1308 None 0 Mouse Functional pEC50 = 9.5 9.5 4 3
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 1308 None 0 Mouse Functional pEC50 = 9.5 9.5 4 3
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 212863 None 0 Human Functional pEC50 = 9.5 9.5 -1 3
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 183434 None 0 Human Functional pEC50 = 9.5 9.5 32 5
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 183434 None 0 Human Functional pEC50 = 9.5 9.5 32 5
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 156681 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 156681 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 123069 None 0 Human Functional pEC50 = 9.4 9.4 15 3
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 123069 None 0 Human Functional pEC50 = 9.4 9.4 15 3
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 753 None 27 Human Functional pEC50 = 9.4 9.4 1 6
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 753 None 27 Human Functional pEC50 = 9.4 9.4 1 6
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 753 None 27 Human Functional pEC50 = 9.4 9.4 1 6
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 204307 None 0 Human Functional pEC50 = 9.4 9.4 -10 3
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 204307 None 0 Human Functional pEC50 = 9.4 9.4 -10 3
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 111272 None 0 Human Functional pEC50 = 9.4 9.4 6 3
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 111272 None 0 Human Functional pEC50 = 9.4 9.4 6 3
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 156050 None 0 Human Functional pEC50 = 9.4 9.4 10 2
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 156050 None 0 Human Functional pEC50 = 9.4 9.4 10 2
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 157257 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 157257 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 157319 None 0 Human Functional pEC50 = 9.4 9.4 13 3
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 157319 None 0 Human Functional pEC50 = 9.4 9.4 13 3
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 158942 None 0 Human Functional pEC50 = 9.4 9.4 -2 2
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 158942 None 0 Human Functional pEC50 = 9.4 9.4 -2 2
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 61282 None 0 Human Functional pEC50 = 9.4 9.4 1 5
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 61282 None 0 Human Functional pEC50 = 9.4 9.4 1 5
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 85359 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 85359 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 91661 None 0 Human Functional pEC50 = 9.3 9.3 12 3
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 91661 None 0 Human Functional pEC50 = 9.3 9.3 12 3
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 205527 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 205527 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 158372 None 0 Human Functional pEC50 = 9.3 9.3 2 3
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 158372 None 0 Human Functional pEC50 = 9.3 9.3 2 3
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 18258 None 9 Human Functional pEC50 = 9.3 9.3 446 3
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 18258 None 9 Human Functional pEC50 = 9.3 9.3 446 3
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 18258 None 9 Human Functional pEC50 = 9.3 9.3 446 3
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 158372 None 0 Human Functional pEC50 = 9.3 9.3 2 3
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 158372 None 0 Human Functional pEC50 = 9.3 9.3 2 3
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 156511 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 156511 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 213353 None 0 Human Functional pEC50 = 9.3 9.3 -2 7
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 199912 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 199912 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 61283 None 0 Human Functional pEC50 = 9.2 9.2 1 5
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 61283 None 0 Human Functional pEC50 = 9.2 9.2 1 5
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 82743 None 0 Human Functional pEC50 = 9.2 9.2 7 2
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 82743 None 0 Human Functional pEC50 = 9.2 9.2 7 2
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 61283 None 0 Human Functional pEC50 = 9.2 9.2 1 5
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 61283 None 0 Human Functional pEC50 = 9.2 9.2 1 5
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 159077 None 0 Human Functional pEC50 = 9.2 9.2 8 3
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 159077 None 0 Human Functional pEC50 = 9.2 9.2 8 3
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 111018 None 0 Human Functional pEC50 = 9.2 9.2 -1 3
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 111018 None 0 Human Functional pEC50 = 9.2 9.2 -1 3
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 159514 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 159514 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 94283 None 0 Human Functional pEC50 = 9.2 9.2 1 3
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 94283 None 0 Human Functional pEC50 = 9.2 9.2 1 3
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 60134 None 0 Human Functional pEC50 = 9.2 9.2 1 3
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 60134 None 0 Human Functional pEC50 = 9.2 9.2 1 3
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 60134 None 0 Human Functional pEC50 = 9.2 9.2 1 3
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 3750 None 6 Human Functional pEC50 = 9.2 9.2 3 3
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 3750 None 6 Human Functional pEC50 = 9.2 9.2 3 3
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 3750 None 6 Human Functional pEC50 = 9.2 9.2 3 3
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 3750 None 6 Human Functional pEC50 = 9.2 9.2 3 3
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 3750 None 6 Human Functional pEC50 = 9.2 9.2 3 3
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 3750 None 6 Human Functional pEC50 = 9.2 9.2 3 3
Agonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assayAgonist activity at human recombinant delta opioid receptor expressed in human HEK293 cells by [35S]GTPgammaS binding assay
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 10.1016/j.bmc.2011.11.047
155538529 176633 None 0 Rat Functional pEC50 = 9.2 9.2 -2 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 548 7 3 5 5.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4476818 176633 None 0 Rat Functional pEC50 = 9.2 9.2 -2 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 548 7 3 5 5.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597054 176633 None 0 Rat Functional pEC50 = 9.2 9.2 -2 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 548 7 3 5 5.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
24768397 146506 None 0 Human Functional pEC50 = 9.1 9.1 -7 3
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 146506 None 0 Human Functional pEC50 = 9.1 9.1 -7 3
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 88542 None 0 Human Functional pEC50 = 9.1 9.1 1 3
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 88542 None 0 Human Functional pEC50 = 9.1 9.1 1 3
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 146506 None 0 Human Functional pEC50 = 9.1 9.1 -7 3
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 146506 None 0 Human Functional pEC50 = 9.1 9.1 -7 3
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 88542 None 0 Human Functional pEC50 = 9.1 9.1 1 3
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 88542 None 0 Human Functional pEC50 = 9.1 9.1 1 3
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 106361 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 106361 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 106361 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 182927 None 0 Human Functional pEC50 = 9.1 9.1 22 5
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 182927 None 0 Human Functional pEC50 = 9.1 9.1 22 5
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 84208 None 0 Human Functional pEC50 = 9.1 9.1 -2 3
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 84208 None 0 Human Functional pEC50 = 9.1 9.1 -2 3
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 137674 None 0 Human Functional pEC50 = 9.1 9.1 158 3
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 137674 None 0 Human Functional pEC50 = 9.1 9.1 158 3
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 139249 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 139249 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 160995 None 0 Human Functional pEC50 = 9.1 9.1 2 2
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 160995 None 0 Human Functional pEC50 = 9.1 9.1 2 2
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 137300 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
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 137300 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
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 171235 None 0 Mouse Functional pEC50 = 9.1 9.1 1 6
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 171235 None 0 Mouse Functional pEC50 = 9.1 9.1 1 6
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 137866 None 0 Human Functional pEC50 = 9.1 9.1 51 2
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 137866 None 0 Human Functional pEC50 = 9.1 9.1 51 2
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 79207 None 0 Human Functional pEC50 = 9.1 9.1 30 3
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 79207 None 0 Human Functional pEC50 = 9.1 9.1 30 3
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 85824 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
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 85824 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
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 214753 None 0 Human Functional pEC50 = 9.1 9.1 8 5
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 214753 None 0 Human Functional pEC50 = 9.1 9.1 8 5
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 77377 None 0 Mouse Functional pEC50 = 9.1 9.1 -1 3
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 77377 None 0 Mouse Functional pEC50 = 9.1 9.1 -1 3
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 77377 None 0 Human Functional pEC50 = 9.1 9.1 1 3
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 77377 None 0 Human Functional pEC50 = 9.1 9.1 1 3
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 19286 None 0 Human Functional pEC50 = 9.1 9.1 776 3
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 19286 None 0 Human Functional pEC50 = 9.1 9.1 776 3
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 79211 None 0 Human Functional pEC50 = 9.0 9.0 5 3
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 79211 None 0 Human Functional pEC50 = 9.0 9.0 5 3
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 61284 None 0 Human Functional pEC50 = 9.0 9.0 -39 5
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 61284 None 0 Human Functional pEC50 = 9.0 9.0 -39 5
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 111271 None 0 Human Functional pEC50 = 9.0 9.0 4 3
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 111271 None 0 Human Functional pEC50 = 9.0 9.0 4 3
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 2297 None 29 Human Functional pEC50 = 9 9.0 -1 7
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 2297 None 29 Human Functional pEC50 = 9 9.0 -1 7
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 2297 None 29 Human Functional pEC50 = 9 9.0 -1 7
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 2297 None 29 Human Functional pEC50 = 9 9.0 -1 7
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 2297 None 29 Human Functional pEC50 = 9 9.0 -1 7
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 72864 None 12 Human Functional pEC50 = 9 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9 9.0 -1 4
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 61284 None 0 Human Functional pEC50 = 9 9.0 -39 5
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 61284 None 0 Human Functional pEC50 = 9 9.0 -39 5
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 2495 None 37 Human Functional pEC50 = 9.0 9.0 -6 5
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 2495 None 37 Human Functional pEC50 = 9.0 9.0 -6 5
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 2495 None 37 Human Functional pEC50 = 9.0 9.0 -6 5
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 2495 None 37 Human Functional pEC50 = 9.0 9.0 -6 5
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 2495 None 37 Human Functional pEC50 = 9.0 9.0 -6 5
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 2495 None 37 Human Functional pEC50 = 9.0 9.0 -6 5
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 2495 None 37 Human Functional pEC50 = 9.0 9.0 -6 5
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 2495 None 37 Human Functional pEC50 = 9.0 9.0 -6 5
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 18286 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 18286 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 18286 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 139224 None 0 Human Functional pEC50 = 9.0 9.0 2 3
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 139224 None 0 Human Functional pEC50 = 9.0 9.0 2 3
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 60135 None 0 Human Functional pEC50 = 9.0 9.0 3 3
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 60135 None 0 Human Functional pEC50 = 9.0 9.0 3 3
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 60135 None 0 Human Functional pEC50 = 9.0 9.0 3 3
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 106369 None 0 Human Functional pEC50 = 9.0 9.0 97 2
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 106369 None 0 Human Functional pEC50 = 9.0 9.0 97 2
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 106369 None 0 Human Functional pEC50 = 9.0 9.0 97 2
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 212902 None 0 Human Functional pEC50 = 9.0 9.0 -1 3
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 111266 None 0 Human Functional pEC50 = 9.0 9.0 1 3
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 111266 None 0 Human Functional pEC50 = 9.0 9.0 1 3
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 212866 None 0 Human Functional pEC50 = 9.0 9.0 1 3
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 104459 None 0 Human Functional pEC50 = 9.0 9.0 -10 3
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 104459 None 0 Human Functional pEC50 = 9.0 9.0 -10 3
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 72864 None 12 Human Functional pEC50 = 9.0 9.0 -1 4
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 200788 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 200788 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 489 9 1 4 5.9 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccc3F)CC2)cc1 10.1016/j.bmcl.2009.09.072
145961376 161704 None 0 Rat Functional pEC50 = 9.0 9.0 -11 3
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 569 15 9 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
CHEMBL4129679 161704 None 0 Rat Functional pEC50 = 9.0 9.0 -11 3
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 569 15 9 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
45486101 199904 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 199904 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 199946 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 199946 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 84214 None 0 Human Functional pEC50 = 8.9 8.9 1 3
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 84214 None 0 Human Functional pEC50 = 8.9 8.9 1 3
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 157789 None 0 Human Functional pEC50 = 8.9 8.9 2 2
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 157789 None 0 Human Functional pEC50 = 8.9 8.9 2 2
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 79208 None 0 Human Functional pEC50 = 8.9 8.9 79 3
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 79208 None 0 Human Functional pEC50 = 8.9 8.9 79 3
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 106400 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 106400 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 106400 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 118240 None 0 Human Functional pEC50 = 8.9 8.9 -5 3
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 118240 None 0 Human Functional pEC50 = 8.9 8.9 -5 3
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 199958 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 199958 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 157357 None 0 Human Functional pEC50 = 8.9 8.9 1 2
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 157357 None 0 Human Functional pEC50 = 8.9 8.9 1 2
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 161404 None 0 Human Functional pEC50 = 8.9 8.9 6 5
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 161404 None 0 Human Functional pEC50 = 8.9 8.9 6 5
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 213353 None 0 Human Functional pEC50 = 8.9 8.9 -2 7
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 161404 None 0 Human Functional pEC50 = 8.9 8.9 6 5
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 161404 None 0 Human Functional pEC50 = 8.9 8.9 6 5
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 106389 None 0 Human Functional pEC50 = 8.9 8.9 11 3
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 106389 None 0 Human Functional pEC50 = 8.9 8.9 11 3
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 106389 None 0 Human Functional pEC50 = 8.9 8.9 11 3
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 97916 None 0 Human Functional pEC50 = 8.9 8.9 -14 4
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 97916 None 0 Human Functional pEC50 = 8.9 8.9 -14 4
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 97916 None 0 Human Functional pEC50 = 8.9 8.9 -14 4
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 139113 None 0 Human Functional pEC50 = 8.9 8.9 2 2
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 139113 None 0 Human Functional pEC50 = 8.9 8.9 2 2
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 157355 None 0 Human Functional pEC50 = 8.9 8.9 15 2
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 157355 None 0 Human Functional pEC50 = 8.9 8.9 15 2
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 187648 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 187648 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 3750 None 6 Human Functional pEC50 = 8.9 8.9 3 3
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 3750 None 6 Human Functional pEC50 = 8.9 8.9 3 3
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 3750 None 6 Human Functional pEC50 = 8.9 8.9 3 3
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 171235 None 0 Human Functional pEC50 = 8.9 8.9 -1 6
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 171235 None 0 Human Functional pEC50 = 8.9 8.9 -1 6
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 171235 None 0 Human Functional pEC50 = 8.9 8.9 -1 6
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 171235 None 0 Human Functional pEC50 = 8.9 8.9 -1 6
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 123167 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 123167 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 79204 None 0 Human Functional pEC50 = 8.9 8.9 3 2
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 79204 None 0 Human Functional pEC50 = 8.9 8.9 3 2
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 106425 None 0 Human Functional pEC50 = 8.9 8.9 81 2
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 106425 None 0 Human Functional pEC50 = 8.9 8.9 81 2
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 106425 None 0 Human Functional pEC50 = 8.9 8.9 81 2
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 199772 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 199772 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 477 9 1 5 5.8 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3cccs3)CC2)cc1 10.1016/j.bmcl.2009.09.072
104787 1473 None 17 Rat Functional pEC50 = 8.9 8.9 -14 4
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL None None None None 10.1016/j.ejmech.2020.112070
1608 1473 None 17 Rat Functional pEC50 = 8.9 8.9 -14 4
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL None None None None 10.1016/j.ejmech.2020.112070
CHEMBL31421 1473 None 17 Rat Functional pEC50 = 8.9 8.9 -14 4
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL None None None None 10.1016/j.ejmech.2020.112070
DB08861 1473 None 17 Rat Functional pEC50 = 8.9 8.9 -14 4
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL None None None None 10.1016/j.ejmech.2020.112070
145961844 161748 None 0 Human Functional pEC50 = 8.8 8.8 2 3
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 161748 None 0 Human Functional pEC50 = 8.8 8.8 2 3
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 161748 None 0 Human Functional pEC50 = 8.8 8.8 2 3
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 161748 None 0 Human Functional pEC50 = 8.8 8.8 2 3
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 85358 None 0 Human Functional pEC50 = 8.8 8.8 15 3
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 85358 None 0 Human Functional pEC50 = 8.8 8.8 15 3
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 157351 None 0 Human Functional pEC50 = 8.8 8.8 -5 2
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 157351 None 0 Human Functional pEC50 = 8.8 8.8 -5 2
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1021/jm800389v
155522549 176342 None 0 Rat Functional pEC50 = 8.8 8.8 1 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 511 6 3 5 4.8 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL4453526 176342 None 0 Rat Functional pEC50 = 8.8 8.8 1 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 511 6 3 5 4.8 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL4594713 176342 None 0 Rat Functional pEC50 = 8.8 8.8 1 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 511 6 3 5 4.8 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL294616 213353 None 0 Human Functional pEC50 = 8.8 8.8 -2 7
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 106394 None 0 Human Functional pEC50 = 8.8 8.8 10 2
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 106394 None 0 Human Functional pEC50 = 8.8 8.8 10 2
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 106394 None 0 Human Functional pEC50 = 8.8 8.8 10 2
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 212859 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 114845 None 0 Human Functional pEC50 = 8.8 8.8 -51 3
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 114845 None 0 Human Functional pEC50 = 8.8 8.8 -51 3
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 159299 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 159299 None 0 Human Functional pEC50 = 8.8 8.8 3 3
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 201281 None 4 Human Functional pEC50 = 8.8 8.8 1 6
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 201281 None 4 Human Functional pEC50 = 8.8 8.8 1 6
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 201281 None 4 Human Functional pEC50 = 8.8 8.8 1 6
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 201281 None 4 Human Functional pEC50 = 8.8 8.8 1 6
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 111019 None 0 Human Functional pEC50 = 8.8 8.8 1 3
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 111019 None 0 Human Functional pEC50 = 8.8 8.8 1 3
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 69355 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 69355 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 3465 None 16 Human Functional pEC50 = 8.7 8.7 -4 3
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 3465 None 16 Human Functional pEC50 = 8.7 8.7 -4 3
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
11667832.0 3465 None 16 Human Functional pEC50 = 8.7 8.7 -4 3
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 3465 None 16 Human Functional pEC50 = 8.7 8.7 -4 3
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 3465 None 16 Human Functional pEC50 = 8.7 8.7 -4 3
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 211917 None 0 Human Functional pEC50 = 8.7 8.7 -4 4
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 206204 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 206204 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 213856 None 0 Mouse Functional pEC50 = 8.7 8.7 2 3
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 211249 None 0 Mouse Functional pEC50 = 8.7 8.7 2 3
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 139134 None 0 Human Functional pEC50 = 8.7 8.7 10 3
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 139134 None 0 Human Functional pEC50 = 8.7 8.7 10 3
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 211917 None 0 Human Functional pEC50 = 8.7 8.7 -4 4
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 3633 None 34 Human Functional pEC50 = 8.7 8.7 1 9
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 3633 None 34 Human Functional pEC50 = 8.7 8.7 1 9
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 3633 None 34 Human Functional pEC50 = 8.7 8.7 1 9
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]-GTP[gammaS] binding
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
134338859 176504 None 0 Rat Functional pEC50 = 8.7 8.7 -4 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 4 5.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4446945 176504 None 0 Rat Functional pEC50 = 8.7 8.7 -4 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 4 5.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4595985 176504 None 0 Rat Functional pEC50 = 8.7 8.7 -4 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 4 5.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
11375776 158205 None 1 Human Functional pEC50 = 8.7 8.7 - 1
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 158205 None 1 Human Functional pEC50 = 8.7 8.7 - 1
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 106372 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 106372 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 106372 None 0 Human Functional pEC50 = 8.7 8.7 -1 2
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 211270 None 0 Human Functional pEC50 = 8.7 8.7 -57 8
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 106379 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 106379 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 106379 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 93745 None 0 Human Functional pEC50 = 8 8.0 26 2
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 93745 None 0 Human Functional pEC50 = 8 8.0 26 2
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 198785 None 0 Human Functional pEC50 = 8 8.0 3 3
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 198785 None 0 Human Functional pEC50 = 8 8.0 3 3
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 3633 None 34 Human Functional pEC50 = 8 8.0 1 9
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 3633 None 34 Human Functional pEC50 = 8 8.0 1 9
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 3633 None 34 Human Functional pEC50 = 8 8.0 1 9
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 1473 None 17 Mouse Functional pEC50 = 8 8.0 -22 4
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 1473 None 17 Mouse Functional pEC50 = 8 8.0 -22 4
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 1473 None 17 Mouse Functional pEC50 = 8 8.0 -22 4
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 1473 None 17 Mouse Functional pEC50 = 8 8.0 -22 4
Agonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysisAgonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
ChEMBL None None None None 10.1021/acs.jmedchem.6b00748
127049272 141059 None 0 Rat Functional pEC50 = 8 8.0 -5 3
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 497 7 3 4 4.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
CHEMBL3823231 141059 None 0 Rat Functional pEC50 = 8 8.0 -5 3
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 497 7 3 4 4.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
1613 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 111024 None 0 Human Functional pEC50 = 8.0 8.0 3 3
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 111024 None 0 Human Functional pEC50 = 8.0 8.0 3 3
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 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 2297 None 29 Human Functional pEC50 = 8.0 8.0 -1 7
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 84740 None 0 Human Functional pEC50 = 8.0 8.0 9 3
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 84740 None 0 Human Functional pEC50 = 8.0 8.0 9 3
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 106464 None 0 Human Functional pEC50 = 8.0 8.0 -3 3
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 106464 None 0 Human Functional pEC50 = 8.0 8.0 -3 3
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 106464 None 0 Human Functional pEC50 = 8.0 8.0 -3 3
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 178319 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 178319 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 112924 None 0 Human Functional pEC50 = 8.0 8.0 8 2
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 112924 None 0 Human Functional pEC50 = 8.0 8.0 8 2
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 19403 None 0 Human Functional pEC50 = 8.0 8.0 1096 2
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 19403 None 0 Human Functional pEC50 = 8.0 8.0 1096 2
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 59930 None 3 Human Functional pEC50 = 8.0 8.0 - 1
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 59930 None 3 Human Functional pEC50 = 8.0 8.0 - 1
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 197608 None 0 Human Functional pEC50 = 7 7.0 - 1
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 197608 None 0 Human Functional pEC50 = 7 7.0 - 1
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 197773 None 0 Human Functional pEC50 = 7 7.0 - 1
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 197773 None 0 Human Functional pEC50 = 7 7.0 - 1
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 78611 None 0 Human Functional pEC50 = 5 5.0 - 1
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 78611 None 0 Human Functional pEC50 = 5 5.0 - 1
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 92086 None 0 Human Functional pEC50 = 4 4.0 -15 3
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 92086 None 0 Human Functional pEC50 = 4 4.0 -15 3
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 117232 None 0 Human Functional pEC50 = 4 4.0 -1445 3
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 117232 None 0 Human Functional pEC50 = 4 4.0 -1445 3
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 117237 None 0 Human Functional pEC50 = 4 4.0 -812 3
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 117237 None 0 Human Functional pEC50 = 4 4.0 -812 3
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 180824 None 0 Human Functional pEC50 = 6.0 6.0 -2 2
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 180824 None 0 Human Functional pEC50 = 6.0 6.0 -2 2
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 81364 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 81364 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 420 7 3 4 4.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(C(C)C)[C@@H](C)c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
9888152 204469 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Compound was evaluated in 3 determinations for the agonistic activity in the Opioid receptor delta 1 of mouse vas deferensCompound was evaluated in 3 determinations for the agonistic activity in the Opioid receptor delta 1 of mouse vas deferens
ChEMBL 416 2 2 4 4.0 CCO[C@@]12Cc3c([nH]c4ccccc34)[C@]3(C)Oc4c(O)ccc5c4[C@]13CCN(C)[C@@H]2C5 10.1016/S0960-894X(96)00599-9
CHEMBL608246 204469 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Compound was evaluated in 3 determinations for the agonistic activity in the Opioid receptor delta 1 of mouse vas deferensCompound was evaluated in 3 determinations for the agonistic activity in the Opioid receptor delta 1 of mouse vas deferens
ChEMBL 416 2 2 4 4.0 CCO[C@@]12Cc3c([nH]c4ccccc34)[C@]3(C)Oc4c(O)ccc5c4[C@]13CCN(C)[C@@H]2C5 10.1016/S0960-894X(96)00599-9
CHEMBL407057 215095 None 1 Human Functional pEC50 = 7.0 7.0 -3 5
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 29930 None 0 Human Functional pEC50 = 6.0 6.0 4 2
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 29930 None 0 Human Functional pEC50 = 6.0 6.0 4 2
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 187534 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 187534 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 117793 None 0 Mouse Functional pEC50 = 7.0 7.0 -3 4
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 117793 None 0 Mouse Functional pEC50 = 7.0 7.0 -3 4
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 78612 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 78612 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1Effective concentration against stimulation of [35S]GTP-gamma-S, binding in CHO cells transfected with the human opioid receptor delta 1
ChEMBL 504 9 0 2 7.4 C=C(C)CN(CC)C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
16756840 142447 None 0 Rat Functional pEC50 = 6.0 6.0 -50 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 337 4 2 3 3.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1 10.1016/j.bmc.2017.02.064
CHEMBL388873 142447 None 0 Rat Functional pEC50 = 6.0 6.0 -50 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 337 4 2 3 3.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1 10.1016/j.bmc.2017.02.064
10033203 211590 None 34 Human Functional pEC50 = 8.0 8.0 -25 3
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 211590 None 34 Human Functional pEC50 = 8.0 8.0 -25 3
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 82742 None 0 Human Functional pEC50 = 8.0 8.0 19 3
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 82742 None 0 Human Functional pEC50 = 8.0 8.0 19 3
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 111267 None 0 Human Functional pEC50 = 8.0 8.0 9 3
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 111267 None 0 Human Functional pEC50 = 8.0 8.0 9 3
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 161508 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 161508 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 112922 None 0 Human Functional pEC50 = 7.9 7.9 13 2
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 112922 None 0 Human Functional pEC50 = 7.9 7.9 13 2
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 215095 None 1 Human Functional pEC50 = 7.0 7.0 -3 5
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 84748 None 0 Human Functional pEC50 = 7.0 7.0 -7 2
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 84748 None 0 Human Functional pEC50 = 7.0 7.0 -7 2
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 197580 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 197580 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 197755 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 197755 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 146536 None 0 Human Functional pEC50 = 7.0 7.0 -10 3
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 146536 None 0 Human Functional pEC50 = 7.0 7.0 -10 3
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 832 19 7 9 2.3 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
10320450 86885 None 0 Rat Functional pEC50 = 7.0 7.0 -69 3
Agonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/jm400050y
CHEMBL2322568 86885 None 0 Rat Functional pEC50 = 7.0 7.0 -69 3
Agonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/jm400050y
CHEMBL4444479 86885 None 0 Rat Functional pEC50 = 7.0 7.0 -69 3
Agonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/jm400050y
10320450 86885 None 0 Rat Functional pEC50 = 7.0 7.0 -69 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL2322568 86885 None 0 Rat Functional pEC50 = 7.0 7.0 -69 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4444479 86885 None 0 Rat Functional pEC50 = 7.0 7.0 -69 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
10320450 86885 None 0 Rat Functional pEC50 = 7.0 7.0 -69 3
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.5b01270
CHEMBL2322568 86885 None 0 Rat Functional pEC50 = 7.0 7.0 -69 3
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.5b01270
CHEMBL4444479 86885 None 0 Rat Functional pEC50 = 7.0 7.0 -69 3
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.5b01270
5748293 109753 None 13 Human Functional pEC50 = 6.0 6.0 -53 3
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 109753 None 13 Human Functional pEC50 = 6.0 6.0 -53 3
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 109753 None 13 Human Functional pEC50 = 6.0 6.0 -53 3
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 50927 None 0 Human Functional pEC50 = 5.0 5.0 1 2
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 50927 None 0 Human Functional pEC50 = 5.0 5.0 1 2
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 192029 None 0 Human Functional pEC50 = 7.0 7.0 -21 3
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 192029 None 0 Human Functional pEC50 = 7.0 7.0 -21 3
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 205528 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 205528 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 146536 None 0 Human Functional pEC50 = 7.0 7.0 -10 3
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 146536 None 0 Human Functional pEC50 = 7.0 7.0 -10 3
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
162667205 183842 None 0 Rat Functional pEC50 = 7.0 7.0 -48 3
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 369 4 3 4 2.7 CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1 10.1016/j.ejmech.2020.112070
CHEMBL4786173 183842 None 0 Rat Functional pEC50 = 7.0 7.0 -48 3
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 369 4 3 4 2.7 CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1 10.1016/j.ejmech.2020.112070
CHEMBL4803577 183842 None 0 Rat Functional pEC50 = 7.0 7.0 -48 3
Agonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 369 4 3 4 2.7 CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1 10.1016/j.ejmech.2020.112070
162658841 181118 None 0 Human Functional pEC50 = 6.9 6.9 -2 5
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 181118 None 0 Human Functional pEC50 = 6.9 6.9 -2 5
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 214762 None 0 Human Functional pEC50 = 6.9 6.9 -15 5
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 181118 None 0 Human Functional pEC50 = 6.9 6.9 -2 5
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 181118 None 0 Human Functional pEC50 = 6.9 6.9 -2 5
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 15337 None 0 Human Functional pEC50 = 6.9 6.9 -239 5
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 15337 None 0 Human Functional pEC50 = 6.9 6.9 -239 5
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 33048 None 6 Human Functional pEC50 = 4.9 4.9 -2 2
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 33048 None 6 Human Functional pEC50 = 4.9 4.9 -2 2
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 117247 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 117247 None 0 Human Functional pEC50 = 5.9 5.9 -2 3
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 216525 None 20 Human Functional pEC50 = 6.9 6.9 7 3
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 43581 None 12 Human Functional pEC50 = 4.9 4.9 -1 2
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 43581 None 12 Human Functional pEC50 = 4.9 4.9 -1 2
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 161508 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 161508 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 72289 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 72289 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 72632 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 72632 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 182492 None 0 Human Functional pEC50 = 6.9 6.9 2 5
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 182492 None 0 Human Functional pEC50 = 6.9 6.9 2 5
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 182492 None 0 Human Functional pEC50 = 6.9 6.9 2 5
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 182492 None 0 Human Functional pEC50 = 6.9 6.9 2 5
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 67511 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 67511 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 180306 None 0 Human Functional pEC50 = 6.9 6.9 2 4
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 180306 None 0 Human Functional pEC50 = 6.9 6.9 2 4
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 59954 None 3 Human Functional pEC50 = 4.9 4.9 - 1
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 59954 None 3 Human Functional pEC50 = 4.9 4.9 - 1
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 84760 None 0 Human Functional pEC50 = 7.9 7.9 10 3
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 84760 None 0 Human Functional pEC50 = 7.9 7.9 10 3
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 187334 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 187334 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 117242 None 0 Human Functional pEC50 = 7.9 7.9 -12 3
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 117242 None 0 Human Functional pEC50 = 7.9 7.9 -12 3
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 123132 None 0 Human Functional pEC50 = 7.9 7.9 -7 3
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 123132 None 0 Human Functional pEC50 = 7.9 7.9 -7 3
Agonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor transfected in HN9.10 cells by [35S]GTPgammaS binding assay
ChEMBL 692 11 5 6 5.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2015.06.030
155542413 176400 None 0 Rat Functional pEC50 = 7.9 7.9 -52 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 507 7 3 5 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4521319 176400 None 0 Rat Functional pEC50 = 7.9 7.9 -52 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 507 7 3 5 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4595172 176400 None 0 Rat Functional pEC50 = 7.9 7.9 -52 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 507 7 3 5 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
9951665 102671 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 102671 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 206156 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 206156 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 117534 None 0 Human Functional pEC50 = 7.9 7.9 1096 2
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 117534 None 0 Human Functional pEC50 = 7.9 7.9 1096 2
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 139219 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
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 139219 None 0 Human Functional pEC50 = 7.9 7.9 -1 2
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 2297 None 29 Human Functional pEC50 = 7.9 7.9 -1 7
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 2297 None 29 Human Functional pEC50 = 7.9 7.9 -1 7
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 2297 None 29 Human Functional pEC50 = 7.9 7.9 -1 7
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 2297 None 29 Human Functional pEC50 = 7.9 7.9 -1 7
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 2297 None 29 Human Functional pEC50 = 7.9 7.9 -1 7
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 213665 None 31 Mouse Functional pEC50 = 7.9 7.9 -1 7
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 214762 None 0 Human Functional pEC50 = 6.9 6.9 -15 5
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 182909 None 0 Human Functional pEC50 = 6.9 6.9 -4 2
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 182909 None 0 Human Functional pEC50 = 6.9 6.9 -4 2
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 155952 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 155952 None 0 Human Functional pEC50 = 6.9 6.9 1 3
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 15337 None 0 Human Functional pEC50 = 6.9 6.9 -239 5
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 15337 None 0 Human Functional pEC50 = 6.9 6.9 -239 5
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 15339 None 0 Human Functional pEC50 = 6.9 6.9 -64 5
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 15339 None 0 Human Functional pEC50 = 6.9 6.9 -64 5
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 180306 None 0 Human Functional pEC50 = 6.9 6.9 2 4
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 180306 None 0 Human Functional pEC50 = 6.9 6.9 2 4
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 18029 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 18029 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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
123797 2791 None 21 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c02093
1479 2791 None 21 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c02093
CHEMBL429731 2791 None 21 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c02093
49863734 15339 None 0 Human Functional pEC50 = 6.9 6.9 -64 5
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 15339 None 0 Human Functional pEC50 = 6.9 6.9 -64 5
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 199987 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 199987 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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
104787 1473 None 17 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c02093
1608 1473 None 17 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c02093
CHEMBL31421 1473 None 17 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c02093
DB08861 1473 None 17 Human Functional pEC50 = 6.9 6.9 -2 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c02093
CHEMBL3580743 214230 None 0 Human Functional pEC50 = 6.9 6.9 -301 6
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 177414 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 177414 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123167 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 123167 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 160682 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
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 160682 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
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 214725 None 0 Human Functional pEC50 = 6.9 6.9 -2 5
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 214773 None 0 Human Functional pEC50 = 6.9 6.9 1 5
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 160094 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 160094 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
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 176547 None 0 Human Functional pEC50 = 6.9 6.9 4 2
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 176547 None 0 Human Functional pEC50 = 6.9 6.9 4 2
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 176547 None 0 Human Functional pEC50 = 6.9 6.9 4 2
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 83256 None 0 Human Functional pEC50 = 7.9 7.9 1 5
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 83256 None 0 Human Functional pEC50 = 7.9 7.9 1 5
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
44421412 84722 None 0 Human Functional pEC50 = 7.9 7.9 10 3
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 474 2 2 5 4.6 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CC2CCCCC2)CCCC4)C[C@@]3(O)C1C5 10.1021/jm040817t
CHEMBL222579 84722 None 0 Human Functional pEC50 = 7.9 7.9 10 3
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 474 2 2 5 4.6 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CC2CCCCC2)CCCC4)C[C@@]3(O)C1C5 10.1021/jm040817t
44573251 187525 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 412 3 1 4 3.8 Nc1ccnc(N2CCC(C(=O)N3CCc4ccccc4C3)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL493744 187525 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 412 3 1 4 3.8 Nc1ccnc(N2CCC(C(=O)N3CCc4ccccc4C3)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2009.01.106
46227363 202121 None 0 Human Functional pEC50 = 7.9 7.9 -54 5
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
CHEMBL592969 202121 None 0 Human Functional pEC50 = 7.9 7.9 -54 5
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
46227363 202121 None 0 Human Functional pEC50 = 7.9 7.9 -54 5
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
CHEMBL592969 202121 None 0 Human Functional pEC50 = 7.9 7.9 -54 5
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
104787 1473 None 17 Human Functional pEC50 = 7.9 7.9 -2 4
Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmcl.2015.10.059
1608 1473 None 17 Human Functional pEC50 = 7.9 7.9 -2 4
Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmcl.2015.10.059
CHEMBL31421 1473 None 17 Human Functional pEC50 = 7.9 7.9 -2 4
Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmcl.2015.10.059
DB08861 1473 None 17 Human Functional pEC50 = 7.9 7.9 -2 4
Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmcl.2015.10.059
172450838 195593 None 0 Human Functional pEC50 = 7.9 7.9 -7 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1150 24 13 13 -0.4 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5406732 195593 None 0 Human Functional pEC50 = 7.9 7.9 -7 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1150 24 13 13 -0.4 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
23435898 165453 None 0 Human Functional pEC50 = 7.9 7.9 27 3
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)c2cccc(OC)c2)cc1 10.1021/jm000229p
CHEMBL423694 165453 None 0 Human Functional pEC50 = 7.9 7.9 27 3
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)c2cccc(OC)c2)cc1 10.1021/jm000229p
CHEMBL542267 165453 None 0 Human Functional pEC50 = 7.9 7.9 27 3
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)c2cccc(OC)c2)cc1 10.1021/jm000229p
CHEMBL379405 214725 None 0 Human Functional pEC50 = 6.9 6.9 -2 5
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 214773 None 0 Human Functional pEC50 = 6.9 6.9 1 5
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
71819402 92085 None 0 Human Functional pEC50 = 4.9 4.9 -3 4
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 331 2 1 5 1.4 COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](OC)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
CHEMBL2418740 92085 None 0 Human Functional pEC50 = 4.9 4.9 -3 4
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 331 2 1 5 1.4 COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](OC)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
122633436 177541 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 478 2 3 4 3.9 O=C(Cc1ccccc1)N1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2020.127176
CHEMBL4638693 177541 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 478 2 3 4 3.9 O=C(Cc1ccccc1)N1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2020.127176
168292466 192150 None 0 Rat Functional pEC50 = 5.9 5.9 -12 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 567 6 0 5 6.2 COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)C(=O)c4ccc(C(F)(F)F)cc4)[C@@H](C2)N(CC2CC2)CC[C@]315 10.1021/acs.jmedchem.2c00014
CHEMBL5202222 192150 None 0 Rat Functional pEC50 = 5.9 5.9 -12 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 567 6 0 5 6.2 COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)C(=O)c4ccc(C(F)(F)F)cc4)[C@@H](C2)N(CC2CC2)CC[C@]315 10.1021/acs.jmedchem.2c00014
155543078 173285 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting
ChEMBL 590 8 1 5 6.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NC(=O)Cc3ccccc3)cc1)C2 10.1021/acs.jmedchem.9b00857
CHEMBL4522335 173285 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting
ChEMBL 590 8 1 5 6.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NC(=O)Cc3ccccc3)cc1)C2 10.1021/acs.jmedchem.9b00857
162648776 179878 None 0 Human Functional pEC50 = 5.9 5.9 -5128 4
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 1338 36 16 16 0.9 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](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4744531 179878 None 0 Human Functional pEC50 = 5.9 5.9 -5128 4
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 1338 36 16 16 0.9 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](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
10206324 206019 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 484 8 0 3 6.9 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2cccs2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL66668 206019 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 484 8 0 3 6.9 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2cccs2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
10343492 75949 None 0 Mouse Functional pEC50 = 6.9 6.9 -15 3
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 445 6 3 4 3.4 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
CHEMBL205049 75949 None 0 Mouse Functional pEC50 = 6.9 6.9 -15 3
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 445 6 3 4 3.4 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
10343492 75949 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
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 445 6 3 4 3.4 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL205049 75949 None 0 Human Functional pEC50 = 6.9 6.9 -15 3
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 445 6 3 4 3.4 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
134563420 195891 None 0 Human Functional pEC50 = 6.9 6.9 -2 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 395 5 1 3 5.1 CC(=O)NCc1cc2ccccc2n1C1CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1 10.1016/j.bmc.2023.117421
CHEMBL5412738 195891 None 0 Human Functional pEC50 = 6.9 6.9 -2 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 395 5 1 3 5.1 CC(=O)NCc1cc2ccccc2n1C1CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1 10.1016/j.bmc.2023.117421
89978686 160305 None 0 Human Functional pEC50 = 6.9 6.9 -14 3
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 549 7 0 4 5.9 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(Br)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL4109652 160305 None 0 Human Functional pEC50 = 6.9 6.9 -14 3
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 549 7 0 4 5.9 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(Br)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
155559679 176535 None 0 Human Functional pEC50 = 5.9 5.9 -8 2
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 425 9 3 5 3.2 CCOc1ccc(CN2CCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4564309 176535 None 0 Human Functional pEC50 = 5.9 5.9 -8 2
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 425 9 3 5 3.2 CCOc1ccc(CN2CCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4596196 176535 None 0 Human Functional pEC50 = 5.9 5.9 -8 2
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 425 9 3 5 3.2 CCOc1ccc(CN2CCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
11271551 206234 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 478 8 0 2 6.8 CCN(CC)C(=O)c1ccc(/C(=C2\C[C@@H]3CC[C@H](C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL68113 206234 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 478 8 0 2 6.8 CCN(CC)C(=O)c1ccc(/C(=C2\C[C@@H]3CC[C@H](C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
44573292 187821 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 432 6 2 6 3.6 COc1ccc(C(=O)NC2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)c(OC)c1 10.1016/j.bmcl.2009.01.106
CHEMBL495346 187821 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 432 6 2 6 3.6 COc1ccc(C(=O)NC2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)c(OC)c1 10.1016/j.bmcl.2009.01.106
16048867 94462 None 0 Human Functional pEC50 = 7.9 7.9 -3 3
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 480 6 1 2 5.4 C[C@H]1C2Cc3ccc(C(=O)NCCc4cccc(Br)c4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
CHEMBL250993 94462 None 0 Human Functional pEC50 = 7.9 7.9 -3 3
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 480 6 1 2 5.4 C[C@H]1C2Cc3ccc(C(=O)NCCc4cccc(Br)c4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
44576628 187833 None 0 Human Functional pEC50 = 7.9 7.9 -38 4
Agonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
CHEMBL495402 187833 None 0 Human Functional pEC50 = 7.9 7.9 -38 4
Agonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
127049274 141105 None 0 Rat Functional pEC50 = 7.9 7.9 -18 3
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 487 6 3 5 4.3 COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
CHEMBL3823830 141105 None 0 Rat Functional pEC50 = 7.9 7.9 -18 3
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 487 6 3 5 4.3 COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
122195956 124277 None 0 Rat Functional pEC50 = 7.9 7.9 -22 3
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 477 6 3 4 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3CCCCC3)ccc21 10.1021/acs.jmedchem.5b01270
CHEMBL3634250 124277 None 0 Rat Functional pEC50 = 7.9 7.9 -22 3
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 477 6 3 4 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3CCCCC3)ccc21 10.1021/acs.jmedchem.5b01270
11440849 74117 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 395 5 0 5 4.3 c1ccc(Cn2ccnc2C2(c3ccccc3)CCN(c3ncccn3)CC2)cc1 10.1016/j.bmcl.2005.09.025
CHEMBL202238 74117 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 395 5 0 5 4.3 c1ccc(Cn2ccnc2C2(c3ccccc3)CCN(c3ncccn3)CC2)cc1 10.1016/j.bmcl.2005.09.025
45486033 201388 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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(CCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL584727 201388 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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(CCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2009.09.072
10549849 17976 None 0 Human Functional pEC50 = 7.9 7.9 181 3
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 416 7 0 2 6.0 CCN(CC)C(=O)c1ccc(C(=C2CCN(CC=C(C)C)CC2)c2ccccc2)cc1 10.1021/jm000229p
CHEMBL126141 17976 None 0 Human Functional pEC50 = 7.9 7.9 181 3
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 416 7 0 2 6.0 CCN(CC)C(=O)c1ccc(C(=C2CCN(CC=C(C)C)CC2)c2ccccc2)cc1 10.1021/jm000229p
71681076 91048 None 0 Human Functional pEC50 = 7.9 7.9 -5 2
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 495 4 2 6 3.5 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1cc2ccccc2cn1 10.1021/jm4012214
CHEMBL2397016 91048 None 0 Human Functional pEC50 = 7.9 7.9 -5 2
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 495 4 2 6 3.5 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1cc2ccccc2cn1 10.1021/jm4012214
CHEMBL3086750 91048 None 0 Human Functional pEC50 = 7.9 7.9 -5 2
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 495 4 2 6 3.5 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1cc2ccccc2cn1 10.1021/jm4012214
123924 3633 None 34 Human Functional pEC50 = 7.8 7.8 1 9
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
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/acs.jmedchem.9b01963
1611 3633 None 34 Human Functional pEC50 = 7.8 7.8 1 9
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
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/acs.jmedchem.9b01963
CHEMBL13470 3633 None 34 Human Functional pEC50 = 7.8 7.8 1 9
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
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/acs.jmedchem.9b01963
156010938 177153 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 476 2 2 4 4.1 O=C(Cc1ccccc1)N1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2020.127176
CHEMBL4632584 177153 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 476 2 2 4 4.1 O=C(Cc1ccccc1)N1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2020.127176
73350639 91664 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 747 11 3 6 5.1 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
CHEMBL2408016 91664 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 747 11 3 6 5.1 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
45486013 200033 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 9 1 6 4.5 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3nccn3C)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL570448 200033 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 9 1 6 4.5 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3nccn3C)CC2)cc1 10.1016/j.bmcl.2009.09.072
58296565 145772 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 501 8 0 5 5.1 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
CHEMBL3916122 145772 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 501 8 0 5 5.1 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
72713091 106486 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 378 6 2 3 4.4 CN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1 10.1021/jm401250s
CHEMBL3139588 106486 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 378 6 2 3 4.4 CN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1 10.1021/jm401250s
CHEMBL3217272 106486 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 378 6 2 3 4.4 CN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1 10.1021/jm401250s
162665119 182255 None 0 Human Functional pEC50 = 6.9 6.9 -10 2
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 510 4 0 8 4.7 CC(=O)O[C@@H]1C=C(OC(=O)c2cccc(F)c2)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
CHEMBL4782368 182255 None 0 Human Functional pEC50 = 6.9 6.9 -10 2
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 510 4 0 8 4.7 CC(=O)O[C@@H]1C=C(OC(=O)c2cccc(F)c2)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
25129780 187769 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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)Oc3cc(O)ccc32)cc1 10.1021/jm8008986
CHEMBL495094 187769 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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)Oc3cc(O)ccc32)cc1 10.1021/jm8008986
17540413 44146 None 3 Human Functional pEC50 = 4.9 4.9 - 1
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 467 10 2 5 3.9 CCOc1ccc(S(=O)(=O)Nc2cccc(C(=O)NCC(c3ccccc3)N(C)C)c2)cc1 nan
CHEMBL1515502 44146 None 3 Human Functional pEC50 = 4.9 4.9 - 1
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 467 10 2 5 3.9 CCOc1ccc(S(=O)(=O)Nc2cccc(C(=O)NCC(c3ccccc3)N(C)C)c2)cc1 nan
45485837 199814 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 10 0 4 6.0 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL569084 199814 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 10 0 4 6.0 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
24789740 55192 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 426 5 1 3 6.7 CCc1ccc(Nc2n[n+](-c3ccccc3)c(-c3c(Cl)cccc3Cl)s2)cc1 nan
CHEMBL1315948 55192 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 426 5 1 3 6.7 CCc1ccc(Nc2n[n+](-c3ccccc3)c(-c3c(Cl)cccc3Cl)s2)cc1 nan
CHEMBL1617450 55192 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 426 5 1 3 6.7 CCc1ccc(Nc2n[n+](-c3ccccc3)c(-c3c(Cl)cccc3Cl)s2)cc1 nan
155566580 176349 None 0 Human Functional pEC50 = 6.9 6.9 -4 3
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1110 12 12 14 0.8 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSCc2ccccc2CSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
CHEMBL4586954 176349 None 0 Human Functional pEC50 = 6.9 6.9 -4 3
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1110 12 12 14 0.8 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSCc2ccccc2CSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
CHEMBL4594798 176349 None 0 Human Functional pEC50 = 6.9 6.9 -4 3
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1110 12 12 14 0.8 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSCc2ccccc2CSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
162650094 180232 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 405 6 1 4 4.5 COC(=O)/C=C/[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
CHEMBL4748689 180232 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 405 6 1 4 4.5 COC(=O)/C=C/[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
118200640 165938 None 0 Rat Functional pEC50 = 6.8 6.8 2 2
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 423 5 0 5 3.5 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C=O)C2 10.1016/j.bmc.2018.07.020
CHEMBL4248801 165938 None 0 Rat Functional pEC50 = 6.8 6.8 2 2
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 423 5 0 5 3.5 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C=O)C2 10.1016/j.bmc.2018.07.020
10116470 206276 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 476 6 0 2 6.6 O=C(c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1)N1CCCC1 10.1016/j.bmcl.2004.02.051
CHEMBL68416 206276 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 476 6 0 2 6.6 O=C(c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1)N1CCCC1 10.1016/j.bmcl.2004.02.051
44406272 141060 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 436 5 1 3 5.5 O=C(Nc1ccccc1)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1 10.1016/j.bmcl.2005.09.025
CHEMBL382326 141060 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 436 5 1 3 5.5 O=C(Nc1ccccc1)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1 10.1016/j.bmcl.2005.09.025
135938588 106939 None 1 Human Functional pEC50 = 4.8 4.8 -5 3
PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]
ChEMBL 376 3 1 4 4.7 Cc1ccc(-n2[nH]c(C)c(C=Nc3ccc(Cl)c4cccnc34)c2=O)cc1 nan
CHEMBL3145240 106939 None 1 Human Functional pEC50 = 4.8 4.8 -5 3
PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]
ChEMBL 376 3 1 4 4.7 Cc1ccc(-n2[nH]c(C)c(C=Nc3ccc(Cl)c4cccnc34)c2=O)cc1 nan
376180 60259 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 509 10 2 6 7.0 CCN(CC)Cc1cc(Nc2c3ccccc3nc3c4ccccc4n(C)c23)cc(CN(CC)CC)c1O nan
CHEMBL1734003 60259 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 509 10 2 6 7.0 CCN(CC)Cc1cc(Nc2c3ccccc3nc3c4ccccc4n(C)c23)cc(CN(CC)CC)c1O nan
CHEMBL1740933 60259 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 509 10 2 6 7.0 CCN(CC)Cc1cc(Nc2c3ccccc3nc3c4ccccc4n(C)c23)cc(CN(CC)CC)c1O nan
44307027 103175 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 388 5 0 2 5.2 CCN(CC)C(=O)c1ccc(/C(=C2\C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL307775 103175 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 388 5 0 2 5.2 CCN(CC)C(=O)c1ccc(/C(=C2\C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
42629165 191212 None 0 Rat Functional pEC50 = 5.8 5.8 -5 2
Agonist activity at recombinant rat DOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at recombinant rat DOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding
ChEMBL 416 5 2 7 2.5 CC[C@@H]1CN2CC[C@]3(O)c4c(cccc4OC)N[C@@H]3[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.0c01915
CHEMBL5187788 191212 None 0 Rat Functional pEC50 = 5.8 5.8 -5 2
Agonist activity at recombinant rat DOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at recombinant rat DOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding
ChEMBL 416 5 2 7 2.5 CC[C@@H]1CN2CC[C@]3(O)c4c(cccc4OC)N[C@@H]3[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.0c01915
CHEMBL408330 215165 None 0 Human Functional pEC50 = 7.8 7.8 -1 4
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](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
CHEMBL294616 213353 None 0 Human Functional pEC50 = 7.8 7.8 -2 7
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 None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1016/j.bmc.2009.07.069
16100409 83266 None 0 Human Functional pEC50 = 7.8 7.8 -1 5
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 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](N)Cc1ccccc1)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
CHEMBL218651 83266 None 0 Human Functional pEC50 = 7.8 7.8 -1 5
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 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](N)Cc1ccccc1)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
73350639 91664 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 747 11 3 6 5.1 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
CHEMBL2408016 91664 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 747 11 3 6 5.1 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
127050831 141104 None 0 Rat Functional pEC50 = 7.8 7.8 -2 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 515 9 3 6 4.1 CCOC(=O)CN1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
CHEMBL3823815 141104 None 0 Rat Functional pEC50 = 7.8 7.8 -2 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 515 9 3 6 4.1 CCOC(=O)CN1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
CHEMBL408330 215165 None 0 Human Functional pEC50 = 7.8 7.8 -1 4
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](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
25232540 192909 None 2 Human Functional pEC50 = 7.8 7.8 -4 3
Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 447 4 3 6 2.2 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1 10.1021/jm301247n
CHEMBL522143 192909 None 2 Human Functional pEC50 = 7.8 7.8 -4 3
Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 447 4 3 6 2.2 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1 10.1021/jm301247n
CHEMBL5086477 217522 None 2 Human Functional pEC50 = 7.8 7.8 -13 3
Antagonist activity at human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cnc[nH]1 10.1021/acs.jmedchem.1c02185
CHEMBL254919 212972 None 0 Human Functional pEC50 = 7.8 7.8 -10 3
Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm060998u
CHEMBL254919 212972 None 0 Human Functional pEC50 = 7.8 7.8 -10 3
Antagonist activity at delta opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assayAntagonist activity at delta opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O 10.1016/j.bmcl.2008.01.009
90655825 111268 None 0 Human Functional pEC50 = 7.8 7.8 6 3
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 502 4 1 6 3.6 CC(C)CN1CC[C@@]23c4c5ccc(O)c4OCO[C@]46CC[C@@]2(O[C@H](C(=O)N4Cc2ccccc2)[C@H]63)[C@H]1C5 10.1021/ml400491k
CHEMBL3264744 111268 None 0 Human Functional pEC50 = 7.8 7.8 6 3
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 502 4 1 6 3.6 CC(C)CN1CC[C@@]23c4c5ccc(O)c4OCO[C@]46CC[C@@]2(O[C@H](C(=O)N4Cc2ccccc2)[C@H]63)[C@H]1C5 10.1021/ml400491k
1627 2594 None 9 Human Functional pEC50 = 7.8 7.8 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm101211p
1845 2594 None 9 Human Functional pEC50 = 7.8 7.8 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm101211p
5288826 2594 None 9 Human Functional pEC50 = 7.8 7.8 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm101211p
5288826.0 2594 None 9 Human Functional pEC50 = 7.8 7.8 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm101211p
CHEMBL70 2594 None 9 Human Functional pEC50 = 7.8 7.8 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm101211p
DB00295 2594 None 9 Human Functional pEC50 = 7.8 7.8 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm101211p
123924 3633 None 34 Human Functional pEC50 = 7.8 7.8 1 9
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 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 10.1016/j.bmcl.2009.03.099
1611 3633 None 34 Human Functional pEC50 = 7.8 7.8 1 9
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 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 10.1016/j.bmcl.2009.03.099
CHEMBL13470 3633 None 34 Human Functional pEC50 = 7.8 7.8 1 9
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 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 10.1016/j.bmcl.2009.03.099
123924 3633 None 34 Human Functional pEC50 = 7.8 7.8 1 9
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 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 10.1016/j.bmc.2011.11.047
1611 3633 None 34 Human Functional pEC50 = 7.8 7.8 1 9
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 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 10.1016/j.bmc.2011.11.047
CHEMBL13470 3633 None 34 Human Functional pEC50 = 7.8 7.8 1 9
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 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 10.1016/j.bmc.2011.11.047
CHEMBL294616 213353 None 0 Human Functional pEC50 = 7.8 7.8 -2 7
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 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/acsmedchemlett.5b00056
10642670 18025 None 0 Human Functional pEC50 = 7.8 7.8 724 2
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 366 5 1 2 4.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccccc2F)cc1 10.1021/jm000229p
CHEMBL126370 18025 None 0 Human Functional pEC50 = 7.8 7.8 724 2
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 366 5 1 2 4.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccccc2F)cc1 10.1021/jm000229p
CHEMBL247064 212962 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 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)Cc1ccc2nc(N)sc2c1)C(=O)O 10.1016/j.bmcl.2007.01.092
24768354 98019 None 0 Human Functional pEC50 = 6.8 6.8 -3 3
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 955 22 8 9 3.0 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)Cc1ccccc1 10.1021/jm070332f
CHEMBL272665 98019 None 0 Human Functional pEC50 = 6.8 6.8 -3 3
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 955 22 8 9 3.0 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)Cc1ccccc1 10.1021/jm070332f
11211122 198169 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 377 4 1 4 3.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cn1 10.1021/jm900773n
CHEMBL557054 198169 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 377 4 1 4 3.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cn1 10.1021/jm900773n
CHEMBL3609616 214290 None 0 Human Functional pEC50 = 6.8 6.8 -3 3
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 None None None C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)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
23635166 169073 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 784 17 7 9 1.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)CCC(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC1 10.1021/jm061465o
CHEMBL439026 169073 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 784 17 7 9 1.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)CCC(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC1 10.1021/jm061465o
1967479 43375 None 4 Human Functional pEC50 = 4.8 4.8 - 1
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 344 2 1 5 3.6 Cc1cc(/C=C2\SC(=S)N(C)C2=O)c(C)n1-c1ccc(O)cc1 nan
CHEMBL1507251 43375 None 4 Human Functional pEC50 = 4.8 4.8 - 1
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 344 2 1 5 3.6 Cc1cc(/C=C2\SC(=S)N(C)C2=O)c(C)n1-c1ccc(O)cc1 nan
86711654 160589 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 578 9 0 6 4.4 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CN(Cc1ccccc1)S(C)(=O)=O)C2 nan
CHEMBL4112051 160589 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 578 9 0 6 4.4 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CN(Cc1ccccc1)S(C)(=O)=O)C2 nan
23635166 169073 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 784 17 7 9 1.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)CCC(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC1 10.1021/jm061465o
CHEMBL439026 169073 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
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 784 17 7 9 1.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)CCC(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC1 10.1021/jm061465o
44307027 205516 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 388 5 0 2 5.2 CCN(CC)C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL63597 205516 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 388 5 0 2 5.2 CCN(CC)C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
168273707 190526 None 0 Rat Functional pEC50 = 6.8 6.8 -74 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 425 5 1 5 3.3 COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)CO)[C@@H](C2)N(CC2CC2)CC[C@]315 10.1021/acs.jmedchem.2c00014
CHEMBL5177908 190526 None 0 Rat Functional pEC50 = 6.8 6.8 -74 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 425 5 1 5 3.3 COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)CO)[C@@H](C2)N(CC2CC2)CC[C@]315 10.1021/acs.jmedchem.2c00014
162643991 181904 None 0 Human Functional pEC50 = 6.8 6.8 -7 5
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 1126 32 14 14 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[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
CHEMBL4777999 181904 None 0 Human Functional pEC50 = 6.8 6.8 -7 5
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 1126 32 14 14 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[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
5461577 67501 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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)c1ccccc1[N+](=O)[O-] nan
CHEMBL1892729 67501 None 0 Human Functional pEC50 = 4.8 4.8 - 1
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)c1ccccc1[N+](=O)[O-] nan
1599 2341 None 28 Human Functional pEC50 = 6.8 6.8 -138 32
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/jm030548r
3955 2341 None 28 Human Functional pEC50 = 6.8 6.8 -138 32
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/jm030548r
3955.0 2341 None 28 Human Functional pEC50 = 6.8 6.8 -138 32
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/jm030548r
7215 2341 None 28 Human Functional pEC50 = 6.8 6.8 -138 32
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/jm030548r
CHEMBL841 2341 None 28 Human Functional pEC50 = 6.8 6.8 -138 32
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/jm030548r
DB00836 2341 None 28 Human Functional pEC50 = 6.8 6.8 -138 32
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/jm030548r
162643991 181904 None 0 Human Functional pEC50 = 6.8 6.8 -7 5
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 1126 32 14 14 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[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
CHEMBL4777999 181904 None 0 Human Functional pEC50 = 6.8 6.8 -7 5
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 1126 32 14 14 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[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
23661598 94092 None 0 Human Functional pEC50 = 7.8 7.8 67 2
Activity at delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S bindingActivity at delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 392 0 3 4 2.9 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccc(F)cc4c2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2007.07.098
CHEMBL248839 94092 None 0 Human Functional pEC50 = 7.8 7.8 67 2
Activity at delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S bindingActivity at delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 392 0 3 4 2.9 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccc(F)cc4c2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2007.07.098
25256782 193240 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 386 3 1 7 3.0 Nc1ccnc(N2CCC(n3c(=O)n(-c4ccccc4)c4cccnc43)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL522854 193240 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 386 3 1 7 3.0 Nc1ccnc(N2CCC(n3c(=O)n(-c4ccccc4)c4cccnc43)CC2)c1 10.1016/j.bmcl.2009.01.106
44254057 198134 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 378 4 1 3 4.2 CCN(CC)C(=O)c1ccc([C@H]2CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL556648 198134 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 378 4 1 3 4.2 CCN(CC)C(=O)c1ccc([C@H]2CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL294616 213353 None 0 Human Functional pEC50 = 7.8 7.8 -2 7
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/jm701440h
10164835 205463 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 517 8 1 2 7.3 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2c[nH]c3ccccc23)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL63213 205463 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 517 8 1 2 7.3 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2c[nH]c3ccccc23)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL2371978 212631 None 0 Human Functional pEC50 = 7.8 7.8 -3 4
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](Cc1ccccc1)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
104787 1473 None 17 Human Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None None 10.1016/j.bmc.2016.02.034
1608 1473 None 17 Human Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None None 10.1016/j.bmc.2016.02.034
CHEMBL31421 1473 None 17 Human Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None None 10.1016/j.bmc.2016.02.034
DB08861 1473 None 17 Human Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None None 10.1016/j.bmc.2016.02.034
44177770 123068 None 0 Human Functional pEC50 = 6.8 6.8 -12 3
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 939 20 8 9 4.1 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCC(=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
CHEMBL3608937 123068 None 0 Human Functional pEC50 = 6.8 6.8 -12 3
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 939 20 8 9 4.1 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCC(=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
16294686 43818 None 3 Human Functional pEC50 = 5.8 5.8 1 3
PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]
ChEMBL 479 10 2 5 3.4 CC(=O)c1ccc(S(=O)(=O)NCc2ccc(C(=O)NCC(c3ccccc3)N(C)C)cc2)cc1 nan
CHEMBL1511139 43818 None 3 Human Functional pEC50 = 5.8 5.8 1 3
PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]
ChEMBL 479 10 2 5 3.4 CC(=O)c1ccc(S(=O)(=O)NCc2ccc(C(=O)NCC(c3ccccc3)N(C)C)cc2)cc1 nan
71819526 92089 None 0 Human Functional pEC50 = 4.8 4.8 -7 4
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 329 1 1 4 2.3 COc1cc(C)c2c3c1O[C@H]1[C@@H](O)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
CHEMBL2418744 92089 None 0 Human Functional pEC50 = 4.8 4.8 -7 4
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 329 1 1 4 2.3 COc1cc(C)c2c3c1O[C@H]1[C@@H](O)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
10594839 18112 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 362 5 0 2 4.7 CCN(CC)C(=O)c1ccc(C(=C2CCN(C)CC2)c2ccccc2)cc1 10.1021/jm000229p
CHEMBL126842 18112 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 362 5 0 2 4.7 CCN(CC)C(=O)c1ccc(C(=C2CCN(C)CC2)c2ccccc2)cc1 10.1021/jm000229p
172467824 196974 None 0 Human Functional pEC50 = 6.8 6.8 -12 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5435869 196974 None 0 Human Functional pEC50 = 6.8 6.8 -12 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
44339472 111399 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 397 7 0 4 4.3 CCCCOc1cccc2c1C13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3 10.1021/jm031126k
CHEMBL326860 111399 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 397 7 0 4 4.3 CCCCOc1cccc2c1C13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3 10.1021/jm031126k
162648597 179865 None 0 Human Functional pEC50 = 6.8 6.8 -5 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4744365 179865 None 0 Human Functional pEC50 = 6.8 6.8 -5 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162648597 179865 None 0 Human Functional pEC50 = 6.8 6.8 -5 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4744365 179865 None 0 Human Functional pEC50 = 6.8 6.8 -5 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL3580744 214231 None 0 Human Functional pEC50 = 6.8 6.8 -107 6
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(C(F)(F)F)cc2)C(=O)N1 10.1021/acsmedchemlett.5b00056
122181052 121865 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assayAgonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
ChEMBL 534 9 1 5 5.8 CC(C)C[C@H]1CN2C(=CC3=NC[C@H](Cc4ccccc4)N3C[C@@H]2Cc2ccc(O)cc2)N1CCc1ccccc1 10.1021/jm501637c
CHEMBL3589705 121865 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assayAgonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
ChEMBL 534 9 1 5 5.8 CC(C)C[C@H]1CN2C(=CC3=NC[C@H](Cc4ccccc4)N3C[C@@H]2Cc2ccc(O)cc2)N1CCc1ccccc1 10.1021/jm501637c
89978382 160259 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
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 561 10 2 7 4.2 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccc(C(O)CO)cc1)C2 nan
CHEMBL4109220 160259 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
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 561 10 2 7 4.2 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccc(C(O)CO)cc1)C2 nan
24768397 146506 None 0 Human Functional pEC50 = 6.8 6.8 -7 3
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 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/jm061465o
CHEMBL392185 146506 None 0 Human Functional pEC50 = 6.8 6.8 -7 3
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 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/jm061465o
123924 3633 None 34 Rat Functional pEC50 = 6.8 6.8 -2 9
Agonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassayAgonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassay
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/jm9007483
1611 3633 None 34 Rat Functional pEC50 = 6.8 6.8 -2 9
Agonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassayAgonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassay
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/jm9007483
CHEMBL13470 3633 None 34 Rat Functional pEC50 = 6.8 6.8 -2 9
Agonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassayAgonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassay
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/jm9007483
24768353 97801 None 0 Human Functional pEC50 = 7.8 7.8 -18 3
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 941 22 9 9 2.7 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm070332f
CHEMBL271619 97801 None 0 Human Functional pEC50 = 7.8 7.8 -18 3
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 941 22 9 9 2.7 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm070332f
CHEMBL2371978 212631 None 0 Human Functional pEC50 = 7.8 7.8 -3 4
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](Cc1ccccc1)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
122182781 122384 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 424 2 3 4 3.4 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CC(F)F)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL3596366 122384 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 424 2 3 4 3.4 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CC(F)F)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL3598302 122384 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 424 2 3 4 3.4 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CC(F)F)CC[C@]314 10.1016/j.bmcl.2015.05.038
661788 23311 None 12 Human Functional pEC50 = 7.8 7.8 245 2
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 497 8 2 6 5.6 COc1ccc(C2Nc3ccccc3C(=O)N2Cc2ccco2)cc1COc1ccc(NC(C)=O)cc1 nan
CHEMBL1332208 23311 None 12 Human Functional pEC50 = 7.8 7.8 245 2
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 497 8 2 6 5.6 COc1ccc(C2Nc3ccccc3C(=O)N2Cc2ccco2)cc1COc1ccc(NC(C)=O)cc1 nan
66826937 160490 None 0 Human Functional pEC50 = 7.8 7.8 -20 3
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 433 5 2 5 3.7 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1)[C@H]2O5 nan
CHEMBL4111231 160490 None 0 Human Functional pEC50 = 7.8 7.8 -20 3
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 433 5 2 5 3.7 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1)[C@H]2O5 nan
45485877 200060 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 491 10 0 5 6.1 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3cccs3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL570645 200060 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 491 10 0 5 6.1 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3cccs3)CC2)cc1 10.1016/j.bmcl.2009.09.072
11849364 204919 None 0 Human Functional pEC50 = 7.8 7.8 -4 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 518 6 1 5 4.3 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5Cl)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm0604777
CHEMBL611139 204919 None 0 Human Functional pEC50 = 7.8 7.8 -4 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 518 6 1 5 4.3 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5Cl)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm0604777
CHEMBL2387327 212865 None 0 Human Functional pEC50 = 6.8 6.8 -4 3
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](CCC(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1016/j.bmcl.2013.03.065
24768397 146506 None 0 Human Functional pEC50 = 6.8 6.8 -7 3
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 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/jm061465o
CHEMBL392185 146506 None 0 Human Functional pEC50 = 6.8 6.8 -7 3
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 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/jm061465o
CHEMBL133719 211180 None 0 Mouse Functional pEC50 = 6.8 6.8 1 3
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
44439875 93671 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 596 16 7 7 -0.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cccc(C(N)=O)c1)C(=O)O 10.1016/j.bmcl.2007.01.092
CHEMBL246682 93671 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 596 16 7 7 -0.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cccc(C(N)=O)c1)C(=O)O 10.1016/j.bmcl.2007.01.092
118725841 117230 None 0 Human Functional pEC50 = 5.8 5.8 -239 3
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 5 1 4 4.7 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.12.064
CHEMBL3393991 117230 None 0 Human Functional pEC50 = 5.8 5.8 -239 3
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 5 1 4 4.7 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2014.12.064
44573332 187526 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 366 4 2 5 2.5 Nc1ccnc(N2CCC(NC(=O)[C@@H]3CCCO3)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL493752 187526 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 366 4 2 5 2.5 Nc1ccnc(N2CCC(NC(=O)[C@@H]3CCCO3)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2009.01.106
1650 1980 None 8 Human Functional pEC50 = 4.8 4.8 -2754 4
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 464 9 1 4 4.3 OC(=O)COc1cccc(c1)C(N(C(=O)Cc1ccc(c(c1)Cl)Cl)C)CN1CCCC1 nan
3683 1980 None 8 Human Functional pEC50 = 4.8 4.8 -2754 4
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 464 9 1 4 4.3 OC(=O)COc1cccc(c1)C(N(C(=O)Cc1ccc(c(c1)Cl)Cl)C)CN1CCCC1 nan
CHEMBL23472 1980 None 8 Human Functional pEC50 = 4.8 4.8 -2754 4
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 464 9 1 4 4.3 OC(=O)COc1cccc(c1)C(N(C(=O)Cc1ccc(c(c1)Cl)Cl)C)CN1CCCC1 nan
157010706 183275 None 2 Human Functional pEC50 = 6.8 6.8 -58 2
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 515 11 1 3 5.0 CCC(=O)N(Cc1ccccc1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
CHEMBL4795492 183275 None 2 Human Functional pEC50 = 6.8 6.8 -58 2
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 515 11 1 3 5.0 CCC(=O)N(Cc1ccccc1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
10185016 205982 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 8 0 3 6.5 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CC(=O)c2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL66387 205982 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 8 0 3 6.5 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CC(=O)c2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
162677056 183660 None 0 Human Functional pEC50 = 6.8 6.8 -22 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4800237 183660 None 0 Human Functional pEC50 = 6.8 6.8 -22 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162677056 183660 None 0 Human Functional pEC50 = 6.8 6.8 -22 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4800237 183660 None 0 Human Functional pEC50 = 6.8 6.8 -22 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
10765126 121089 None 0 Mouse Functional pEC50 = 6.8 6.8 -5 3
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 358 5 1 3 4.3 Oc1cccc(C(c2ccccc2)N2CCN(Cc3ccccc3)CC2)c1 10.1021/jm980374r
CHEMBL356587 121089 None 0 Mouse Functional pEC50 = 6.8 6.8 -5 3
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 358 5 1 3 4.3 Oc1cccc(C(c2ccccc2)N2CCN(Cc3ccccc3)CC2)c1 10.1021/jm980374r
86711656 160105 None 0 Human Functional pEC50 = 6.8 6.8 -77 3
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 517 8 0 5 5.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CSCc1ccccc1)C2 nan
CHEMBL4107918 160105 None 0 Human Functional pEC50 = 6.8 6.8 -77 3
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 517 8 0 5 5.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CSCc1ccccc1)C2 nan
89978524 160667 None 0 Human Functional pEC50 = 6.8 6.8 -7 3
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 447 6 1 5 4.0 COc1ccc2c3c1O[C@@H]1[C@]34CCN[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
CHEMBL4112656 160667 None 0 Human Functional pEC50 = 6.8 6.8 -7 3
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 447 6 1 5 4.0 COc1ccc2c3c1O[C@@H]1[C@]34CCN[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
145986165 165633 None 0 Rat Functional pEC50 = 5.8 5.8 -10 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 567 6 0 5 6.2 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccc(C(F)(F)F)cc1)C2 10.1016/j.bmc.2018.07.020
CHEMBL4241369 165633 None 0 Rat Functional pEC50 = 5.8 5.8 -10 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 567 6 0 5 6.2 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccc(C(F)(F)F)cc1)C2 10.1016/j.bmc.2018.07.020
162648890 180002 None 0 Human Functional pEC50 = 6.8 6.8 -26 4
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 1394 36 20 16 -0.8 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](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2cccc(O)c2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4745899 180002 None 0 Human Functional pEC50 = 6.8 6.8 -26 4
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 1394 36 20 16 -0.8 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](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2cccc(O)c2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
10093250 102795 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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
CHEMBL304989 102795 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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
3606260 20469 None 4 Human Functional pEC50 = 4.8 4.8 -6 2
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 328 5 2 3 3.7 Cc1cccc(NC(S)=NCC(c2cccnc2)N(C)C)c1C nan
CHEMBL1307063 20469 None 4 Human Functional pEC50 = 4.8 4.8 -6 2
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 328 5 2 3 3.7 Cc1cccc(NC(S)=NCC(c2cccnc2)N(C)C)c1C nan
16048941 155072 None 0 Human Functional pEC50 = 7.8 7.8 -2 3
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 478 7 1 2 6.3 C[C@H]1C2Cc3ccc(C(=O)NCCc4cccc(-c5ccccc5)c4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
CHEMBL401278 155072 None 0 Human Functional pEC50 = 7.8 7.8 -2 3
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 478 7 1 2 6.3 C[C@H]1C2Cc3ccc(C(=O)NCCc4cccc(-c5ccccc5)c4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
58443192 84217 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 536 9 1 3 7.0 CC(C)Oc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1 10.1016/j.bmcl.2012.10.081
CHEMBL2208361 84217 None 0 Human Functional pEC50 = 7.8 7.8 -3 3
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 536 9 1 3 7.0 CC(C)Oc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1 10.1016/j.bmcl.2012.10.081
44279594 107170 None 0 Human Functional pEC50 = 7.7 7.7 -23 3
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 423 1 2 5 3.2 CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm991165p
CHEMBL31605 107170 None 0 Human Functional pEC50 = 7.7 7.7 -23 3
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 423 1 2 5 3.2 CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm991165p
1619 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None None 10.1016/j.ejmech.2015.12.012
25075996 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None None 10.1016/j.ejmech.2015.12.012
25077992 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None None 10.1016/j.ejmech.2015.12.012
CHEMBL265813 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None None 10.1016/j.ejmech.2015.12.012
CHEMBL405618 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None None 10.1016/j.ejmech.2015.12.012
1619 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None None 10.1016/j.bmc.2016.02.034
25075996 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None None 10.1016/j.bmc.2016.02.034
25077992 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None None 10.1016/j.bmc.2016.02.034
CHEMBL265813 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None None 10.1016/j.bmc.2016.02.034
CHEMBL405618 1517 None 34 Human Functional pEC50 = 7.7 7.7 -6 7
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None None 10.1016/j.bmc.2016.02.034
101600082 1516 None 24 Human Functional pEC50 = 7.7 7.7 -30 6
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 None 10.1021/acsmedchemlett.5b00056
16133805 1516 None 24 Human Functional pEC50 = 7.7 7.7 -30 6
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 None 10.1021/acsmedchemlett.5b00056
1620 1516 None 24 Human Functional pEC50 = 7.7 7.7 -30 6
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 None 10.1021/acsmedchemlett.5b00056
44298303 1516 None 24 Human Functional pEC50 = 7.7 7.7 -30 6
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 None 10.1021/acsmedchemlett.5b00056
91928823 1516 None 24 Human Functional pEC50 = 7.7 7.7 -30 6
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 None 10.1021/acsmedchemlett.5b00056
CHEMBL411557 1516 None 24 Human Functional pEC50 = 7.7 7.7 -30 6
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 None 10.1021/acsmedchemlett.5b00056
DB16146 1516 None 24 Human Functional pEC50 = 7.7 7.7 -30 6
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 None 10.1021/acsmedchemlett.5b00056
45486028 199999 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 4 6.4 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCC3CCCCC3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL570233 199999 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 4 6.4 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCC3CCCCC3)CC2)cc1 10.1016/j.bmcl.2009.09.072
132079905 181517 None 0 Human Functional pEC50 = 6.8 6.8 -10 3
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 510 4 0 8 4.6 COC(=O)[C@@H]1C=C(OC(=O)c2ccccc2F)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
CHEMBL4763725 181517 None 0 Human Functional pEC50 = 6.8 6.8 -10 3
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 510 4 0 8 4.6 COC(=O)[C@@H]1C=C(OC(=O)c2ccccc2F)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
118725741 117215 None 0 Human Functional pEC50 = 5.8 5.8 -53 3
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 352 5 1 4 3.5 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.12.064
CHEMBL3393881 117215 None 0 Human Functional pEC50 = 5.8 5.8 -53 3
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 352 5 1 4 3.5 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.12.064
118725856 117245 None 0 Human Functional pEC50 = 5.7 5.7 -186 3
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 384 5 2 5 3.0 O=C(Nc1nc2ccccc2n1CCN1CC[C@H](O)C1)c1ccc(Cl)cc1 10.1016/j.bmcl.2014.12.064
CHEMBL3394006 117245 None 0 Human Functional pEC50 = 5.7 5.7 -186 3
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 384 5 2 5 3.0 O=C(Nc1nc2ccccc2n1CCN1CC[C@H](O)C1)c1ccc(Cl)cc1 10.1016/j.bmcl.2014.12.064
89978582 161015 None 0 Human Functional pEC50 = 6.7 6.7 -28 3
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 457 6 0 4 5.0 C=Cc1ccc2c3c1O[C@@H]1[C@]34CCN(C)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
CHEMBL4115338 161015 None 0 Human Functional pEC50 = 6.7 6.7 -28 3
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 457 6 0 4 5.0 C=Cc1ccc2c3c1O[C@@H]1[C@]34CCN(C)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
9932852 123238 None 0 Mouse Functional pEC50 = 7.7 7.7 1 3
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 438 5 3 4 4.0 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
CHEMBL361274 123238 None 0 Mouse Functional pEC50 = 7.7 7.7 1 3
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 438 5 3 4 4.0 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
16100410 141885 None 0 Human Functional pEC50 = 7.7 7.7 1 5
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 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)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
CHEMBL386212 141885 None 0 Human Functional pEC50 = 7.7 7.7 1 5
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 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)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
53388316 66574 None 0 Human Functional pEC50 = 7.7 7.7 -6 3
Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 504 6 4 7 1.3 O=C(CNC(=O)c1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm301247n
CHEMBL1824517 66574 None 0 Human Functional pEC50 = 7.7 7.7 -6 3
Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 504 6 4 7 1.3 O=C(CNC(=O)c1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm301247n
CHEMBL1852458 66574 None 0 Human Functional pEC50 = 7.7 7.7 -6 3
Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 504 6 4 7 1.3 O=C(CNC(=O)c1ccncc1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm301247n
9932852 123238 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 438 5 3 4 4.0 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL361274 123238 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 438 5 3 4 4.0 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
71460945 82748 None 0 Human Functional pEC50 = 7.7 7.7 4 3
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 4 1 6 5.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2ncc(-c4ccc(Cl)cc4)cc2C[C@@]3(OC(=O)Cc2ccccc2)[C@H]1C5 10.1021/jm300686p
CHEMBL2179661 82748 None 0 Human Functional pEC50 = 7.7 7.7 4 3
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 4 1 6 5.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2ncc(-c4ccc(Cl)cc4)cc2C[C@@]3(OC(=O)Cc2ccccc2)[C@H]1C5 10.1021/jm300686p
11428837 187645 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 376 4 1 3 4.1 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL494462 187645 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 376 4 1 3 4.1 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
11428837 187645 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 376 4 1 3 4.1 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
CHEMBL494462 187645 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 376 4 1 3 4.1 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
71456256 79203 None 0 Human Functional pEC50 = 7.7 7.7 2 2
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 485 6 3 4 4.9 CCCCCCC(=O)N[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm021073r
CHEMBL2113372 79203 None 0 Human Functional pEC50 = 7.7 7.7 2 2
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 485 6 3 4 4.9 CCCCCCC(=O)N[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm021073r
145961895 161477 None 0 Rat Functional pEC50 = 7.7 7.7 -194 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 622 16 9 7 0.4 CC(C)=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4126322 161477 None 0 Rat Functional pEC50 = 7.7 7.7 -194 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 622 16 9 7 0.4 CC(C)=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
71680922 91052 None 0 Human Functional pEC50 = 7.7 7.7 -11 2
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 445 4 2 6 2.4 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1ccccn1 10.1021/jm4012214
CHEMBL2397020 91052 None 0 Human Functional pEC50 = 7.7 7.7 -11 2
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 445 4 2 6 2.4 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1ccccn1 10.1021/jm4012214
CHEMBL3086746 91052 None 0 Human Functional pEC50 = 7.7 7.7 -11 2
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 445 4 2 6 2.4 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1ccccn1 10.1021/jm4012214
156012282 178405 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 1223 13 12 18 0.0 Cc1cc(=O)oc2ccc(N3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)cc12 10.1021/acsmedchemlett.9b00569
CHEMBL4636807 178405 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 1223 13 12 18 0.0 Cc1cc(=O)oc2ccc(N3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)cc12 10.1021/acsmedchemlett.9b00569
CHEMBL4650976 178405 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 1223 13 12 18 0.0 Cc1cc(=O)oc2ccc(N3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)cc12 10.1021/acsmedchemlett.9b00569
CHEMBL2419540 212900 None 0 Human Functional pEC50 = 6.7 6.7 -22 3
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)N1CCC[C@@H]1C(=O)N[C@@H](CC(C)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.2013.06.065
44254957 197783 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 374 2 1 3 3.7 CCN1CCc2cc(C3=CC4(CCNCC4)Oc4ccccc43)ccc2C1=O 10.1021/jm900773n
CHEMBL551615 197783 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 374 2 1 3 3.7 CCN1CCc2cc(C3=CC4(CCNCC4)Oc4ccccc43)ccc2C1=O 10.1021/jm900773n
CHEMBL235743 212033 None 1 Human Functional pEC50 = 6.7 6.7 -31 4
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 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm100982d
25129432 187765 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 307 2 1 3 3.6 COc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
CHEMBL495073 187765 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 307 2 1 3 3.6 COc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
CHEMBL235743 212033 None 1 Human Functional pEC50 = 6.7 6.7 -31 4
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 None None None C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061465o
CHEMBL235743 212033 None 1 Human Functional pEC50 = 6.7 6.7 -31 4
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 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm100982d
CHEMBL235743 212033 None 1 Human Functional pEC50 = 6.7 6.7 -31 4
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 None None None C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061465o
134563361 195627 None 0 Human Functional pEC50 = 6.7 6.7 -10 4
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 458 6 1 4 5.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CNC(=O)c4cccnc4)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
CHEMBL5407403 195627 None 0 Human Functional pEC50 = 6.7 6.7 -10 4
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 458 6 1 4 5.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CNC(=O)c4cccnc4)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
162644880 179554 None 0 Human Functional pEC50 = 6.7 6.7 -2 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4740521 179554 None 0 Human Functional pEC50 = 6.7 6.7 -2 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162644880 179554 None 0 Human Functional pEC50 = 6.7 6.7 -2 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4740521 179554 None 0 Human Functional pEC50 = 6.7 6.7 -2 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162651091 180338 None 0 Human Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4750006 180338 None 0 Human Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
155520785 170612 None 0 Human Functional pEC50 = 5.7 5.7 -8 4
Agonist activity at delta-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at delta-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins
ChEMBL 1165 30 12 11 2.7 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmc.2019.01.003
CHEMBL4449491 170612 None 0 Human Functional pEC50 = 5.7 5.7 -8 4
Agonist activity at delta-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at delta-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins
ChEMBL 1165 30 12 11 2.7 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmc.2019.01.003
16048864 169055 None 0 Human Functional pEC50 = 8.7 8.7 1 3
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 512 7 1 2 6.9 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(Cl)cc5)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
CHEMBL438871 169055 None 0 Human Functional pEC50 = 8.7 8.7 1 3
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 512 7 1 2 6.9 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(Cl)cc5)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
CHEMBL294616 213353 None 0 Mouse Functional pEC50 = 8.7 8.7 -2 7
Agonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins 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 10.1016/j.ejmech.2013.09.031
172439036 195311 None 0 Human Functional pEC50 = 8.7 8.7 17 3
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assay
ChEMBL 338 5 1 3 4.2 Cc1ccc(C(CNC(=O)c2cc3ccccc3s2)N(C)C)cc1 10.1016/j.ejmech.2022.114728
CHEMBL5400535 195311 None 0 Human Functional pEC50 = 8.7 8.7 17 3
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assay
ChEMBL 338 5 1 3 4.2 Cc1ccc(C(CNC(=O)c2cc3ccccc3s2)N(C)C)cc1 10.1016/j.ejmech.2022.114728
CHEMBL2387213 212861 None 0 Human Functional pEC50 = 8.7 8.7 1 3
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](CCCCNC(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)O 10.1016/j.bmcl.2013.03.065
11849361 204279 None 0 Human Functional pEC50 = 8.7 8.7 -4 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 478 4 1 5 3.5 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5Cl)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
CHEMBL607016 204279 None 0 Human Functional pEC50 = 8.7 8.7 -4 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 478 4 1 5 3.5 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5Cl)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
44177669 61281 None 0 Human Functional pEC50 = 8.6 8.6 -5 5
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 1233 27 9 10 6.3 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)N(C)Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766205 61281 None 0 Human Functional pEC50 = 8.6 8.6 -5 5
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 1233 27 9 10 6.3 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)N(C)Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
72735390 106374 None 0 Human Functional pEC50 = 8.6 8.6 69 2
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 402 2 3 5 2.3 OCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL3139110 106374 None 0 Human Functional pEC50 = 8.6 8.6 69 2
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 402 2 3 5 2.3 OCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL4296735 106374 None 0 Human Functional pEC50 = 8.6 8.6 69 2
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 402 2 3 5 2.3 OCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
57390707 69353 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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]1Cc1cccc(O)c13 10.1016/j.bmc.2011.11.047
CHEMBL1929362 69353 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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]1Cc1cccc(O)c13 10.1016/j.bmc.2011.11.047
102270006 112914 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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
CHEMBL3309264 112914 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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
145953986 161453 None 0 Rat Functional pEC50 = 8.6 8.6 -199 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 484 11 6 6 0.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
CHEMBL4126050 161453 None 0 Rat Functional pEC50 = 8.6 8.6 -199 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 484 11 6 6 0.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
104787 1473 None 17 Human Functional pEC50 = 8.6 8.6 -2 4
Agonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assayAgonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay
ChEMBL None None None None 10.1016/j.ejmech.2021.113986
1608 1473 None 17 Human Functional pEC50 = 8.6 8.6 -2 4
Agonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assayAgonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay
ChEMBL None None None None 10.1016/j.ejmech.2021.113986
CHEMBL31421 1473 None 17 Human Functional pEC50 = 8.6 8.6 -2 4
Agonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assayAgonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay
ChEMBL None None None None 10.1016/j.ejmech.2021.113986
DB08861 1473 None 17 Human Functional pEC50 = 8.6 8.6 -2 4
Agonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assayAgonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay
ChEMBL None None None None 10.1016/j.ejmech.2021.113986
CHEMBL218763 211858 None 0 Human Functional pEC50 = 8.6 8.6 2 5
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](N)Cc1ccc(O)cc1 10.1021/jm050921q
81689720 111855 None 0 Human Functional pEC50 = 8.6 8.6 77 3
Agonist activity at delta-opioid receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at delta-opioid receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 396 2 1 3 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)C[C@@]1(C2)Cc1cc2ccccc2nc1C3 10.1016/j.bmcl.2014.04.098
CHEMBL3287467 111855 None 0 Human Functional pEC50 = 8.6 8.6 77 3
Agonist activity at delta-opioid receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at delta-opioid receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 396 2 1 3 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)C[C@@]1(C2)Cc1cc2ccccc2nc1C3 10.1016/j.bmcl.2014.04.098
CHEMBL2419537 212897 None 0 Human Functional pEC50 = 8.6 8.6 4 3
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)N[C@@H](C)C(=O)N[C@@H](CC(C)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.2013.06.065
44439876 93894 None 0 Human Functional pEC50 = 8.6 8.6 19 2
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 624 16 7 7 0.2 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)O 10.1016/j.bmcl.2007.01.092
CHEMBL247758 93894 None 0 Human Functional pEC50 = 8.6 8.6 19 2
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 624 16 7 7 0.2 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)O 10.1016/j.bmcl.2007.01.092
5487663 72864 None 12 Human Functional pEC50 = 8.6 8.6 -1 4
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 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.bmcl.2013.03.065
CHEMBL200199 72864 None 12 Human Functional pEC50 = 8.6 8.6 -1 4
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 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.bmcl.2013.03.065
16720650 138001 None 0 Human Functional pEC50 = 8.6 8.6 3 3
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 381 2 2 5 3.5 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CCC1)C2 10.1021/jm0701674
CHEMBL376355 138001 None 0 Human Functional pEC50 = 8.6 8.6 3 3
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 381 2 2 5 3.5 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CCC1)C2 10.1021/jm0701674
CHEMBL218763 211858 None 0 Human Functional pEC50 = 8.6 8.6 2 5
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](N)Cc1ccc(O)cc1 10.1021/jm050921q
25129135 172700 None 0 Human Functional pEC50 = 8.6 8.6 2 5
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 1073 27 10 11 2.9 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm800389v
CHEMBL448998 172700 None 0 Human Functional pEC50 = 8.6 8.6 2 5
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 1073 27 10 11 2.9 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm800389v
72735564 106380 None 0 Human Functional pEC50 = 8.6 8.6 53 3
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 430 4 2 5 3.4 CCOCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL3139135 106380 None 0 Human Functional pEC50 = 8.6 8.6 53 3
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 430 4 2 5 3.4 CCOCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
CHEMBL4296736 106380 None 0 Human Functional pEC50 = 8.6 8.6 53 3
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 430 4 2 5 3.4 CCOCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmc.2013.10.032
162676173 183557 None 0 Human Functional pEC50 = 8.6 8.6 -8 3
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 337 4 2 3 3.5 Oc1cccc([C@@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1 10.1039/d0md00104j
CHEMBL4798954 183557 None 0 Human Functional pEC50 = 8.6 8.6 -8 3
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 337 4 2 3 3.5 Oc1cccc([C@@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1 10.1039/d0md00104j
25129135 172700 None 0 Human Functional pEC50 = 8.6 8.6 2 5
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 1073 27 10 11 2.9 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm800389v
CHEMBL448998 172700 None 0 Human Functional pEC50 = 8.6 8.6 2 5
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 1073 27 10 11 2.9 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm800389v
45486035 199806 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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(CCc3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL569006 199806 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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(CCc3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2009.09.072
71229805 111015 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL3262089 111015 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
58443217 84209 None 0 Human Functional pEC50 = 8.6 8.6 -4 3
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 8 1 3 6.6 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1C 10.1016/j.bmcl.2012.10.081
CHEMBL2208352 84209 None 0 Human Functional pEC50 = 8.6 8.6 -4 3
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 8 1 3 6.6 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1C 10.1016/j.bmcl.2012.10.081
16083055 136712 None 0 Human Functional pEC50 = 8.6 8.6 1 3
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 732 10 3 7 5.8 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3 10.1021/jm0605785
CHEMBL373984 136712 None 0 Human Functional pEC50 = 8.6 8.6 1 3
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 732 10 3 7 5.8 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3 10.1021/jm0605785
50994381 57230 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
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 683 15 4 6 4.7 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649939 57230 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
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 683 15 4 6 4.7 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL2387329 212867 None 0 Human Functional pEC50 = 8.6 8.6 4 3
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](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
50994381 57230 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
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 683 15 4 6 4.7 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649939 57230 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
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 683 15 4 6 4.7 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
168282265 191121 None 0 Human Functional pEC50 = 8.5 8.5 -1 3
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 444 4 2 4 3.8 O=C(N[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2)c1ccccc1 10.1016/j.bmc.2021.116552
CHEMBL5186730 191121 None 0 Human Functional pEC50 = 8.5 8.5 -1 3
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 444 4 2 4 3.8 O=C(N[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2)c1ccccc1 10.1016/j.bmc.2021.116552
CHEMBL389652 214890 None 0 Human Functional pEC50 = 8.5 8.5 -12 5
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 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm061369n
CHEMBL389652 214890 None 0 Human Functional pEC50 = 8.5 8.5 -12 5
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 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm061369n
CHEMBL389652 214890 None 0 Human Functional pEC50 = 8.5 8.5 -12 5
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 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm800389v
CHEMBL294616 213353 None 0 Human Functional pEC50 = 8.5 8.5 -2 7
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 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/jm900604g
123924 3633 None 34 Human Functional pEC50 = 8.5 8.5 1 9
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
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 10.1016/j.bmcl.2009.09.072
1611 3633 None 34 Human Functional pEC50 = 8.5 8.5 1 9
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
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 10.1016/j.bmcl.2009.09.072
CHEMBL13470 3633 None 34 Human Functional pEC50 = 8.5 8.5 1 9
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
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 10.1016/j.bmcl.2009.09.072
71454964 81365 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 468 8 3 4 5.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(Cc1ccccc1)[C@@H](C)c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL2159118 81365 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 468 8 3 4 5.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(Cc1ccccc1)[C@@H](C)c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
16048866 94224 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 480 6 1 2 5.4 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(Br)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
CHEMBL249567 94224 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
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 480 6 1 2 5.4 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(Br)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
11269310 199031 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 390 4 1 3 4.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL563893 199031 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 390 4 1 3 4.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
11417954 286 None 27 Human Functional pEC50 = 7.7 7.7 - 1
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(C(=O)c1ccc(cc1)C1=CC2(CCNCC2)Oc2c1c(O)ccc2)CC 10.1021/jm8008986
9004 286 None 27 Human Functional pEC50 = 7.7 7.7 - 1
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(C(=O)c1ccc(cc1)C1=CC2(CCNCC2)Oc2c1c(O)ccc2)CC 10.1021/jm8008986
CHEMBL494480 286 None 27 Human Functional pEC50 = 7.7 7.7 - 1
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(C(=O)c1ccc(cc1)C1=CC2(CCNCC2)Oc2c1c(O)ccc2)CC 10.1021/jm8008986
CHEMBL5089740 217715 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
Antagonist activity at human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity at human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80-induced [3S]-GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(Cc1cc[nH]n1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/acs.jmedchem.1c02185
10808721 18543 None 0 Human Functional pEC50 = 7.7 7.7 831 2
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 363 5 2 3 3.9 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(N)c2)cc1 10.1021/jm000229p
CHEMBL127495 18543 None 0 Human Functional pEC50 = 7.7 7.7 831 2
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 363 5 2 3 3.9 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(N)c2)cc1 10.1021/jm000229p
44339521 9229 None 0 Human Functional pEC50 = 7.7 7.7 -10 2
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 459 8 0 4 5.1 COc1cccc2c1C13CCN(CC4CC4)[C@H](C2)[C@]1(OCCCc1ccccc1)CCC(=O)C3 10.1021/jm031126k
CHEMBL110640 9229 None 0 Human Functional pEC50 = 7.7 7.7 -10 2
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 459 8 0 4 5.1 COc1cccc2c1C13CCN(CC4CC4)[C@H](C2)[C@]1(OCCCc1ccccc1)CCC(=O)C3 10.1021/jm031126k
CHEMBL2371977 212630 None 0 Human Functional pEC50 = 7.7 7.7 -8 4
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](Cc1ccccc1)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
11849247 204961 None 0 Human Functional pEC50 = 7.7 7.7 -11 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 498 6 1 5 4.0 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm0604777
CHEMBL611400 204961 None 0 Human Functional pEC50 = 7.7 7.7 -11 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 498 6 1 5 4.0 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm0604777
162651091 180338 None 0 Human Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4750006 180338 None 0 Human Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
44254506 199168 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 374 2 1 3 3.9 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1CCCC1 10.1021/jm900773n
CHEMBL564922 199168 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 374 2 1 3 3.9 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1CCCC1 10.1021/jm900773n
25129434 187808 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 302 1 1 3 3.5 N#Cc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
CHEMBL495278 187808 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 302 1 1 3 3.5 N#Cc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
1121183 36685 None 8 Human Functional pEC50 = 5.7 5.7 -2 4
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 368 5 1 4 4.0 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2014.12.064
CHEMBL1449023 36685 None 8 Human Functional pEC50 = 5.7 5.7 -2 4
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 368 5 1 4 4.0 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2014.12.064
5113104 59162 None 4 Human Functional pEC50 = 4.7 4.7 -2 2
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 334 5 2 3 3.7 CN(C)C(CN=C(S)Nc1cccc(Cl)c1)c1cccnc1 nan
CHEMBL1698841 59162 None 4 Human Functional pEC50 = 4.7 4.7 -2 2
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 334 5 2 3 3.7 CN(C)C(CN=C(S)Nc1cccc(Cl)c1)c1cccnc1 nan
44573333 193307 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 310 3 1 4 2.7 CC(=O)N(c1ccccc1)C1CCN(c2cc(N)ccn2)CC1 10.1016/j.bmcl.2009.01.106
CHEMBL523358 193307 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 310 3 1 4 2.7 CC(=O)N(c1ccccc1)C1CCN(c2cc(N)ccn2)CC1 10.1016/j.bmcl.2009.01.106
172467290 196726 None 0 Human Functional pEC50 = 6.7 6.7 -4 2
Inverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assayInverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
ChEMBL 684 13 1 8 8.8 COc1cccc(Cn2nc(CNCc3cccc(OCc4ccccc4)c3)c3c4cc(OC)c(OC)cc4c(-c4ccccc4Cl)nc32)c1 10.1021/acs.jmedchem.3c00064
CHEMBL5430894 196726 None 0 Human Functional pEC50 = 6.7 6.7 -4 2
Inverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assayInverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
ChEMBL 684 13 1 8 8.8 COc1cccc(Cn2nc(CNCc3cccc(OCc4ccccc4)c3)c3c4cc(OC)c(OC)cc4c(-c4ccccc4Cl)nc32)c1 10.1021/acs.jmedchem.3c00064
16100411 137531 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
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 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@H](CC(=O)O)C(=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
CHEMBL375359 137531 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
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 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@H](CC(=O)O)C(=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
104787 1473 None 17 Human Functional pEC50 = 7.7 7.7 -2 4
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 None None None None 10.1016/j.bmcl.2007.01.092
1608 1473 None 17 Human Functional pEC50 = 7.7 7.7 -2 4
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 None None None None 10.1016/j.bmcl.2007.01.092
CHEMBL31421 1473 None 17 Human Functional pEC50 = 7.7 7.7 -2 4
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 None None None None 10.1016/j.bmcl.2007.01.092
DB08861 1473 None 17 Human Functional pEC50 = 7.7 7.7 -2 4
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 None None None None 10.1016/j.bmcl.2007.01.092
1639 2726 None 32 Human Functional pEC50 = 7.7 7.7 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2009.02.078
1765 2726 None 32 Human Functional pEC50 = 7.7 7.7 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2009.02.078
5360515 2726 None 32 Human Functional pEC50 = 7.7 7.7 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2009.02.078
5360515.0 2726 None 32 Human Functional pEC50 = 7.7 7.7 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2009.02.078
CHEMBL19019 2726 None 32 Human Functional pEC50 = 7.7 7.7 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2009.02.078
DB00704 2726 None 32 Human Functional pEC50 = 7.7 7.7 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2009.02.078
11337925 198183 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 378 4 1 3 4.2 CCN(CC)C(=O)c1ccc(C2CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL557121 198183 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 378 4 1 3 4.2 CCN(CC)C(=O)c1ccc(C2CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
44433399 89965 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
Agonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assay
ChEMBL 387 2 3 6 1.2 CO[C@]12C(O)C[C@@]3(C[C@@H]1[C@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1016/j.bmcl.2007.06.050
CHEMBL238017 89965 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
Agonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assay
ChEMBL 387 2 3 6 1.2 CO[C@]12C(O)C[C@@]3(C[C@@H]1[C@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1016/j.bmcl.2007.06.050
CHEMBL2371977 212630 None 0 Human Functional pEC50 = 7.7 7.7 -8 4
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](Cc1ccccc1)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
44268589 24286 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 391 8 0 3 5.0 C=CCN1CCC(N(c2ccccc2)c2ccc(C(=O)N(CC)CC)cc2)CC1 10.1016/j.bmcl.2004.02.051
CHEMBL13403 24286 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 391 8 0 3 5.0 C=CCN1CCC(N(c2ccccc2)c2ccc(C(=O)N(CC)CC)cc2)CC1 10.1016/j.bmcl.2004.02.051
155521726 170737 None 0 Rat Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting
ChEMBL 472 5 1 5 4.7 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(N)cc1)C2 10.1021/acs.jmedchem.9b00857
CHEMBL4451186 170737 None 0 Rat Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting
ChEMBL 472 5 1 5 4.7 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(N)cc1)C2 10.1021/acs.jmedchem.9b00857
168290224 192071 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
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 486 6 1 4 4.5 CN(C(=O)CCc1ccccc1)[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
CHEMBL5200992 192071 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
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 486 6 1 4 4.5 CN(C(=O)CCc1ccccc1)[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
10074239 9209 None 0 Human Functional pEC50 = 7.7 7.7 37 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 488 3 2 3 6.3 CN1CC[C@]23c4c5ccc(O)c4O[C@@]2(C)c2[nH]c4ccccc4c2C[C@@]3(C/C=C/c2ccccc2)C1C5 10.1021/jm030801n
CHEMBL110461 9209 None 0 Human Functional pEC50 = 7.7 7.7 37 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 488 3 2 3 6.3 CN1CC[C@]23c4c5ccc(O)c4O[C@@]2(C)c2[nH]c4ccccc4c2C[C@@]3(C/C=C/c2ccccc2)C1C5 10.1021/jm030801n
123924 3633 None 34 Human Functional pEC50 = 6.7 6.7 1 9
Agonist activity at human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
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/acsmedchemlett.8b00495
1611 3633 None 34 Human Functional pEC50 = 6.7 6.7 1 9
Agonist activity at human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
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/acsmedchemlett.8b00495
CHEMBL13470 3633 None 34 Human Functional pEC50 = 6.7 6.7 1 9
Agonist activity at human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
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/acsmedchemlett.8b00495
44433401 146624 None 0 Human Functional pEC50 = 6.7 6.7 -2 3
Agonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assay
ChEMBL 387 2 3 6 1.2 CO[C@]12CC(O)[C@@]3(C[C@@H]1[C@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1016/j.bmcl.2007.06.050
CHEMBL392269 146624 None 0 Human Functional pEC50 = 6.7 6.7 -2 3
Agonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assay
ChEMBL 387 2 3 6 1.2 CO[C@]12CC(O)[C@@]3(C[C@@H]1[C@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1016/j.bmcl.2007.06.050
9909743 35264 None 1 Mouse Functional pEC50 = 6.7 6.7 -19 4
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 414 5 1 3 5.6 CC(C)(C)c1ccc(C(c2cccc(O)c2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm980374r
CHEMBL143592 35264 None 1 Mouse Functional pEC50 = 6.7 6.7 -19 4
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 414 5 1 3 5.6 CC(C)(C)c1ccc(C(c2cccc(O)c2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm980374r
44337645 5414 None 0 Human Functional pEC50 = 6.7 6.7 4 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 440 1 2 3 5.4 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12CC(=C(C)C)[C@@H]3c1[nH]c3ccccc3c1C2 10.1021/jm030801n
CHEMBL107207 5414 None 0 Human Functional pEC50 = 6.7 6.7 4 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 440 1 2 3 5.4 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12CC(=C(C)C)[C@@H]3c1[nH]c3ccccc3c1C2 10.1021/jm030801n
89978537 159936 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
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 560 7 0 7 6.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CSc1nc3ccccc3s1)C2 nan
CHEMBL4106544 159936 None 0 Human Functional pEC50 = 6.7 6.7 -3 2
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 560 7 0 7 6.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CSc1nc3ccccc3s1)C2 nan
162649206 180089 None 0 Human Functional pEC50 = 6.7 6.7 -8 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4746919 180089 None 0 Human Functional pEC50 = 6.7 6.7 -8 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
44307356 205897 None 1 Human Functional pEC50 = 6.7 6.7 - 1
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 9 0 3 6.8 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL65772 205897 None 1 Human Functional pEC50 = 6.7 6.7 - 1
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 9 0 3 6.8 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.02.051
162649206 180089 None 0 Human Functional pEC50 = 6.7 6.7 -8 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4746919 180089 None 0 Human Functional pEC50 = 6.7 6.7 -8 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162659824 181316 None 0 Human Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4761246 181316 None 0 Human Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162659824 181316 None 0 Human Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4761246 181316 None 0 Human Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
25208095 191318 None 0 Human Functional pEC50 = 5.7 5.7 -1548 4
Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL518950 191318 None 0 Human Functional pEC50 = 5.7 5.7 -1548 4
Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
10255149 166412 None 0 Mouse Functional pEC50 = 7.7 7.7 -1 3
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 493 6 3 4 4.0 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
CHEMBL427214 166412 None 0 Mouse Functional pEC50 = 7.7 7.7 -1 3
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 493 6 3 4 4.0 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
10255149 166412 None 0 Human Functional pEC50 = 7.7 7.7 1 3
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 493 6 3 4 4.0 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL427214 166412 None 0 Human Functional pEC50 = 7.7 7.7 1 3
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 493 6 3 4 4.0 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL3759294 214690 None 0 Rat Functional pEC50 = 7.7 7.7 -4 2
Agonist activity at rat delta opioid receptor transfected in C6 cells by [35S]GTPgammaS binding assayAgonist activity at rat delta opioid receptor transfected in C6 cells by [35S]GTPgammaS binding assay
ChEMBL None None None CCCC[C@@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(N)=O)NC1=O 10.1016/j.ejmech.2015.11.028
CHEMBL3759831 214696 None 0 Rat Functional pEC50 = 7.7 7.7 -4 2
Agonist activity at rat delta opioid receptor transfected in C6 cells by [35S]GTPgammaS binding assayAgonist activity at rat delta opioid receptor transfected in C6 cells by [35S]GTPgammaS binding assay
ChEMBL None None None CCCC[C@@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC1=O 10.1016/j.ejmech.2015.11.028
66826776 160550 None 0 Human Functional pEC50 = 7.7 7.7 2 2
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 559 9 2 6 4.6 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1cccc(NC(N)=O)c1)C2 nan
CHEMBL4111717 160550 None 0 Human Functional pEC50 = 7.7 7.7 2 2
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 559 9 2 6 4.6 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1cccc(NC(N)=O)c1)C2 nan
89978695 160488 None 0 Human Functional pEC50 = 7.7 7.7 -5 3
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 505 8 1 6 4.0 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1C)[C@H]1Cc4ccc(OCCO)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
CHEMBL4111224 160488 None 0 Human Functional pEC50 = 7.7 7.7 -5 3
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 505 8 1 6 4.0 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1C)[C@H]1Cc4ccc(OCCO)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
CHEMBL206974 211641 None 0 Human Functional pEC50 = 7.6 7.6 -2 5
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
25129436 187610 None 1 Human Functional pEC50 = 6.7 6.7 - 1
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 321 2 2 3 3.3 O=C(O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
CHEMBL494266 187610 None 1 Human Functional pEC50 = 6.7 6.7 - 1
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 321 2 2 3 3.3 O=C(O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
25129433 187766 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 293 1 2 3 3.3 Oc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
CHEMBL495074 187766 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 293 1 2 3 3.3 Oc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
122182779 122383 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 406 2 3 4 3.1 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL3596365 122383 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 406 2 3 4 3.1 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL3598301 122383 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 406 2 3 4 3.1 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL134652 211190 None 0 Mouse Functional pEC50 = 5.7 5.7 1 3
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
44337839 108630 None 0 Human Functional pEC50 = 6.7 6.7 7 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 426 1 2 3 5.1 C/C=C1\C[C@@]23Cc4c([nH]c5ccccc45)[C@@H]1[C@@]21CCN(C)C3Cc2ccc(OC)c(O)c21 10.1021/jm030801n
CHEMBL320306 108630 None 0 Human Functional pEC50 = 6.7 6.7 7 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 426 1 2 3 5.1 C/C=C1\C[C@@]23Cc4c([nH]c5ccccc45)[C@@H]1[C@@]21CCN(C)C3Cc2ccc(OC)c(O)c21 10.1021/jm030801n
155520785 170612 None 0 Human Functional pEC50 = 5.7 5.7 -8 4
Agonist activity at delta-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at delta-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins
ChEMBL 1165 30 12 11 2.7 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmc.2019.01.003
CHEMBL4449491 170612 None 0 Human Functional pEC50 = 5.7 5.7 -8 4
Agonist activity at delta-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 minsAgonist activity at delta-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins
ChEMBL 1165 30 12 11 2.7 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmc.2019.01.003
162647042 179720 None 0 Human Functional pEC50 = 6.6 6.6 -3 4
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 1406 33 19 16 -0.6 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](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2Cc3ccc(O)cc3C[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4742666 179720 None 0 Human Functional pEC50 = 6.6 6.6 -3 4
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 1406 33 19 16 -0.6 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](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2Cc3ccc(O)cc3C[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
172467824 196974 None 0 Human Functional pEC50 = 6.6 6.6 -12 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5435869 196974 None 0 Human Functional pEC50 = 6.6 6.6 -12 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
10184592 206183 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 484 8 0 2 7.6 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCC2CCCCC2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL67734 206183 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 484 8 0 2 7.6 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCC2CCCCC2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
66828846 160639 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 520 8 0 7 4.7 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1c(C)noc1C)C2 nan
CHEMBL4112472 160639 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
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 520 8 0 7 4.7 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1c(C)noc1C)C2 nan
CHEMBL206974 211641 None 0 Human Functional pEC50 = 7.6 7.6 -2 5
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
16720747 137673 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 412 3 1 2 5.3 COc1ccc2c(c1)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3 10.1021/jm0701674
CHEMBL375503 137673 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 412 3 1 2 5.3 COc1ccc2c(c1)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3 10.1021/jm0701674
10692042 19466 None 0 Human Functional pEC50 = 7.6 7.6 954 2
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 394 6 1 3 5.1 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(SC)cc2)cc1 10.1021/jm000229p
CHEMBL129693 19466 None 0 Human Functional pEC50 = 7.6 7.6 954 2
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 394 6 1 3 5.1 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(SC)cc2)cc1 10.1021/jm000229p
172465082 196717 None 0 Human Functional pEC50 = 7.6 7.6 -1 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5430632 196717 None 0 Human Functional pEC50 = 7.6 7.6 -1 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
86711655 160124 None 0 Human Functional pEC50 = 6.6 6.6 -25 3
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 533 8 0 5 4.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](C[S+]([O-])Cc1ccccc1)C2 nan
CHEMBL4108066 160124 None 0 Human Functional pEC50 = 6.6 6.6 -25 3
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 533 8 0 5 4.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](C[S+]([O-])Cc1ccccc1)C2 nan
73351885 89678 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human delta opioid receptor transfected in CHOK1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor transfected in CHOK1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 348 1 1 6 3.0 COc1cc(O)c2c(c1)CC(=O)CCCC(=O)CCC[C@@H](C)OC2=O 10.1021/np300653d
CHEMBL2375656 89678 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human delta opioid receptor transfected in CHOK1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor transfected in CHOK1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 348 1 1 6 3.0 COc1cc(O)c2c(c1)CC(=O)CCCC(=O)CCC[C@@H](C)OC2=O 10.1021/np300653d
44573250 187524 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 437 4 1 6 2.5 CCOC(=O)N1CCN(C(=O)C2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)CC1 10.1016/j.bmcl.2009.01.106
CHEMBL493743 187524 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 437 4 1 6 2.5 CCOC(=O)N1CCN(C(=O)C2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)CC1 10.1016/j.bmcl.2009.01.106
CHEMBL246572 212961 None 0 Human Functional pEC50 = 7.6 7.6 14 2
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 None None None CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc2nc(N)sc2c1)C(=O)O 10.1016/j.bmcl.2007.01.092
122187725 123133 None 0 Human Functional pEC50 = 7.6 7.6 -4 3
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 691 11 6 5 4.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2015.06.030
CHEMBL3609621 123133 None 0 Human Functional pEC50 = 7.6 7.6 -4 3
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 691 11 6 5 4.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2015.06.030
10387038 9628 None 0 Human Functional pEC50 = 7.6 7.6 2 3
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 413 1 2 6 2.8 CN1CCC23c4c5ccc(O)c4OC2c2nc(-c4ccccc4)ncc2CC3(O)C1C5 10.1016/s0960-894x(99)00608-3
CHEMBL112656 9628 None 0 Human Functional pEC50 = 7.6 7.6 2 3
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 413 1 2 6 2.8 CN1CCC23c4c5ccc(O)c4OC2c2nc(-c4ccccc4)ncc2CC3(O)C1C5 10.1016/s0960-894x(99)00608-3
122182789 122379 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 418 2 2 5 3.2 Oc1ccc2c3c1O[C@H]1c4nc5ccccc5cc4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL3596370 122379 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 418 2 2 5 3.2 Oc1ccc2c3c1O[C@H]1c4nc5ccccc5cc4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL3598212 122379 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 418 2 2 5 3.2 Oc1ccc2c3c1O[C@H]1c4nc5ccccc5cc4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314 10.1016/j.bmcl.2015.05.038
44254584 197756 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 390 2 1 4 3.1 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1CCOCC1 10.1021/jm900773n
CHEMBL551414 197756 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 390 2 1 4 3.1 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1CCOCC1 10.1021/jm900773n
145963106 161731 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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 1024 12 10 14 -0.7 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)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
CHEMBL4130069 161731 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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 1024 12 10 14 -0.7 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)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
145963106 161731 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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 1024 12 10 14 -0.7 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)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
CHEMBL4130069 161731 None 0 Human Functional pEC50 = 6.6 6.6 1 3
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 1024 12 10 14 -0.7 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)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
162649599 180271 None 0 Human Functional pEC50 = 6.6 6.6 -134 4
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 1380 37 16 16 1.9 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](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4749016 180271 None 0 Human Functional pEC50 = 6.6 6.6 -134 4
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 1380 37 16 16 1.9 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](CCCCN)CC(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL3609615 214289 None 0 Human Functional pEC50 = 7.6 7.6 1 3
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 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)NCC(=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
127051733 141125 None 0 Rat Functional pEC50 = 7.6 7.6 -2 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 499 7 3 4 4.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C(C)C)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
CHEMBL3824042 141125 None 0 Rat Functional pEC50 = 7.6 7.6 -2 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 499 7 3 4 4.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C(C)C)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
9932852 123238 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 438 5 3 4 4.0 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1021/jm030548r
CHEMBL361274 123238 None 0 Human Functional pEC50 = 7.6 7.6 -1 3
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 438 5 3 4 4.0 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1021/jm030548r
9949205 9495 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 325 0 3 5 1.0 CN1CCC23c4c5ccc(O)c4OC2c2n[nH]cc2CC3(O)C1C5 10.1016/s0960-894x(99)00608-3
CHEMBL112035 9495 None 0 Human Functional pEC50 = 7.6 7.6 -1 2
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 325 0 3 5 1.0 CN1CCC23c4c5ccc(O)c4OC2c2n[nH]cc2CC3(O)C1C5 10.1016/s0960-894x(99)00608-3
44408526 137032 None 0 Human Functional pEC50 = 7.6 7.6 -1 5
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 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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
CHEMBL374325 137032 None 0 Human Functional pEC50 = 7.6 7.6 -1 5
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 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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
102270008 112920 None 0 Human Functional pEC50 = 7.6 7.6 3 2
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 368 0 2 5 1.3 CN1C(=O)CCC2=C1[C@@H]1Oc3c(O)ccc4c3[C@@]13CCN(C)[C@H](C4)[C@]3(O)C2 10.1016/j.bmc.2014.05.065
CHEMBL3309506 112920 None 0 Human Functional pEC50 = 7.6 7.6 3 2
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 368 0 2 5 1.3 CN1C(=O)CCC2=C1[C@@H]1Oc3c(O)ccc4c3[C@@]13CCN(C)[C@H](C4)[C@]3(O)C2 10.1016/j.bmc.2014.05.065
10714960 18223 None 0 Human Functional pEC50 = 7.6 7.6 489 3
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 382 5 1 2 5.0 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(Cl)cc2)cc1 10.1021/jm000229p
CHEMBL127007 18223 None 0 Human Functional pEC50 = 7.6 7.6 489 3
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 382 5 1 2 5.0 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(Cl)cc2)cc1 10.1021/jm000229p
45485826 200160 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 4 4.1 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(C)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL571324 200160 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 4 4.1 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(C)CC2)cc1 10.1016/j.bmcl.2009.09.072
50994529 57236 None 0 Human Functional pEC50 = 7.6 7.6 -6 3
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 675 12 4 6 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649945 57236 None 0 Human Functional pEC50 = 7.6 7.6 -6 3
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 675 12 4 6 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
156015144 178373 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 1294 16 13 19 -0.2 Cc1cc(=O)oc2cc(NC(=O)CCN3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)ccc12 10.1021/acsmedchemlett.9b00569
CHEMBL4641588 178373 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 1294 16 13 19 -0.2 Cc1cc(=O)oc2cc(NC(=O)CCN3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)ccc12 10.1021/acsmedchemlett.9b00569
CHEMBL4650776 178373 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 1294 16 13 19 -0.2 Cc1cc(=O)oc2cc(NC(=O)CCN3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)ccc12 10.1021/acsmedchemlett.9b00569
71819525 92088 None 0 Human Functional pEC50 = 5.6 5.6 -3 5
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 329 2 0 4 2.6 COc1ccc2c3c1O[C@H]1[C@@H](OC)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
CHEMBL2418743 92088 None 0 Human Functional pEC50 = 5.6 5.6 -3 5
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 329 2 0 4 2.6 COc1ccc2c3c1O[C@H]1[C@@H](OC)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
137630442 161160 None 0 Rat Functional pEC50 = 6.6 6.6 -131 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 4 2 3 4.0 Oc1cccc([C@@]23CCC[C@@H]([C@@H]2O)N(C/C=C/c2ccccc2)CC3)c1 10.1016/j.bmc.2017.02.064
CHEMBL4078283 161160 None 0 Rat Functional pEC50 = 6.6 6.6 -131 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 4 2 3 4.0 Oc1cccc([C@@]23CCC[C@@H]([C@@H]2O)N(C/C=C/c2ccccc2)CC3)c1 10.1016/j.bmc.2017.02.064
CHEMBL4116647 161160 None 0 Rat Functional pEC50 = 6.6 6.6 -131 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 4 2 3 4.0 Oc1cccc([C@@]23CCC[C@@H]([C@@H]2O)N(C/C=C/c2ccccc2)CC3)c1 10.1016/j.bmc.2017.02.064
11191431 67769 None 0 Human Functional pEC50 = 5.6 5.6 -5 3
Stimulation of [35S]-GTP gammaS binding to Opioid receptor delta 1 expressed in CHO cells; ND = Not determinedStimulation of [35S]-GTP gammaS binding to Opioid receptor delta 1 expressed in CHO cells; ND = Not determined
ChEMBL 509 4 1 8 4.7 COC(=O)[C@@H]1C[C@H](OC(=O)Nc2ccccc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C 10.1021/jm048963m
CHEMBL190785 67769 None 0 Human Functional pEC50 = 5.6 5.6 -5 3
Stimulation of [35S]-GTP gammaS binding to Opioid receptor delta 1 expressed in CHO cells; ND = Not determinedStimulation of [35S]-GTP gammaS binding to Opioid receptor delta 1 expressed in CHO cells; ND = Not determined
ChEMBL 509 4 1 8 4.7 COC(=O)[C@@H]1C[C@H](OC(=O)Nc2ccccc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@]21C 10.1021/jm048963m
16326480 59583 None 4 Human Functional pEC50 = 4.6 4.6 -18 2
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 332 8 1 4 3.1 COc1ccc(C(CNC(=O)CCc2ccsc2)N(C)C)cc1 nan
CHEMBL1717557 59583 None 4 Human Functional pEC50 = 4.6 4.6 -18 2
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 332 8 1 4 3.1 COc1ccc(C(CNC(=O)CCc2ccsc2)N(C)C)cc1 nan
50994529 57236 None 0 Human Functional pEC50 = 7.6 7.6 -6 3
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 675 12 4 6 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649945 57236 None 0 Human Functional pEC50 = 7.6 7.6 -6 3
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 675 12 4 6 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
11406708 198206 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 392 4 2 4 3.8 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1O 10.1021/jm900773n
CHEMBL557458 198206 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 392 4 2 4 3.8 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1O 10.1021/jm900773n
44406350 73043 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 450 5 0 5 6.1 c1ccc(Cn2ccnc2C2(c3ccccc3)CCN(c3nc4ccccc4s3)CC2)cc1 10.1016/j.bmcl.2005.09.025
CHEMBL200940 73043 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 450 5 0 5 6.1 c1ccc(Cn2ccnc2C2(c3ccccc3)CCN(c3nc4ccccc4s3)CC2)cc1 10.1016/j.bmcl.2005.09.025
44408526 137032 None 0 Human Functional pEC50 = 7.6 7.6 -1 5
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 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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
CHEMBL374325 137032 None 0 Human Functional pEC50 = 7.6 7.6 -1 5
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 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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
145961135 161662 None 0 Rat Functional pEC50 = 7.6 7.6 -380 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 636 15 9 7 -0.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(C(F)(F)F)cc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4128945 161662 None 0 Rat Functional pEC50 = 7.6 7.6 -380 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 636 15 9 7 -0.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(C(F)(F)F)cc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
145961165 161703 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 1090 12 12 16 0.2 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)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
CHEMBL4129668 161703 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 1090 12 12 16 0.2 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)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
CHEMBL5077166 218016 None 0 Human Functional pEC50 = 7.6 7.6 -7 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc[nH]1 10.1021/acs.jmedchem.2c00087
CHEMBL5095532 218016 None 0 Human Functional pEC50 = 7.6 7.6 -7 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc[nH]1 10.1021/acs.jmedchem.2c00087
145961165 161703 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 1090 12 12 16 0.2 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)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
CHEMBL4129668 161703 None 0 Human Functional pEC50 = 7.6 7.6 3 3
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 1090 12 12 16 0.2 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)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
104787 1473 None 17 Human Functional pEC50 = 7.6 7.6 -2 4
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None None 10.1016/j.ejmech.2015.12.012
1608 1473 None 17 Human Functional pEC50 = 7.6 7.6 -2 4
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None None 10.1016/j.ejmech.2015.12.012
CHEMBL31421 1473 None 17 Human Functional pEC50 = 7.6 7.6 -2 4
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None None 10.1016/j.ejmech.2015.12.012
DB08861 1473 None 17 Human Functional pEC50 = 7.6 7.6 -2 4
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None None 10.1016/j.ejmech.2015.12.012
44408524 155795 None 0 Human Functional pEC50 = 7.6 7.6 -2 5
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 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL405192 155795 None 0 Human Functional pEC50 = 7.6 7.6 -2 5
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 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
25217787 187714 None 4 Human Functional pEC50 = 6.6 6.6 - 1
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 295 3 1 4 2.8 CC(=O)C1(c2ccccc2)CCN(c2cc(N)ccn2)CC1 10.1016/j.bmcl.2009.01.106
CHEMBL494771 187714 None 4 Human Functional pEC50 = 6.6 6.6 - 1
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 295 3 1 4 2.8 CC(=O)C1(c2ccccc2)CCN(c2cc(N)ccn2)CC1 10.1016/j.bmcl.2009.01.106
1177949 34298 None 10 Human Functional pEC50 = 4.6 4.6 -2 3
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 429 6 0 7 5.3 COc1ccc2c(Cl)c(-c3nnc(SCC(=O)c4ccccc4)n3C)sc2c1 nan
CHEMBL1426979 34298 None 10 Human Functional pEC50 = 4.6 4.6 -2 3
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 429 6 0 7 5.3 COc1ccc2c(Cl)c(-c3nnc(SCC(=O)c4ccccc4)n3C)sc2c1 nan
5113106 59206 None 4 Human Functional pEC50 = 4.6 4.6 -7 2
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 334 5 2 3 3.7 CN(C)C(CN=C(S)Nc1ccccc1Cl)c1cccnc1 nan
CHEMBL1700847 59206 None 4 Human Functional pEC50 = 4.6 4.6 -7 2
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 334 5 2 3 3.7 CN(C)C(CN=C(S)Nc1ccccc1Cl)c1cccnc1 nan
145961131 161657 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 0.8 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)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1016/j.bmc.2018.05.045
CHEMBL4128853 161657 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 0.8 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)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1016/j.bmc.2018.05.045
145961131 161657 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 0.8 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)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1016/j.bmc.2018.05.045
CHEMBL4128853 161657 None 0 Human Functional pEC50 = 6.6 6.6 -1 3
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 0.8 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)N2CCN(CC2)C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1016/j.bmc.2018.05.045
4881395 59427 None 2 Human Functional pEC50 = 4.6 4.6 -1 2
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 377 6 1 4 2.9 COc1ccc(C(CNC(=O)c2cncc(Br)c2)N(C)C)cc1 nan
CHEMBL1709988 59427 None 2 Human Functional pEC50 = 4.6 4.6 -1 2
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 377 6 1 4 2.9 COc1ccc(C(CNC(=O)c2cncc(Br)c2)N(C)C)cc1 nan
16730814 187397 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 350 2 1 4 2.8 CN(C)C(=O)[C@H]1CC2(CCN(c3cc(N)ccn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.01.106
CHEMBL492908 187397 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 350 2 1 4 2.8 CN(C)C(=O)[C@H]1CC2(CCN(c3cc(N)ccn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.01.106
CHEMBL2419544 212904 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
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 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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
10206991 205493 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 496 8 0 2 7.0 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccc(F)cc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL63400 205493 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 496 8 0 2 7.0 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccc(F)cc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
16224612 206089 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 418 6 0 3 5.2 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3C)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL67157 206089 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 418 6 0 3 5.2 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3C)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2004.02.051
44408524 155795 None 0 Human Functional pEC50 = 7.6 7.6 -2 5
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 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL405192 155795 None 0 Human Functional pEC50 = 7.6 7.6 -2 5
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 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
44408632 158329 None 0 Human Functional pEC50 = 7.6 7.6 4 5
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 1212 31 12 15 3.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL408832 158329 None 0 Human Functional pEC50 = 7.6 7.6 4 5
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 1212 31 12 15 3.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
44233184 194880 None 0 Human Functional pEC50 = 7.6 7.6 -11 5
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 1343 32 15 16 1.7 CCCC[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](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=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/jm900473p
CHEMBL538131 194880 None 0 Human Functional pEC50 = 7.6 7.6 -11 5
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 1343 32 15 16 1.7 CCCC[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](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=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/jm900473p
45271306 198128 None 0 Human Functional pEC50 = 7.6 7.6 -89 5
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 1438 33 14 16 3.1 CCCC[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](CC(C)C)C(=O)N[C@@H](CO[C@@H]1O[C@H](CC)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
CHEMBL556537 198128 None 0 Human Functional pEC50 = 7.6 7.6 -89 5
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 1438 33 14 16 3.1 CCCC[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](CC(C)C)C(=O)N[C@@H](CO[C@@H]1O[C@H](CC)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
44408632 158329 None 0 Human Functional pEC50 = 7.6 7.6 4 5
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 1212 31 12 15 3.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL408832 158329 None 0 Human Functional pEC50 = 7.6 7.6 4 5
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 1212 31 12 15 3.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
172449219 195759 None 0 Human Functional pEC50 = 7.6 7.6 1 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1122 24 13 13 -1.2 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5410237 195759 None 0 Human Functional pEC50 = 7.6 7.6 1 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1122 24 13 13 -1.2 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
44254061 198596 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 377 4 1 4 3.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)nc1 10.1021/jm900773n
CHEMBL561138 198596 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 377 4 1 4 3.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)nc1 10.1021/jm900773n
127050830 141141 None 0 Rat Functional pEC50 = 6.6 6.6 -177 3
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 486 8 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(CC(N)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
CHEMBL3824309 141141 None 0 Rat Functional pEC50 = 6.6 6.6 -177 3
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 486 8 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(CC(N)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
66826826 160081 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 446 5 1 5 3.9 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(N)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
CHEMBL4107680 160081 None 0 Human Functional pEC50 = 6.6 6.6 -6 3
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 446 5 1 5 3.9 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(N)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
44573446 187563 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 400 4 1 7 3.1 Nc1ccnc(N2CCC(n3c(=O)n(Cc4ccccc4)c4cccnc43)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL493973 187563 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 400 4 1 7 3.1 Nc1ccnc(N2CCC(n3c(=O)n(Cc4ccccc4)c4cccnc43)CC2)c1 10.1016/j.bmcl.2009.01.106
44255041 198109 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 362 4 1 3 3.7 CCN(CC)C(=O)c1ccc(C2=CC3(CCNC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL556439 198109 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 362 4 1 3 3.7 CCN(CC)C(=O)c1ccc(C2=CC3(CCNC3)Oc3ccccc32)cc1 10.1021/jm900773n
45271306 198128 None 0 Human Functional pEC50 = 7.6 7.6 -89 5
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 1438 33 14 16 3.1 CCCC[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](CC(C)C)C(=O)N[C@@H](CO[C@@H]1O[C@H](CC)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
CHEMBL556537 198128 None 0 Human Functional pEC50 = 7.6 7.6 -89 5
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 1438 33 14 16 3.1 CCCC[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](CC(C)C)C(=O)N[C@@H](CO[C@@H]1O[C@H](CC)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
71459993 79654 None 0 Human Functional pEC50 = 7.6 7.6 194 2
Effective concentration for agonistic activity towards delta opioid receptor was determined by [35S]GTP-gamma-S functional assayEffective concentration for agonistic activity towards delta opioid receptor was determined by [35S]GTP-gamma-S functional assay
ChEMBL 554 5 3 5 3.5 COc1c(Br)cc2c(c1Br)CN(C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)[C@H](C(=O)O)C2 10.1016/s0960-894x(99)00652-6
CHEMBL2114981 79654 None 0 Human Functional pEC50 = 7.6 7.6 194 2
Effective concentration for agonistic activity towards delta opioid receptor was determined by [35S]GTP-gamma-S functional assayEffective concentration for agonistic activity towards delta opioid receptor was determined by [35S]GTP-gamma-S functional assay
ChEMBL 554 5 3 5 3.5 COc1c(Br)cc2c(c1Br)CN(C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)[C@H](C(=O)O)C2 10.1016/s0960-894x(99)00652-6
CHEMBL5086601 217528 None 0 Human Functional pEC50 = 7.6 7.6 1 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
CHEMBL5086601 217528 None 0 Human Functional pEC50 = 7.6 7.6 1 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
10452891 18004 None 0 Human Functional pEC50 = 7.6 7.6 251 3
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 388 7 0 2 5.3 C=CCN1CCC(=C(c2ccccc2)c2ccc(C(=O)N(CC)CC)cc2)CC1 10.1021/jm000229p
CHEMBL126255 18004 None 0 Human Functional pEC50 = 7.6 7.6 251 3
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 388 7 0 2 5.3 C=CCN1CCC(=C(c2ccccc2)c2ccc(C(=O)N(CC)CC)cc2)CC1 10.1021/jm000229p
70693567 78406 None 0 Human Functional pEC50 = 7.6 7.6 -14 3
Activity was evaluated in human delta opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human delta opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay
ChEMBL 395 0 1 4 4.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@]24CC[C@@]3(C[C@H]2C(C)(C)C(C)(C)O4)C1C5 10.1016/s0960-894x(99)00085-2
CHEMBL2110315 78406 None 0 Human Functional pEC50 = 7.6 7.6 -14 3
Activity was evaluated in human delta opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human delta opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay
ChEMBL 395 0 1 4 4.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@]24CC[C@@]3(C[C@H]2C(C)(C)C(C)(C)O4)C1C5 10.1016/s0960-894x(99)00085-2
CHEMBL218327 211853 None 0 Human Functional pEC50 = 7.5 7.5 -2 5
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](N)Cc1ccc(O)cc1 10.1021/jm050921q
23634920 88540 None 0 Human Functional pEC50 = 7.5 7.5 -1 3
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 756 18 8 9 0.4 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)NC1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
CHEMBL235107 88540 None 0 Human Functional pEC50 = 7.5 7.5 -1 3
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 756 18 8 9 0.4 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)NC1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
CHEMBL3609617 214291 None 0 Human Functional pEC50 = 6.6 6.6 -12 3
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 None None None C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=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
118725850 117239 None 0 Human Functional pEC50 = 5.6 5.6 -354 3
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 323 5 2 4 2.7 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc[nH]1 10.1016/j.bmcl.2014.12.064
CHEMBL3394000 117239 None 0 Human Functional pEC50 = 5.6 5.6 -354 3
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 323 5 2 4 2.7 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc[nH]1 10.1016/j.bmcl.2014.12.064
66553195 93198 None 26 Human Functional pEC50 = 5.6 5.6 -380 5
Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay
ChEMBL 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 10.1021/jm4010829
66553195.0 93198 None 26 Human Functional pEC50 = 5.6 5.6 -380 5
Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay
ChEMBL 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 10.1021/jm4010829
CHEMBL2443262 93198 None 26 Human Functional pEC50 = 5.6 5.6 -380 5
Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay
ChEMBL 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 10.1021/jm4010829
DB14881 93198 None 26 Human Functional pEC50 = 5.6 5.6 -380 5
Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay
ChEMBL 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 10.1021/jm4010829
172454342 196099 None 0 Human Functional pEC50 = 5.6 5.6 -301 4
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 448 6 1 5 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CNC(=O)c4cnco4)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
CHEMBL5416899 196099 None 0 Human Functional pEC50 = 5.6 5.6 -301 4
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 448 6 1 5 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CNC(=O)c4cnco4)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
134578494 196222 None 0 Human Functional pEC50 = 6.5 6.5 -16 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 425 6 1 4 5.7 CCOC(=O)NCc1cc2ccccc2n1C1CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1 10.1016/j.bmc.2023.117421
CHEMBL5419235 196222 None 0 Human Functional pEC50 = 6.5 6.5 -16 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 425 6 1 4 5.7 CCOC(=O)NCc1cc2ccccc2n1C1CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1 10.1016/j.bmc.2023.117421
162644535 179524 None 0 Human Functional pEC50 = 6.5 6.5 5 2
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 500 10 1 5 4.5 CCC(=O)N(Cc1ccncc1)C1(C(=O)Nc2ccc(OC)cc2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
CHEMBL4740220 179524 None 0 Human Functional pEC50 = 6.5 6.5 5 2
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 500 10 1 5 4.5 CCC(=O)N(Cc1ccncc1)C1(C(=O)Nc2ccc(OC)cc2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
CHEMBL218327 211853 None 0 Human Functional pEC50 = 7.5 7.5 -2 5
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](N)Cc1ccc(O)cc1 10.1021/jm050921q
23634920 88540 None 0 Human Functional pEC50 = 7.5 7.5 -1 3
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 756 18 8 9 0.4 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)NC1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
CHEMBL235107 88540 None 0 Human Functional pEC50 = 7.5 7.5 -1 3
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 756 18 8 9 0.4 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)NC1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
CHEMBL218433 211855 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None Cc1cc(C[C@H](N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)cc(C)c1O 10.1021/jm060998u
172449219 195759 None 0 Human Functional pEC50 = 7.5 7.5 1 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1122 24 13 13 -1.2 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5410237 195759 None 0 Human Functional pEC50 = 7.5 7.5 1 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1122 24 13 13 -1.2 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCC/C=C/C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
663898 48042 None 11 Human Functional pEC50 = 4.5 4.5 -1 2
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 409 4 0 5 4.0 O=C(c1sc2ccccc2c1Cl)N(Cc1ccco1)C1CCS(=O)(=O)C1 nan
CHEMBL1550356 48042 None 11 Human Functional pEC50 = 4.5 4.5 -1 2
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 409 4 0 5 4.0 O=C(c1sc2ccccc2c1Cl)N(Cc1ccco1)C1CCS(=O)(=O)C1 nan
5928348 72971 None 1 Human Functional pEC50 = 4.5 4.5 1 2
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 310 3 2 4 4.3 C/C(=N/Nc1ccnc2cc(Cl)ccc12)c1ccc(N)cc1 nan
CHEMBL2005743 72971 None 1 Human Functional pEC50 = 4.5 4.5 1 2
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 310 3 2 4 4.3 C/C(=N/Nc1ccnc2cc(Cl)ccc12)c1ccc(N)cc1 nan
11754240 76002 None 0 Mouse Functional pEC50 = 8.5 8.5 - 1
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 465 6 3 4 3.4 NC(=O)c1ccc(C[C@H](N)C(=O)N2Cc3ccccc3C[C@H]2c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/j.bmcl.2006.01.082
CHEMBL205388 76002 None 0 Mouse Functional pEC50 = 8.5 8.5 - 1
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 465 6 3 4 3.4 NC(=O)c1ccc(C[C@H](N)C(=O)N2Cc3ccccc3C[C@H]2c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/j.bmcl.2006.01.082
44573445 187562 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 416 4 1 8 3.0 COc1ccc(-n2c(=O)n(C3CCN(c4cc(N)ccn4)CC3)c3ncccc32)cc1 10.1016/j.bmcl.2009.01.106
CHEMBL493972 187562 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 416 4 1 8 3.0 COc1ccc(-n2c(=O)n(C3CCN(c4cc(N)ccn4)CC3)c3ncccc32)cc1 10.1016/j.bmcl.2009.01.106
16006949 138763 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 478 7 1 2 6.3 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
CHEMBL377789 138763 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 478 7 1 2 6.3 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2007.09.082
117705986 155934 None 0 Human Functional pEC50 = 8.5 8.5 32 2
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 458 3 1 4 4.0 CC(C)CN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1 10.1016/j.bmcl.2017.04.059
CHEMBL4060073 155934 None 0 Human Functional pEC50 = 8.5 8.5 32 2
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 458 3 1 4 4.0 CC(C)CN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1 10.1016/j.bmcl.2017.04.059
102270003 112921 None 0 Human Functional pEC50 = 8.5 8.5 1 2
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 444 2 2 5 2.9 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2C2=C(CCC(=O)N2Cc2ccccc2)C[C@@]3(O)[C@H]1C5 10.1016/j.bmc.2014.05.065
CHEMBL3309507 112921 None 0 Human Functional pEC50 = 8.5 8.5 1 2
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 444 2 2 5 2.9 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2C2=C(CCC(=O)N2Cc2ccccc2)C[C@@]3(O)[C@H]1C5 10.1016/j.bmc.2014.05.065
16006949 138763 None 0 Human Functional pEC50 = 8.5 8.5 1 3
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTP-gamma-S bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTP-gamma-S binding
ChEMBL 478 7 1 2 6.3 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1021/jm060278n
CHEMBL377789 138763 None 0 Human Functional pEC50 = 8.5 8.5 1 3
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTP-gamma-S bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTP-gamma-S binding
ChEMBL 478 7 1 2 6.3 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1021/jm060278n
11269707 206221 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 404 5 1 3 4.9 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3C)c2cccc(O)c2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL67996 206221 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 404 5 1 3 4.9 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3C)c2cccc(O)c2)cc1 10.1016/j.bmcl.2004.02.051
11016572 188485 None 0 Mouse Functional pEC50 = 8.5 8.5 - 1
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 500 7 4 5 2.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCC(=O)Nc1ccccc1 10.1021/jm010449i
CHEMBL501451 188485 None 0 Mouse Functional pEC50 = 8.5 8.5 - 1
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 500 7 4 5 2.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCC(=O)Nc1ccccc1 10.1021/jm010449i
CHEMBL389652 214890 None 0 Human Functional pEC50 = 8.5 8.5 -12 5
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 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm800389v
49863731 15336 None 0 Human Functional pEC50 = 8.5 8.5 -269 5
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
CHEMBL1214024 15336 None 0 Human Functional pEC50 = 8.5 8.5 -269 5
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
127032213 139055 None 0 Human Functional pEC50 = 8.5 8.5 17 2
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
CHEMBL3785265 139055 None 0 Human Functional pEC50 = 8.5 8.5 17 2
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
10001960 117528 None 0 Human Functional pEC50 = 8.5 8.5 1071 3
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 416 5 1 2 5.4 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm000229p
CHEMBL339898 117528 None 0 Human Functional pEC50 = 8.5 8.5 1071 3
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 416 5 1 2 5.4 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm000229p
71680923 91053 None 0 Human Functional pEC50 = 8.5 8.5 -5 2
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 445 4 2 6 2.4 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1cccnc1 10.1021/jm4012214
CHEMBL2397021 91053 None 0 Human Functional pEC50 = 8.5 8.5 -5 2
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 445 4 2 6 2.4 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1cccnc1 10.1021/jm4012214
CHEMBL3086747 91053 None 0 Human Functional pEC50 = 8.5 8.5 -5 2
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 445 4 2 6 2.4 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1cccnc1 10.1021/jm4012214
49863731 15336 None 0 Human Functional pEC50 = 8.5 8.5 -269 5
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
CHEMBL1214024 15336 None 0 Human Functional pEC50 = 8.5 8.5 -269 5
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
44421399 84705 None 0 Human Functional pEC50 = 8.5 8.5 4 2
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 446 3 2 5 3.8 CCn1c2c(c3c1[C@@H]1Oc4c(O)ccc5c4[C@@]14CCN(CC1CC1)C(C5)[C@]4(O)C3)CCCC2 10.1021/jm040817t
CHEMBL222486 84705 None 0 Human Functional pEC50 = 8.5 8.5 4 2
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 446 3 2 5 3.8 CCn1c2c(c3c1[C@@H]1Oc4c(O)ccc5c4[C@@]14CCN(CC1CC1)C(C5)[C@]4(O)C3)CCCC2 10.1021/jm040817t
71456258 79210 None 0 Human Functional pEC50 = 8.5 8.5 16 3
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 457 4 3 4 4.1 CCCCC(=O)N[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm021073r
CHEMBL2113381 79210 None 0 Human Functional pEC50 = 8.5 8.5 16 3
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 457 4 3 4 4.1 CCCCC(=O)N[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm021073r
72735759 106375 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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
CHEMBL3139111 106375 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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
CHEMBL4296725 106375 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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
45486032 201489 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 435 9 1 4 5.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCC3CC3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL585900 201489 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 435 9 1 4 5.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCC3CC3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL3608939 214288 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 None None None C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)NCC(=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
44439905 93895 None 0 Human Functional pEC50 = 8.5 8.5 72 2
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 741 20 10 10 -1.9 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1016/j.bmcl.2007.01.092
CHEMBL247760 93895 None 0 Human Functional pEC50 = 8.5 8.5 72 2
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 741 20 10 10 -1.9 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1016/j.bmcl.2007.01.092
CHEMBL385583 214816 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None Cc1cc(C[C@H](N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(N)=O)cc(C)c1O 10.1021/jm060998u
123924 3633 None 34 Human Functional pEC50 = 8.4 8.4 1 9
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 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/jm000229p
1611 3633 None 34 Human Functional pEC50 = 8.4 8.4 1 9
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 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/jm000229p
CHEMBL13470 3633 None 34 Human Functional pEC50 = 8.4 8.4 1 9
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 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/jm000229p
44592015 189350 None 0 Human Functional pEC50 = 8.4 8.4 -10 3
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 386 3 4 5 1.4 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3 10.1016/j.bmcl.2009.02.078
CHEMBL511645 189350 None 0 Human Functional pEC50 = 8.4 8.4 -10 3
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 386 3 4 5 1.4 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3 10.1016/j.bmcl.2009.02.078
155522441 176598 None 0 Rat Functional pEC50 = 8.4 8.4 -4 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 537 7 3 5 5.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4451910 176598 None 0 Rat Functional pEC50 = 8.4 8.4 -4 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 537 7 3 5 5.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4596711 176598 None 0 Rat Functional pEC50 = 8.4 8.4 -4 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 537 7 3 5 5.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
45486062 199786 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 6.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CC(C)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL568865 199786 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 6.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CC(C)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
168273055 190392 None 0 Human Functional pEC50 = 8.4 8.4 1 3
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 5 2 4 3.7 O=C(Cc1ccccc1)N[C@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
CHEMBL5175717 190392 None 0 Human Functional pEC50 = 8.4 8.4 1 3
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 5 2 4 3.7 O=C(Cc1ccccc1)N[C@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
44421400 84727 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
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 472 4 2 5 4.2 Oc1ccc2c3c1O[C@H]1c4c(c5c(n4CC4CC4)CCCC5)C[C@@]4(O)C(C2)N(CC2CC2)CC[C@]314 10.1021/jm040817t
CHEMBL222597 84727 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
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 472 4 2 5 4.2 Oc1ccc2c3c1O[C@H]1c4c(c5c(n4CC4CC4)CCCC5)C[C@@]4(O)C(C2)N(CC2CC2)CC[C@]314 10.1021/jm040817t
CHEMBL439019 216279 None 0 Human Functional pEC50 = 8.4 8.4 -1 4
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 CCCC[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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm061369n
44573404 187492 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 379 4 1 5 3.6 Nc1ccnc(N2CCC(N(C(=O)C3CCCCC3)c3ccccn3)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL493516 187492 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 379 4 1 5 3.6 Nc1ccnc(N2CCC(N(C(=O)C3CCCCC3)c3ccccn3)CC2)c1 10.1016/j.bmcl.2009.01.106
50994461 57235 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 717 15 4 6 5.4 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649944 57235 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 717 15 4 6 5.4 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
50994461 57235 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 717 15 4 6 5.4 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649944 57235 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
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 717 15 4 6 5.4 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
102270005 112923 None 0 Human Functional pEC50 = 7.5 7.5 22 2
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
CHEMBL3309509 112923 None 0 Human Functional pEC50 = 7.5 7.5 22 2
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
10760626 19406 None 0 Human Functional pEC50 = 7.5 7.5 575 2
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 354 5 1 3 4.4 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccs2)cc1 10.1021/jm000229p
CHEMBL129315 19406 None 0 Human Functional pEC50 = 7.5 7.5 575 2
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 354 5 1 3 4.4 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccs2)cc1 10.1021/jm000229p
CHEMBL247368 212965 None 16 Human Functional pEC50 = 6.5 6.5 2 2
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 None None None CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2007.01.092
162669697 182826 None 0 Human Functional pEC50 = 6.5 6.5 -1258 4
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 1394 36 20 16 -0.8 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](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4789659 182826 None 0 Human Functional pEC50 = 6.5 6.5 -1258 4
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 1394 36 20 16 -0.8 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](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
135510996 20461 None 6 Human Functional pEC50 = 5.5 5.5 -1 2
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 452 4 2 6 3.8 Cc1cc(/C=C2\SC(Nc3ccccc3)=NC2=O)c(C)n1-c1ccc(S(N)(=O)=O)cc1 nan
CHEMBL1307021 20461 None 6 Human Functional pEC50 = 5.5 5.5 -1 2
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 452 4 2 6 3.8 Cc1cc(/C=C2\SC(Nc3ccccc3)=NC2=O)c(C)n1-c1ccc(S(N)(=O)=O)cc1 nan
162643877 181823 None 0 Human Functional pEC50 = 6.5 6.5 -354 4
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 1436 37 20 16 0.2 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)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4776986 181823 None 0 Human Functional pEC50 = 6.5 6.5 -354 4
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 1436 37 20 16 0.2 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)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
4206984 52748 None 1 Human Functional pEC50 = 4.5 4.5 -8 3
PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]
ChEMBL 325 4 2 4 4.8 CCC(=NNc1ccnc2cc(Cl)ccc12)c1ccc(O)cc1 nan
CHEMBL1594497 52748 None 1 Human Functional pEC50 = 4.5 4.5 -8 3
PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]PUBCHEM_BIOASSAY: SAR Analysis of Agonists of the DOR Receptor using an Image-Based Assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1785, AID1786, AID1966, AID2133, AID2136, AID2284, AID2285, AID2493]
ChEMBL 325 4 2 4 4.8 CCC(=NNc1ccnc2cc(Cl)ccc12)c1ccc(O)cc1 nan
44573334 187527 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 281 1 1 4 2.7 Nc1ccnc(N2CCC3(CC2)OCc2ccccc23)c1 10.1016/j.bmcl.2009.01.106
CHEMBL493753 187527 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 281 1 1 4 2.7 Nc1ccnc(N2CCC3(CC2)OCc2ccccc23)c1 10.1016/j.bmcl.2009.01.106
2999792 52898 None 4 Human Functional pEC50 = 4.5 4.5 - 1
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 343 8 2 4 2.3 CC(=O)NC(CC(=O)NCC(c1ccco1)N(C)C)c1ccccc1 nan
CHEMBL1595735 52898 None 4 Human Functional pEC50 = 4.5 4.5 - 1
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 343 8 2 4 2.3 CC(=O)NC(CC(=O)NCC(c1ccco1)N(C)C)c1ccccc1 nan
145982828 165818 None 0 Rat Functional pEC50 = 7.5 7.5 2 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 575 7 0 5 6.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccc(-c3ccccc3)cc1)C2 10.1016/j.bmc.2018.07.020
CHEMBL4245987 165818 None 0 Rat Functional pEC50 = 7.5 7.5 2 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 575 7 0 5 6.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccc(-c3ccccc3)cc1)C2 10.1016/j.bmc.2018.07.020
CHEMBL5088056 218060 None 0 Human Functional pEC50 = 7.5 7.5 -33 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccsc1 10.1021/acs.jmedchem.2c00087
CHEMBL5096013 218060 None 0 Human Functional pEC50 = 7.5 7.5 -33 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccsc1 10.1021/acs.jmedchem.2c00087
9911115 190152 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 344 1 1 3 3.9 CN1CC[C@@]2(c3cccc(O)c3)Cc3nc4ccccc4cc3C[C@@H]2C1 10.1021/acs.jmedchem.2c01061
CHEMBL5171947 190152 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 344 1 1 3 3.9 CN1CC[C@@]2(c3cccc(O)c3)Cc3nc4ccccc4cc3C[C@@H]2C1 10.1021/acs.jmedchem.2c01061
132079915 183581 None 0 Human Functional pEC50 = 6.5 6.5 -4 2
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 526 4 0 8 5.1 COC(=O)[C@@H]1C=C(OC(=O)c2ccc(Cl)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
CHEMBL4799292 183581 None 0 Human Functional pEC50 = 6.5 6.5 -4 2
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 526 4 0 8 5.1 COC(=O)[C@@H]1C=C(OC(=O)c2ccc(Cl)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
44254062 198188 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 390 4 1 3 4.4 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1C 10.1021/jm900773n
CHEMBL557257 198188 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 390 4 1 3 4.4 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1C 10.1021/jm900773n
16195681 21056 None 0 Human Functional pEC50 = 4.5 4.5 -14 2
PUBCHEM_BIOASSAY: HTS Image-Based Screen for Agonists of the DOR Receptor. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1786, AID2133]PUBCHEM_BIOASSAY: HTS Image-Based Screen for Agonists of the DOR Receptor. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1786, AID2133]
ChEMBL 560 8 2 5 4.8 Cc1ccc(C(=O)N[C@@H](C)CN2C3=NC[C@@H](Cc4ccccc4)N3C[C@H]2Cc2ccc(O)cc2)cc1Br nan
CHEMBL1311831 21056 None 0 Human Functional pEC50 = 4.5 4.5 -14 2
PUBCHEM_BIOASSAY: HTS Image-Based Screen for Agonists of the DOR Receptor. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1786, AID2133]PUBCHEM_BIOASSAY: HTS Image-Based Screen for Agonists of the DOR Receptor. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1777, AID1786, AID2133]
ChEMBL 560 8 2 5 4.8 Cc1ccc(C(=O)N[C@@H](C)CN2C3=NC[C@@H](Cc4ccccc4)N3C[C@H]2Cc2ccc(O)cc2)cc1Br nan
162675694 183549 None 0 Human Functional pEC50 = 6.5 6.5 -245 4
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 1422 36 20 16 -0.2 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](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4798887 183549 None 0 Human Functional pEC50 = 6.5 6.5 -245 4
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 1422 36 20 16 -0.2 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](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
90656667 111025 None 0 Human Functional pEC50 = 6.5 6.5 -2 3
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 479 5 2 5 4.6 CC[C@](O)([C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
CHEMBL3262362 111025 None 0 Human Functional pEC50 = 6.5 6.5 -2 3
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 479 5 2 5 4.6 CC[C@](O)([C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
1627 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm8012272
1845 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm8012272
5288826 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm8012272
5288826.0 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm8012272
CHEMBL70 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm8012272
DB00295 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm8012272
1627 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm0604777
1845 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm0604777
5288826 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm0604777
5288826.0 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm0604777
CHEMBL70 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm0604777
DB00295 2594 None 9 Human Functional pEC50 = 6.5 6.5 -13 9
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm0604777
127050108 141036 None 0 Rat Functional pEC50 = 7.5 7.5 -8 3
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 485 7 3 4 4.5 CCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
CHEMBL3822956 141036 None 0 Rat Functional pEC50 = 7.5 7.5 -8 3
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 485 7 3 4 4.5 CCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
72164175 92097 None 0 Mouse Functional pEC50 = 7.5 7.5 -18 4
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 561 5 3 7 4.0 COc1c(C(=O)N[C@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)nc(Cl)c2ccccc12 10.1016/j.bmc.2015.02.055
CHEMBL2419121 92097 None 0 Mouse Functional pEC50 = 7.5 7.5 -18 4
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 561 5 3 7 4.0 COc1c(C(=O)N[C@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)nc(Cl)c2ccccc12 10.1016/j.bmc.2015.02.055
73354725 89511 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 672 8 7 9 0.5 CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1016/j.bmcl.2007.01.092
CHEMBL2372104 89511 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 672 8 7 9 0.5 CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1016/j.bmcl.2007.01.092
71819400 92083 None 0 Human Functional pEC50 = 5.5 5.5 -5 5
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 315 1 1 4 2.0 COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
CHEMBL2418738 92083 None 0 Human Functional pEC50 = 5.5 5.5 -5 5
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 315 1 1 4 2.0 COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
73352234 92090 None 0 Human Functional pEC50 = 5.5 5.5 -3 5
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 331 1 0 3 3.3 COc1cc(C)c2c3c1O[C@H]1[C@H](F)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@@]341 10.1016/j.bmcl.2013.06.084
CHEMBL2418745 92090 None 0 Human Functional pEC50 = 5.5 5.5 -3 5
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 331 1 0 3 3.3 COc1cc(C)c2c3c1O[C@H]1[C@H](F)[C@H](C)C[C@H]4[C@@H](C2)N(C)CC[C@@]341 10.1016/j.bmcl.2013.06.084
11949196 23362 None 0 Human Functional pEC50 = 5.5 5.5 6 2
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 443 5 0 3 6.2 c1ccc(C2[C@H]3CN(Cc4cccnc4)[C@H](c4ccccc4)C34CC2(c2cccnc2)C4)cc1 nan
CHEMBL1332532 23362 None 0 Human Functional pEC50 = 5.5 5.5 6 2
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 443 5 0 3 6.2 c1ccc(C2[C@H]3CN(Cc4cccnc4)[C@H](c4ccccc4)C34CC2(c2cccnc2)C4)cc1 nan
156014669 177354 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Inverse agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayInverse agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 2 2 4 3.4 COC1=CC=C2C[C@H]3N(C(=O)C4CC4)CC[C@]45C2C1O[C@H]4c1[nH]c2ccccc2c1C[C@@]35O 10.1016/j.bmcl.2020.127176
CHEMBL4635947 177354 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Inverse agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayInverse agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 2 2 4 3.4 COC1=CC=C2C[C@H]3N(C(=O)C4CC4)CC[C@]45C2C1O[C@H]4c1[nH]c2ccccc2c1C[C@@]35O 10.1016/j.bmcl.2020.127176
2417585 56024 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 377 6 2 4 3.5 CCn1c(N)[n+](CC(=O)Nc2ccc(SC(F)F)cc2)c2ccccc21 nan
CHEMBL1566118 56024 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 377 6 2 4 3.5 CCn1c(N)[n+](CC(=O)Nc2ccc(SC(F)F)cc2)c2ccccc21 nan
CHEMBL1624550 56024 None 0 Human Functional pEC50 = 4.5 4.5 - 1
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 377 6 2 4 3.5 CCn1c(N)[n+](CC(=O)Nc2ccc(SC(F)F)cc2)c2ccccc21 nan
4973873 26172 None 4 Human Functional pEC50 = 4.5 4.5 -1 2
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 379 4 1 4 4.1 CN1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4F)o3)cc2)CC1 nan
CHEMBL1356740 26172 None 4 Human Functional pEC50 = 4.5 4.5 -1 2
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 379 4 1 4 4.1 CN1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4F)o3)cc2)CC1 nan
CHEMBL3580748 214235 None 0 Human Functional pEC50 = 7.5 7.5 -61 6
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 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.5b00056
162666206 182360 None 0 Human Functional pEC50 = 5.5 5.5 -10 2
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 505 11 1 4 4.6 CCC(=O)N(Cc1ccco1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
CHEMBL4783653 182360 None 0 Human Functional pEC50 = 5.5 5.5 -10 2
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 505 11 1 4 4.6 CCC(=O)N(Cc1ccco1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
134563683 195927 None 0 Human Functional pEC50 = 6.5 6.5 -15 4
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 431 6 1 4 4.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CNS(C)(=O)=O)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
CHEMBL5413519 195927 None 0 Human Functional pEC50 = 6.5 6.5 -15 4
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 431 6 1 4 4.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CNS(C)(=O)=O)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
12461184 98471 None 14 Human Functional pEC50 = 4.5 4.5 -5 2
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 243 2 0 1 4.3 c1ccc(C2(N3CCCCC3)CCCCC2)cc1 nan
6468 98471 None 14 Human Functional pEC50 = 4.5 4.5 -5 2
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 243 2 0 1 4.3 c1ccc(C2(N3CCCCC3)CCCCC2)cc1 nan
CHEMBL275528 98471 None 14 Human Functional pEC50 = 4.5 4.5 -5 2
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 243 2 0 1 4.3 c1ccc(C2(N3CCCCC3)CCCCC2)cc1 nan
CHEMBL542581 98471 None 14 Human Functional pEC50 = 4.5 4.5 -5 2
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 243 2 0 1 4.3 c1ccc(C2(N3CCCCC3)CCCCC2)cc1 nan
11271551 102242 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 478 8 0 2 6.8 CCN(CC)C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL302801 102242 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 478 8 0 2 6.8 CCN(CC)C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
54756990 65725 None 0 Human Functional pEC50 = 5.5 5.5 -3890 3
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834411 65725 None 0 Human Functional pEC50 = 5.5 5.5 -3890 3
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
16189942 36569 None 5 Human Functional pEC50 = 4.5 4.5 -1 2
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 419 8 1 6 4.5 CCn1cc(CNCc2cn(-c3ccccc3C)nc2-c2ccc(OC)c(F)c2)cn1 nan
CHEMBL1448229 36569 None 5 Human Functional pEC50 = 4.5 4.5 -1 2
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 419 8 1 6 4.5 CCn1cc(CNCc2cn(-c3ccccc3C)nc2-c2ccc(OC)c(F)c2)cn1 nan
71449607 81366 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 495 9 3 4 4.5 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N(Cc1ccccc1)[C@@H](C)c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL2159119 81366 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 495 9 3 4 4.5 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)N(Cc1ccccc1)[C@@H](C)c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL261390 212977 None 0 Human Functional pEC50 = 7.5 7.5 3 3
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 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)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm070332f
CHEMBL5083695 218030 None 0 Human Functional pEC50 = 7.5 7.5 -36 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccco1 10.1021/acs.jmedchem.2c00087
CHEMBL5095764 218030 None 0 Human Functional pEC50 = 7.5 7.5 -36 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccco1 10.1021/acs.jmedchem.2c00087
132079908 180880 None 0 Human Functional pEC50 = 6.5 6.5 -6 3
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 510 4 0 8 4.6 COC(=O)[C@@H]1C=C(OC(=O)c2ccc(F)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
CHEMBL4756271 180880 None 0 Human Functional pEC50 = 6.5 6.5 -6 3
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 510 4 0 8 4.6 COC(=O)[C@@H]1C=C(OC(=O)c2ccc(F)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
10141332 205556 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 6 0 3 5.8 O=C(c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1)N1CCOCC1 10.1016/j.bmcl.2004.02.051
CHEMBL63948 205556 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 6 0 3 5.8 O=C(c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1)N1CCOCC1 10.1016/j.bmcl.2004.02.051
10185709 100809 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 506 10 0 2 7.6 CCCN(CCC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL292794 100809 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 506 10 0 2 7.6 CCCN(CCC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
9551332 51750 None 5 Human Functional pEC50 = 4.5 4.5 1 2
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 341 3 2 3 4.0 CCc1ccc(NC(=O)Nc2ccc3c(c2)N(C)C(=O)CS3)cc1 nan
CHEMBL1584594 51750 None 5 Human Functional pEC50 = 4.5 4.5 1 2
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 341 3 2 3 4.0 CCc1ccc(NC(=O)Nc2ccc3c(c2)N(C)C(=O)CS3)cc1 nan
44598284 200311 None 0 Rat Functional pEC50 = 7.4 7.4 -30 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassayAgonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassay
ChEMBL 742 9 7 9 1.8 NC(=O)[C@@H]1CSCSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1 10.1021/jm9007483
CHEMBL572525 200311 None 0 Rat Functional pEC50 = 7.4 7.4 -30 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassayAgonist activity at rat delta opioid receptor expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by radioimmunoassay
ChEMBL 742 9 7 9 1.8 NC(=O)[C@@H]1CSCSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1 10.1021/jm9007483
127025219 137725 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at delta opioid receptor (unknown origin) assessed as inhibition of adenylyl cyclase activityPartial agonist activity at delta opioid receptor (unknown origin) assessed as inhibition of adenylyl cyclase activity
ChEMBL 742 9 7 9 1.8 NC(=O)[C@H]1CSCSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1 10.1016/j.ejmech.2015.11.028
CHEMBL3758259 137725 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Partial agonist activity at delta opioid receptor (unknown origin) assessed as inhibition of adenylyl cyclase activityPartial agonist activity at delta opioid receptor (unknown origin) assessed as inhibition of adenylyl cyclase activity
ChEMBL 742 9 7 9 1.8 NC(=O)[C@H]1CSCSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1 10.1016/j.ejmech.2015.11.028
10569964 117089 None 0 Human Functional pEC50 = 7.4 7.4 407 2
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 351 6 1 3 3.2 CCN(CC)C(=O)c1ccc(C(c2ccccc2)N2CCNCC2)cc1 10.1021/jm000229p
CHEMBL338980 117089 None 0 Human Functional pEC50 = 7.4 7.4 407 2
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 351 6 1 3 3.2 CCN(CC)C(=O)c1ccc(C(c2ccccc2)N2CCNCC2)cc1 10.1021/jm000229p
44254063 198808 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 390 4 1 3 4.4 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)c(C)c1 10.1021/jm900773n
CHEMBL562478 198808 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 390 4 1 3 4.4 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)c(C)c1 10.1021/jm900773n
CHEMBL387670 214871 None 0 Human Functional pEC50 = 6.4 6.4 -83 4
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 CCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(C)C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061369n
118713811 114481 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 1026 12 12 14 0.3 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)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/ml500241n
CHEMBL3331511 114481 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 1026 12 12 14 0.3 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)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/ml500241n
9909743 35264 None 1 Mouse Functional pEC50 = 6.4 6.4 -19 4
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 414 5 1 3 5.6 CC(C)(C)c1ccc(C(c2cccc(O)c2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm980374r
CHEMBL143592 35264 None 1 Mouse Functional pEC50 = 6.4 6.4 -19 4
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 414 5 1 3 5.6 CC(C)(C)c1ccc(C(c2cccc(O)c2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm980374r
4587627 59194 None 3 Human Functional pEC50 = 4.4 4.4 - 1
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 360 6 1 2 3.4 CN(C)C(CNC(=O)Cc1ccc(Br)cc1)c1ccccc1 nan
CHEMBL1700227 59194 None 3 Human Functional pEC50 = 4.4 4.4 - 1
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 360 6 1 2 3.4 CN(C)C(CNC(=O)Cc1ccc(Br)cc1)c1ccccc1 nan
CHEMBL387670 214871 None 0 Human Functional pEC50 = 6.4 6.4 -83 4
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 CCCC[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)N(C)C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061369n
122181110 121888 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assayAgonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
ChEMBL 486 8 1 5 5.2 CC(C)C[C@H]1CN2C(=CC3=NC[C@H](C(C)C)N3C[C@@H]2Cc2ccc(O)cc2)N1CCc1ccccc1 10.1021/jm501637c
CHEMBL3589796 121888 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assayAgonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
ChEMBL 486 8 1 5 5.2 CC(C)C[C@H]1CN2C(=CC3=NC[C@H](C(C)C)N3C[C@@H]2Cc2ccc(O)cc2)N1CCc1ccccc1 10.1021/jm501637c
104787 1473 None 17 Rat Functional pEC50 = 6.4 6.4 -14 4
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2017.02.064
1608 1473 None 17 Rat Functional pEC50 = 6.4 6.4 -14 4
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2017.02.064
CHEMBL31421 1473 None 17 Rat Functional pEC50 = 6.4 6.4 -14 4
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2017.02.064
DB08861 1473 None 17 Rat Functional pEC50 = 6.4 6.4 -14 4
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2017.02.064
44337800 5451 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 502 2 2 3 6.6 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12C/C(=C(/C)c1ccccc1)[C@@H]3c1[nH]c3ccccc3c1C2 10.1021/jm030801n
CHEMBL107420 5451 None 0 Human Functional pEC50 = 6.4 6.4 -4 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 502 2 2 3 6.6 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12C/C(=C(/C)c1ccccc1)[C@@H]3c1[nH]c3ccccc3c1C2 10.1021/jm030801n
9909946 138370 None 0 Mouse Functional pEC50 = 7.4 7.4 -18 3
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 418 5 3 4 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
CHEMBL377069 138370 None 0 Mouse Functional pEC50 = 7.4 7.4 -18 3
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 418 5 3 4 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2006.01.082
9909946 138370 None 0 Human Functional pEC50 = 7.4 7.4 -18 3
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 418 5 3 4 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
CHEMBL377069 138370 None 0 Human Functional pEC50 = 7.4 7.4 -18 3
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 418 5 3 4 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCCC[C@H]1c1nc(-c2ccccc2)c[nH]1 10.1016/j.bmcl.2012.05.042
71625485 90595 None 0 Human Functional pEC50 = 7.4 7.4 1 3
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 874 22 7 9 2.6 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
CHEMBL2387338 90595 None 0 Human Functional pEC50 = 7.4 7.4 1 3
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 874 22 7 9 2.6 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
44436083 146537 None 0 Human Functional pEC50 = 7.4 7.4 2 3
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 817 18 6 8 2.8 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)Cc2ccc(O)cc2)CC1 10.1021/jm061465o
CHEMBL392207 146537 None 0 Human Functional pEC50 = 7.4 7.4 2 3
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 817 18 6 8 2.8 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)Cc2ccc(O)cc2)CC1 10.1021/jm061465o
11235302 123909 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 412 4 3 4 3.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc2ccccc2[nH]1 10.1021/jm030548r
CHEMBL362514 123909 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 412 4 3 4 3.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc2ccccc2[nH]1 10.1021/jm030548r
44436083 146537 None 0 Human Functional pEC50 = 7.4 7.4 2 3
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 817 18 6 8 2.8 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)Cc2ccc(O)cc2)CC1 10.1021/jm061465o
CHEMBL392207 146537 None 0 Human Functional pEC50 = 7.4 7.4 2 3
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 817 18 6 8 2.8 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)Cc2ccc(O)cc2)CC1 10.1021/jm061465o
44254060 198875 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 382 4 1 4 4.2 CCN(CC)C(=O)c1cc(C2=CC3(CCNCC3)Oc3ccccc32)cs1 10.1021/jm900773n
CHEMBL562898 198875 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 382 4 1 4 4.2 CCN(CC)C(=O)c1cc(C2=CC3(CCNCC3)Oc3ccccc32)cs1 10.1021/jm900773n
118725857 117246 None 0 Human Functional pEC50 = 4.4 4.4 -1000 3
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 5 1 5 3.4 O=C(Nc1nc2cccnc2n1CCN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2014.12.064
CHEMBL3394007 117246 None 0 Human Functional pEC50 = 4.4 4.4 -1000 3
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 5 1 5 3.4 O=C(Nc1nc2cccnc2n1CCN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2014.12.064
CHEMBL5082892 217319 None 0 Human Functional pEC50 = 6.4 6.4 -4 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
CHEMBL285479 213322 None 0 Human Functional pEC50 = 6.4 6.4 -89 2
Agonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assayAgonist activity at human recombinant DOR expressed in CHO cells by calcium mobilization assay
ChEMBL None None None C[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1016/j.bmc.2016.02.034
16192289 38458 None 1 Human Functional pEC50 = 4.4 4.4 -15 2
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 389 6 1 5 4.6 Cc1ccc(-n2cc(CNC(C)c3cnn(C)c3)c(-c3ccc(F)cc3)n2)cc1 nan
CHEMBL1463894 38458 None 1 Human Functional pEC50 = 4.4 4.4 -15 2
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 389 6 1 5 4.6 Cc1ccc(-n2cc(CNC(C)c3cnn(C)c3)c(-c3ccc(F)cc3)n2)cc1 nan
CHEMBL5082892 217319 None 0 Human Functional pEC50 = 6.4 6.4 -4 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
162652836 180494 None 0 Human Functional pEC50 = 6.4 6.4 -23 2
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 489 10 1 5 4.7 CCC(=O)N(Cc1ccco1)C1(C(=O)Nc2ccc(OC)cc2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
CHEMBL4751847 180494 None 0 Human Functional pEC50 = 6.4 6.4 -23 2
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 489 10 1 5 4.7 CCC(=O)N(Cc1ccco1)C1(C(=O)Nc2ccc(OC)cc2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
72713095 106412 None 0 Human Functional pEC50 = 7.4 7.4 -5 2
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 392 6 1 3 4.7 C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N(C)C)C[C@]1(c1cccc(O)c1)C2 10.1021/jm401250s
CHEMBL3139213 106412 None 0 Human Functional pEC50 = 7.4 7.4 -5 2
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 392 6 1 3 4.7 C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N(C)C)C[C@]1(c1cccc(O)c1)C2 10.1021/jm401250s
CHEMBL3216613 106412 None 0 Human Functional pEC50 = 7.4 7.4 -5 2
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 392 6 1 3 4.7 C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N(C)C)C[C@]1(c1cccc(O)c1)C2 10.1021/jm401250s
53388149 66555 None 1 Human Functional pEC50 = 7.4 7.4 -25 3
Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 461 4 3 6 2.5 Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm301247n
CHEMBL1824515 66555 None 1 Human Functional pEC50 = 7.4 7.4 -25 3
Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 461 4 3 6 2.5 Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm301247n
CHEMBL1852393 66555 None 1 Human Functional pEC50 = 7.4 7.4 -25 3
Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 461 4 3 6 2.5 Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm301247n
162643968 181889 None 0 Human Functional pEC50 = 7.4 7.4 2 5
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
CHEMBL4777803 181889 None 0 Human Functional pEC50 = 7.4 7.4 2 5
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
CHEMBL5074403 218061 None 2 Human Functional pEC50 = 7.4 7.4 -36 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccsc1 10.1021/acs.jmedchem.2c00087
CHEMBL5096015 218061 None 2 Human Functional pEC50 = 7.4 7.4 -36 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccsc1 10.1021/acs.jmedchem.2c00087
162643968 181889 None 0 Human Functional pEC50 = 7.4 7.4 2 5
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
CHEMBL4777803 181889 None 0 Human Functional pEC50 = 7.4 7.4 2 5
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
132079911 179661 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
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 506 4 0 8 4.7 COC(=O)[C@@H]1C=C(OC(=O)c2ccc(C)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
CHEMBL4741711 179661 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
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 506 4 0 8 4.7 COC(=O)[C@@H]1C=C(OC(=O)c2ccc(C)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
25129089 187325 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 277 1 1 2 3.6 C1=C(c2ccccc2)c2ccccc2OC12CCNCC2 10.1021/jm8008986
CHEMBL492447 187325 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 277 1 1 2 3.6 C1=C(c2ccccc2)c2ccccc2OC12CCNCC2 10.1021/jm8008986
7362 2114 None 29 Human Functional pEC50 = 6.4 6.4 -63 3
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 465 6 4 5 3.6 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CC[C@@]([C@H](C1)C)(C)c1cccc(c1)O 10.1021/jm1004978
9956146 2114 None 29 Human Functional pEC50 = 6.4 6.4 -63 3
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 465 6 4 5 3.6 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CC[C@@]([C@H](C1)C)(C)c1cccc(c1)O 10.1021/jm1004978
CHEMBL415247 2114 None 29 Human Functional pEC50 = 6.4 6.4 -63 3
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 465 6 4 5 3.6 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CC[C@@]([C@H](C1)C)(C)c1cccc(c1)O 10.1021/jm1004978
1642 2859 None 17 Human Functional pEC50 = 6.4 6.4 -30 7
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 661 4 5 8 3.8 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2C[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)CC1CC1 10.1021/jm1004978
5480230 2859 None 17 Human Functional pEC50 = 6.4 6.4 -30 7
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 661 4 5 8 3.8 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2C[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)CC1CC1 10.1021/jm1004978
CHEMBL573214 2859 None 17 Human Functional pEC50 = 6.4 6.4 -30 7
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 661 4 5 8 3.8 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2C[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)CC1CC1 10.1021/jm1004978
46867404 6580 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 460 6 3 4 5.3 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)c1ccc2cc(O)ccc2c1 10.1021/jm1004978
CHEMBL1083061 6580 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 460 6 3 4 5.3 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)c1ccc2cc(O)ccc2c1 10.1021/jm1004978
CHEMBL1204084 6580 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 460 6 3 4 5.3 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)c1ccc2cc(O)ccc2c1 10.1021/jm1004978
11712760 6581 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 482 6 3 5 4.7 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2CS1 10.1021/jm1004978
CHEMBL1083062 6581 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 482 6 3 5 4.7 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2CS1 10.1021/jm1004978
11540292 6654 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 482 6 3 5 4.7 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CS1 10.1021/jm1004978
CHEMBL1083371 6654 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 482 6 3 5 4.7 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CS1 10.1021/jm1004978
CHEMBL1204085 6654 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 482 6 3 5 4.7 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CS1 10.1021/jm1004978
11562377 6655 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 498 6 3 5 3.7 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2C[S+]1[O-] 10.1021/jm1004978
CHEMBL1083372 6655 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 498 6 3 5 3.7 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2C[S+]1[O-] 10.1021/jm1004978
11619680 6958 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 466 6 3 5 4.0 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CO1 10.1021/jm1004978
CHEMBL1084529 6958 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 466 6 3 5 4.0 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1Cc2ccc(O)cc2CO1 10.1021/jm1004978
11698381 7081 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 464 6 3 4 4.6 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1CCc2cc(O)ccc2C1 10.1021/jm1004978
CHEMBL1085023 7081 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 464 6 3 4 4.6 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@@H]1CCc2cc(O)ccc2C1 10.1021/jm1004978
11496383 7082 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 464 6 3 4 4.6 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1CCc2cc(O)ccc2C1 10.1021/jm1004978
CHEMBL1085024 7082 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 464 6 3 4 4.6 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1CCc2cc(O)ccc2C1 10.1021/jm1004978
11698420 7083 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 466 6 3 5 4.0 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2CO1 10.1021/jm1004978
CHEMBL1085025 7083 None 0 Human Functional pEC50 = 6.4 6.4 -63 3
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 466 6 3 5 4.0 CC(C)[C@@H](CN1CC[C@@](C)(c2cccc(O)c2)[C@@H](C)C1)NC(=O)[C@H]1Cc2ccc(O)cc2CO1 10.1021/jm1004978
168293279 192259 None 0 Human Functional pEC50 = 5.4 5.4 -8 4
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 583 15 5 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)N(C)C 10.1039/D1MD00025J
CHEMBL5203813 192259 None 0 Human Functional pEC50 = 5.4 5.4 -8 4
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 583 15 5 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)N(C)C 10.1039/D1MD00025J
168293279 192259 None 0 Human Functional pEC50 = 5.4 5.4 -8 4
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 583 15 5 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)N(C)C 10.1039/D1MD00025J
CHEMBL5203813 192259 None 0 Human Functional pEC50 = 5.4 5.4 -8 4
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 583 15 5 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)N(C)C 10.1039/D1MD00025J
25208099 188477 None 0 Human Functional pEC50 = 6.4 6.4 -245 4
Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL501331 188477 None 0 Human Functional pEC50 = 6.4 6.4 -245 4
Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
168275838 190465 None 0 Human Functional pEC50 = 5.4 5.4 -28 3
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 657 14 4 6 3.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc2ccc(O)cc2)CC1 10.1039/D1MD00025J
CHEMBL5177001 190465 None 0 Human Functional pEC50 = 5.4 5.4 -28 3
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 657 14 4 6 3.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc2ccc(O)cc2)CC1 10.1039/D1MD00025J
168275838 190465 None 0 Human Functional pEC50 = 5.4 5.4 -28 3
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 657 14 4 6 3.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc2ccc(O)cc2)CC1 10.1039/D1MD00025J
CHEMBL5177001 190465 None 0 Human Functional pEC50 = 5.4 5.4 -28 3
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 657 14 4 6 3.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc2ccc(O)cc2)CC1 10.1039/D1MD00025J
16191631 30251 None 5 Human Functional pEC50 = 4.4 4.4 - 1
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 404 5 1 3 4.8 CC(=O)Nc1ccc(CN2CCCC(C(=O)c3cccc(C(F)(F)F)c3)C2)cc1 nan
CHEMBL1390846 30251 None 5 Human Functional pEC50 = 4.4 4.4 - 1
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 404 5 1 3 4.8 CC(=O)Nc1ccc(CN2CCCC(C(=O)c3cccc(C(F)(F)F)c3)C2)cc1 nan
2037119 52068 None 10 Human Functional pEC50 = 5.4 5.4 18 2
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 446 7 1 8 3.8 COc1ccc(CN2CN=C(Nc3nc(C)cc(C)n3)N(Cc3ccc(OC)cc3)C2)cc1 nan
CHEMBL1587149 52068 None 10 Human Functional pEC50 = 5.4 5.4 18 2
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 446 7 1 8 3.8 COc1ccc(CN2CN=C(Nc3nc(C)cc(C)n3)N(Cc3ccc(OC)cc3)C2)cc1 nan
89978612 160492 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 575 11 1 7 4.6 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccc(OCC(=O)O)cc1)C2 nan
CHEMBL4111244 160492 None 0 Human Functional pEC50 = 6.4 6.4 -1 2
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 575 11 1 7 4.6 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccc(OCC(=O)O)cc1)C2 nan
155555051 176399 None 0 Human Functional pEC50 = 8.4 8.4 -6 3
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1060 12 10 14 -0.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
CHEMBL4551481 176399 None 0 Human Functional pEC50 = 8.4 8.4 -6 3
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1060 12 10 14 -0.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
CHEMBL4595157 176399 None 0 Human Functional pEC50 = 8.4 8.4 -6 3
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1060 12 10 14 -0.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
CHEMBL439019 216279 None 0 Human Functional pEC50 = 8.4 8.4 -1 4
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 CCCC[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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm061369n
CHEMBL205306 211627 None 0 Human Functional pEC50 = 8.4 8.4 8 4
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](CCCC)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
CHEMBL205306 211627 None 0 Human Functional pEC50 = 8.4 8.4 8 4
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](CCCC)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
44439880 93690 None 0 Human Functional pEC50 = 8.4 8.4 43 2
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 610 16 7 7 -0.2 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)O 10.1016/j.bmcl.2007.01.092
CHEMBL246739 93690 None 0 Human Functional pEC50 = 8.4 8.4 43 2
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 610 16 7 7 -0.2 Cc1cc(C(N)=O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)O 10.1016/j.bmcl.2007.01.092
CHEMBL294616 213353 None 0 Mouse Functional pEC50 = 8.4 8.4 -2 7
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 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/jm0303103
45486027 199998 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 421 9 1 4 5.1 C=CCCN1CCC(N(c2ccc(C(=O)N(CC)CC)cc2)c2cccc(O)c2)CC1 10.1016/j.bmcl.2009.09.072
CHEMBL570232 199998 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
ChEMBL 421 9 1 4 5.1 C=CCCN1CCC(N(c2ccc(C(=O)N(CC)CC)cc2)c2cccc(O)c2)CC1 10.1016/j.bmcl.2009.09.072
44337613 7934 None 0 Human Functional pEC50 = 8.4 8.4 1 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 415 2 1 4 4.4 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@]12CCC(=O)[C@H]3/C(=C/c1ccccc1)C2 10.1021/jm030801n
CHEMBL109040 7934 None 0 Human Functional pEC50 = 8.4 8.4 1 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 415 2 1 4 4.4 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@]12CCC(=O)[C@H]3/C(=C/c1ccccc1)C2 10.1021/jm030801n
155536563 176674 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1164 12 10 14 1.3 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSCc2ccccc2CSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
CHEMBL4473632 176674 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1164 12 10 14 1.3 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSCc2ccccc2CSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
CHEMBL4597415 176674 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1164 12 10 14 1.3 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSCc2ccccc2CSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCN(CC2)C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
104787 1473 None 17 Human Functional pEC50 = 8.4 8.4 -2 4
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 None None None None 10.1016/j.bmc.2021.116552
1608 1473 None 17 Human Functional pEC50 = 8.4 8.4 -2 4
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 None None None None 10.1016/j.bmc.2021.116552
CHEMBL31421 1473 None 17 Human Functional pEC50 = 8.4 8.4 -2 4
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 None None None None 10.1016/j.bmc.2021.116552
DB08861 1473 None 17 Human Functional pEC50 = 8.4 8.4 -2 4
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 None None None None 10.1016/j.bmc.2021.116552
1639 2726 None 32 Human Functional pEC50 = 8.4 8.4 -25 9
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm4012214
1765 2726 None 32 Human Functional pEC50 = 8.4 8.4 -25 9
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm4012214
5360515 2726 None 32 Human Functional pEC50 = 8.4 8.4 -25 9
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm4012214
5360515.0 2726 None 32 Human Functional pEC50 = 8.4 8.4 -25 9
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm4012214
CHEMBL19019 2726 None 32 Human Functional pEC50 = 8.4 8.4 -25 9
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm4012214
DB00704 2726 None 32 Human Functional pEC50 = 8.4 8.4 -25 9
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm4012214
1639 2726 None 32 Mouse Functional pEC50 = 8.4 8.4 -6 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
1765 2726 None 32 Mouse Functional pEC50 = 8.4 8.4 -6 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
5360515 2726 None 32 Mouse Functional pEC50 = 8.4 8.4 -6 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
5360515.0 2726 None 32 Mouse Functional pEC50 = 8.4 8.4 -6 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
CHEMBL19019 2726 None 32 Mouse Functional pEC50 = 8.4 8.4 -6 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
DB00704 2726 None 32 Mouse Functional pEC50 = 8.4 8.4 -6 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
145963053 161628 None 0 Rat Functional pEC50 = 8.4 8.4 -12 3
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 523 12 5 6 0.7 C=Cc1ccccc1C[C@@H](C(=O)NCC(N)=O)N(C)C(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1016/j.bmcl.2018.05.015
CHEMBL4128530 161628 None 0 Rat Functional pEC50 = 8.4 8.4 -12 3
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 523 12 5 6 0.7 C=Cc1ccccc1C[C@@H](C(=O)NCC(N)=O)N(C)C(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1016/j.bmcl.2018.05.015
CHEMBL208479 211658 None 0 Human Functional pEC50 = 8.4 8.4 1 5
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](CCCC)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
CHEMBL208479 211658 None 0 Human Functional pEC50 = 8.4 8.4 1 5
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](CCCC)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
71230334 111016 None 0 Human Functional pEC50 = 8.3 8.3 -4 3
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
CHEMBL3262090 111016 None 0 Human Functional pEC50 = 8.3 8.3 -4 3
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
104787 1473 None 17 Human Functional pEC50 = 8.3 8.3 -2 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
1608 1473 None 17 Human Functional pEC50 = 8.3 8.3 -2 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
CHEMBL31421 1473 None 17 Human Functional pEC50 = 8.3 8.3 -2 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
DB08861 1473 None 17 Human Functional pEC50 = 8.3 8.3 -2 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
10570940 117287 None 2 Human Functional pEC50 = 8.3 8.3 3090 2
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 366 5 1 2 4.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(F)c2)cc1 10.1021/jm000229p
CHEMBL339457 117287 None 2 Human Functional pEC50 = 8.3 8.3 3090 2
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 366 5 1 2 4.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(F)c2)cc1 10.1021/jm000229p
11849284 204280 None 0 Human Functional pEC50 = 8.3 8.3 -9 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 458 4 1 5 3.2 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
CHEMBL607017 204280 None 0 Human Functional pEC50 = 8.3 8.3 -9 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 458 4 1 5 3.2 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
155569411 176766 None 0 Human Functional pEC50 = 8.3 8.3 3 2
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 461 11 4 5 3.9 CCOc1ccc(CNCc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4592669 176766 None 0 Human Functional pEC50 = 8.3 8.3 3 2
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 461 11 4 5 3.9 CCOc1ccc(CNCc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4598103 176766 None 0 Human Functional pEC50 = 8.3 8.3 3 2
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 461 11 4 5 3.9 CCOc1ccc(CNCc2ccccc2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
89435275 156586 None 0 Human Functional pEC50 = 8.3 8.3 1 3
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 426 3 1 3 5.0 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1c1ccccc1)C2 10.1016/j.bmcl.2017.05.072
CHEMBL4067629 156586 None 0 Human Functional pEC50 = 8.3 8.3 1 3
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 426 3 1 3 5.0 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1c1ccccc1)C2 10.1016/j.bmcl.2017.05.072
71450932 79206 None 0 Human Functional pEC50 = 8.3 8.3 57 3
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 429 4 3 4 4.2 CCCCN[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm021073r
CHEMBL2113377 79206 None 0 Human Functional pEC50 = 8.3 8.3 57 3
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 429 4 3 4 4.2 CCCCN[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm021073r
CHEMBL2419541 212901 None 0 Human Functional pEC50 = 8.3 8.3 2 3
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)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
123924 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
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 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 10.1016/j.bmcl.2007.09.082
1611 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
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 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 10.1016/j.bmcl.2007.09.082
CHEMBL13470 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
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 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 10.1016/j.bmcl.2007.09.082
123924 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
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 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 10.1016/j.bmcl.2012.10.081
1611 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
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 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 10.1016/j.bmcl.2012.10.081
CHEMBL13470 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
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 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 10.1016/j.bmcl.2012.10.081
123924 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S 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/jm060278n
1611 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S 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/jm060278n
CHEMBL13470 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S 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/jm060278n
123924 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
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 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 10.1016/j.bmcl.2009.02.078
1611 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
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 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 10.1016/j.bmcl.2009.02.078
CHEMBL13470 3633 None 34 Human Functional pEC50 = 8.3 8.3 1 9
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 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 10.1016/j.bmcl.2009.02.078
145961040 161489 None 0 Rat Functional pEC50 = 8.3 8.3 -40 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 559 12 6 6 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1-c1ccccc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4126470 161489 None 0 Rat Functional pEC50 = 8.3 8.3 -40 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 559 12 6 6 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1-c1ccccc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
156011205 178419 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 1341 18 13 19 -0.4 CN(C)c1cccc2c(S(=O)(=O)NCCN3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)cccc12 10.1021/acsmedchemlett.9b00569
CHEMBL4638703 178419 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 1341 18 13 19 -0.4 CN(C)c1cccc2c(S(=O)(=O)NCCN3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)cccc12 10.1021/acsmedchemlett.9b00569
CHEMBL4651062 178419 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 1341 18 13 19 -0.4 CN(C)c1cccc2c(S(=O)(=O)NCCN3C(=O)C4=C(SC[C@@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)C(=O)NCC(=O)N[C@@H](Cc5ccccc5)C(=O)NNC(=O)[C@H](Cc5ccccc5)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc5ccc(O)cc5)CS4)C3=O)cccc12 10.1021/acsmedchemlett.9b00569
71605755 87535 None 0 Human Functional pEC50 = 7.4 7.4 -26 2
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 650 12 6 6 2.8 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1)c1ccccc1 10.1021/jm400195y
CHEMBL2334774 87535 None 0 Human Functional pEC50 = 7.4 7.4 -26 2
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 650 12 6 6 2.8 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1)c1ccccc1 10.1021/jm400195y
1647 1313 None 34 Human Functional pEC50 = 6.4 6.4 -19 9
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 None None None None 10.1016/j.bmcl.2013.06.084
5462471 1313 None 34 Human Functional pEC50 = 6.4 6.4 -19 9
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 None None None None 10.1016/j.bmcl.2013.06.084
CHEMBL113995 1313 None 34 Human Functional pEC50 = 6.4 6.4 -19 9
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 None None None None 10.1016/j.bmcl.2013.06.084
CHEMBL38874 1313 None 34 Human Functional pEC50 = 6.4 6.4 -19 9
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 None None None None 10.1016/j.bmcl.2013.06.084
5284603 205871 None 8 Human Functional pEC50 = 5.4 5.4 -5 6
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 315 1 1 5 1.0 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
CHEMBL656 205871 None 8 Human Functional pEC50 = 5.4 5.4 -5 6
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 315 1 1 5 1.0 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(O)[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2013.06.084
44307131 206070 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 538 12 0 4 6.1 COCCN(CCOC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL67068 206070 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 538 12 0 4 6.1 COCCN(CCOC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
89978722 160248 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
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 569 10 1 8 4.2 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OCc5nn[nH]n5)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL4109142 160248 None 0 Human Functional pEC50 = 6.4 6.4 -13 3
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 569 10 1 8 4.2 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OCc5nn[nH]n5)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
2947809 25938 None 6 Human Functional pEC50 = 5.4 5.4 - 1
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 383 5 1 6 3.8 CCN1CCN(c2ccc([N+](=O)[O-])c(Sc3nc4ccccc4[nH]3)c2)CC1 nan
CHEMBL1353993 25938 None 6 Human Functional pEC50 = 5.4 5.4 - 1
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 383 5 1 6 3.8 CCN1CCN(c2ccc([N+](=O)[O-])c(Sc3nc4ccccc4[nH]3)c2)CC1 nan
44573447 193320 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 364 4 1 7 2.4 Nc1ccnc(N2CCC(n3c(=O)n(CC4CC4)c4cccnc43)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL523504 193320 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 364 4 1 7 2.4 Nc1ccnc(N2CCC(n3c(=O)n(CC4CC4)c4cccnc43)CC2)c1 10.1016/j.bmcl.2009.01.106
44367182 44094 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Maximum percentage effect of standard Opioid receptor delta 1 (Cl-DPDPE)Maximum percentage effect of standard Opioid receptor delta 1 (Cl-DPDPE)
ChEMBL 490 3 2 5 4.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c(-c4ccccc4)cn2Cc2ccccc2)C[C@@]3(O)C1C5 10.1021/jm010841w
CHEMBL151476 44094 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Maximum percentage effect of standard Opioid receptor delta 1 (Cl-DPDPE)Maximum percentage effect of standard Opioid receptor delta 1 (Cl-DPDPE)
ChEMBL 490 3 2 5 4.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c(-c4ccccc4)cn2Cc2ccccc2)C[C@@]3(O)C1C5 10.1021/jm010841w
24824635 158915 None 0 Human Functional pEC50 = 7.4 7.4 -6 4
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 480 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)cc1 10.1016/j.bmc.2009.07.069
CHEMBL409458 158915 None 0 Human Functional pEC50 = 7.4 7.4 -6 4
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 480 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611933 158915 None 0 Human Functional pEC50 = 7.4 7.4 -6 4
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 480 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)cc1 10.1016/j.bmc.2009.07.069
CHEMBL5085221 218065 None 0 Human Functional pEC50 = 7.4 7.4 -43 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(Cc1ccco1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/acs.jmedchem.2c00087
CHEMBL5096025 218065 None 0 Human Functional pEC50 = 7.4 7.4 -43 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(Cc1ccco1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/acs.jmedchem.2c00087
10668838 18762 None 0 Human Functional pEC50 = 7.4 7.4 169 3
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 402 7 0 2 5.5 CCN(CC)C(=O)c1ccc(C(=C2CCN(CC3CC3)CC2)c2ccccc2)cc1 10.1021/jm000229p
CHEMBL127788 18762 None 0 Human Functional pEC50 = 7.4 7.4 169 3
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 402 7 0 2 5.5 CCN(CC)C(=O)c1ccc(C(=C2CCN(CC3CC3)CC2)c2ccccc2)cc1 10.1021/jm000229p
118722557 116214 None 0 Human Functional pEC50 = 7.4 7.4 1 3
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 516 5 3 8 3.0 CCOC(=O)Cc1c2c(n(Cc3ccccc3)c1O)[C@@H]1Oc3c(O)ccc4c3[C@@]13CCN(C)[C@H](C4)[C@]3(O)C2 10.1016/j.bmc.2014.05.065
CHEMBL3357966 116214 None 0 Human Functional pEC50 = 7.4 7.4 1 3
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 516 5 3 8 3.0 CCOC(=O)Cc1c2c(n(Cc3ccccc3)c1O)[C@@H]1Oc3c(O)ccc4c3[C@@]13CCN(C)[C@H](C4)[C@]3(O)C2 10.1016/j.bmc.2014.05.065
44337789 7312 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 488 2 2 3 6.2 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12C/C(=C\c1ccccc1)[C@@H]3c1[nH]c3ccccc3c1C2 10.1021/jm030801n
CHEMBL108608 7312 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 488 2 2 3 6.2 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12C/C(=C\c1ccccc1)[C@@H]3c1[nH]c3ccccc3c1C2 10.1021/jm030801n
44255042 197634 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 378 4 1 3 4.2 CCN(CC)C(=O)c1ccc([C@@H]2CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL550471 197634 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 378 4 1 3 4.2 CCN(CC)C(=O)c1ccc([C@@H]2CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
155516812 176749 None 0 Human Functional pEC50 = 7.4 7.4 -5 2
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 473 9 3 5 4.1 CCOc1ccc(CN2Cc3ccccc3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4443716 176749 None 0 Human Functional pEC50 = 7.4 7.4 -5 2
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 473 9 3 5 4.1 CCOc1ccc(CN2Cc3ccccc3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4597980 176749 None 0 Human Functional pEC50 = 7.4 7.4 -5 2
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 473 9 3 5 4.1 CCOc1ccc(CN2Cc3ccccc3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
10273422 205510 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 416 7 0 2 6.0 CCCN1C2CCC1CC(=C(c1ccccc1)c1ccc(C(=O)N(CC)CC)cc1)C2 10.1016/j.bmcl.2004.02.051
CHEMBL63571 205510 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 416 7 0 2 6.0 CCCN1C2CCC1CC(=C(c1ccccc1)c1ccc(C(=O)N(CC)CC)cc1)C2 10.1016/j.bmcl.2004.02.051
168282639 191074 None 0 Human Functional pEC50 = 7.4 7.4 -6 3
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 5 1 4 4.1 CN(C(=O)Cc1ccccc1)[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
CHEMBL5185996 191074 None 0 Human Functional pEC50 = 7.4 7.4 -6 3
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 5 1 4 4.1 CN(C(=O)Cc1ccccc1)[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
10788323 167943 None 0 Human Functional pEC50 = 7.4 7.4 3 4
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 421 8 1 4 4.1 C=CCN1C[C@H](C)N([C@H](c2ccc(C(=O)NCC)cc2)c2cccc(OC)c2)C[C@H]1C 10.1021/acs.jmedchem.2c01061
CHEMBL430851 167943 None 0 Human Functional pEC50 = 7.4 7.4 3 4
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 421 8 1 4 4.1 C=CCN1C[C@H](C)N([C@H](c2ccc(C(=O)NCC)cc2)c2cccc(OC)c2)C[C@H]1C 10.1021/acs.jmedchem.2c01061
168291710 192066 None 0 Rat Functional pEC50 = 7.4 7.4 2 2
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 423 5 0 5 3.5 COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)C=O)[C@@H](C2)N(CC2CC2)CC[C@]315 10.1021/acs.jmedchem.2c00014
CHEMBL5200910 192066 None 0 Rat Functional pEC50 = 7.4 7.4 2 2
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 423 5 0 5 3.5 COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)C=O)[C@@H](C2)N(CC2CC2)CC[C@]315 10.1021/acs.jmedchem.2c00014
25257431 180145 None 0 Human Functional pEC50 = 6.4 6.4 -16 3
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 485 6 0 6 4.1 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(OC(=O)/C=C/c5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm8012272
CHEMBL474755 180145 None 0 Human Functional pEC50 = 6.4 6.4 -16 3
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 485 6 0 6 4.1 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(OC(=O)/C=C/c5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm8012272
89981608 160625 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 486 7 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1CNCc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL4112358 160625 None 0 Human Functional pEC50 = 6.4 6.4 -3 2
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 486 7 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1CNCc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
4305845 36816 None 11 Human Functional pEC50 = 4.4 4.4 1 2
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 303 2 1 4 3.2 O=c1c2ccc(Cl)cc2[nH]c(=S)n1Cc1cccnc1 nan
CHEMBL1450071 36816 None 11 Human Functional pEC50 = 4.4 4.4 1 2
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 303 2 1 4 3.2 O=c1c2ccc(Cl)cc2[nH]c(=S)n1Cc1cccnc1 nan
44406225 72831 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 COc1cccc(NC(=O)N2CCC(c3ccccc3)(c3nccn3Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2005.09.025
CHEMBL200098 72831 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 COc1cccc(NC(=O)N2CCC(c3ccccc3)(c3nccn3Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2005.09.025
11235302 123909 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 412 4 3 4 3.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc2ccccc2[nH]1 10.1021/jm030548r
CHEMBL362514 123909 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 412 4 3 4 3.5 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc2ccccc2[nH]1 10.1021/jm030548r
CHEMBL2151734 211749 None 0 Human Functional pEC50 = 5.4 5.4 -54954 4
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 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(C)[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)CC(N)=O 10.1021/jm200894e
253793 10559 None 31 Human Functional pEC50 = 4.4 4.4 1 2
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 594 2 2 8 6.6 COc1cc2c3cc1Oc1cc(ccc1O)C[C@@H]1c4c(cc(OC)c(O)c4Oc4ccc(cc4)C[C@H]3N(C)CC2)CCN1C nan
CHEMBL1169627 10559 None 31 Human Functional pEC50 = 4.4 4.4 1 2
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 594 2 2 8 6.6 COc1cc2c3cc1Oc1cc(ccc1O)C[C@@H]1c4c(cc(OC)c(O)c4Oc4ccc(cc4)C[C@H]3N(C)CC2)CCN1C nan
44254956 197781 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 422 2 1 3 4.8 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1Cc2ccccc2C1 10.1021/jm900773n
CHEMBL551613 197781 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 422 2 1 3 4.8 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1Cc2ccccc2C1 10.1021/jm900773n
122182783 122385 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 442 1 3 4 3.7 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CC(F)(F)F)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL3596367 122385 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 442 1 3 4 3.7 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CC(F)(F)F)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL3598303 122385 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 442 1 3 4 3.7 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CC(F)(F)F)CC[C@]314 10.1016/j.bmcl.2015.05.038
66826321 160082 None 0 Human Functional pEC50 = 7.3 7.3 2 2
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 574 11 2 7 4.6 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1cccc(NCC(=O)O)c1)C2 nan
CHEMBL4107681 160082 None 0 Human Functional pEC50 = 7.3 7.3 2 2
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 574 11 2 7 4.6 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1cccc(NCC(=O)O)c1)C2 nan
44254504 198917 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 376 4 2 3 4.0 CC(C)CNC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL563137 198917 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 376 4 2 3 4.0 CC(C)CNC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
23723457 54842 None 39 Human Functional pEC50 = 5.4 5.4 -1 2
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 408 8 1 4 4.4 CCOC(=O)C1(CCc2ccccc2)CCN(Cc2ccc(NC(C)=O)cc2)CC1 nan
CHEMBL1612697 54842 None 39 Human Functional pEC50 = 5.4 5.4 -1 2
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 408 8 1 4 4.4 CCOC(=O)C1(CCc2ccccc2)CCN(Cc2ccc(NC(C)=O)cc2)CC1 nan
162649323 180123 None 0 Human Functional pEC50 = 6.3 6.3 -30 4
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 1338 36 16 16 0.9 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](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2cccc(O)c2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4747286 180123 None 0 Human Functional pEC50 = 6.3 6.3 -30 4
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 1338 36 16 16 0.9 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](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2cccc(O)c2)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL3582484 214255 None 0 Human Functional pEC50 = 6.3 6.3 -630 6
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](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/acsmedchemlett.5b00056
12988885 206031 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 351 6 1 3 4.1 CCN(CC)C(=O)c1ccc(N(c2ccccc2)C2CCNCC2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL66755 206031 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 351 6 1 3 4.1 CCN(CC)C(=O)c1ccc(N(c2ccccc2)C2CCNCC2)cc1 10.1016/j.bmcl.2004.02.051
73354965 90505 None 0 Human Functional pEC50 = 7.3 7.3 -5 3
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 832 20 7 9 1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
CHEMBL2387210 90505 None 0 Human Functional pEC50 = 7.3 7.3 -5 3
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 832 20 7 9 1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
10787424 18785 None 0 Human Functional pEC50 = 7.3 7.3 239 3
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 404 8 0 2 5.9 CCCCN1CCC(=C(c2ccccc2)c2ccc(C(=O)N(CC)CC)cc2)CC1 10.1021/jm000229p
CHEMBL127802 18785 None 0 Human Functional pEC50 = 7.3 7.3 239 3
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 404 8 0 2 5.9 CCCCN1CCC(=C(c2ccccc2)c2ccc(C(=O)N(CC)CC)cc2)CC1 10.1021/jm000229p
155512748 176765 None 0 Human Functional pEC50 = 6.3 6.3 2 2
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 437 9 3 5 3.0 CCOc1ccc(CN2CC3CC3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4437661 176765 None 0 Human Functional pEC50 = 6.3 6.3 2 2
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 437 9 3 5 3.0 CCOc1ccc(CN2CC3CC3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
CHEMBL4598102 176765 None 0 Human Functional pEC50 = 6.3 6.3 2 2
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 437 9 3 5 3.0 CCOc1ccc(CN2CC3CC3C2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1021/acs.jmedchem.9b01818
129188464 195438 None 0 Human Functional pEC50 = 5.3 5.3 -151 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CO)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
CHEMBL5403724 195438 None 0 Human Functional pEC50 = 5.3 5.3 -151 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CO)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
12419 2474 None 22 Human Functional pEC50 = 5.3 5.3 -12022 4
Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
24800108 2474 None 22 Human Functional pEC50 = 5.3 5.3 -12022 4
Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
CHEMBL481512 2474 None 22 Human Functional pEC50 = 5.3 5.3 -12022 4
Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
1614 2495 None 37 Human Functional pEC50 = 7.3 7.3 -6 5
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 None None None None 10.1016/j.bmcl.2007.01.092
443363 2495 None 37 Human Functional pEC50 = 7.3 7.3 -6 5
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 None None None None 10.1016/j.bmcl.2007.01.092
CHEMBL13786 2495 None 37 Human Functional pEC50 = 7.3 7.3 -6 5
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 None None None None 10.1016/j.bmcl.2007.01.092
DB12668 2495 None 37 Human Functional pEC50 = 7.3 7.3 -6 5
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 None None None None 10.1016/j.bmcl.2007.01.092
44254954 198720 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 404 4 1 3 4.9 CC(C)N(C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)C(C)C 10.1021/jm900773n
CHEMBL561882 198720 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 404 4 1 3 4.9 CC(C)N(C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)C(C)C 10.1021/jm900773n
71605756 87536 None 0 Human Functional pEC50 = 7.3 7.3 -48 2
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 640 12 6 7 2.4 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1)c1ccco1 10.1021/jm400195y
CHEMBL2334775 87536 None 0 Human Functional pEC50 = 7.3 7.3 -48 2
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 640 12 6 7 2.4 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1)c1ccco1 10.1021/jm400195y
71605588 87537 None 0 Human Functional pEC50 = 7.3 7.3 -117 2
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 650 12 6 6 2.8 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCN(C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1)c1ccccc1 10.1021/jm400195y
CHEMBL2334776 87537 None 0 Human Functional pEC50 = 7.3 7.3 -117 2
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 650 12 6 6 2.8 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCN(C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1)c1ccccc1 10.1021/jm400195y
162660385 181310 None 0 Human Functional pEC50 = 6.3 6.3 -25 4
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 1358 40 14 15 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C 10.1021/acs.jmedchem.0c01376
CHEMBL4761165 181310 None 0 Human Functional pEC50 = 6.3 6.3 -25 4
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 1358 40 14 15 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C 10.1021/acs.jmedchem.0c01376
71719454 87534 None 0 Human Functional pEC50 = 7.3 7.3 -91 2
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 641 12 6 7 3.2 C=C(C(=O)O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)c1ccco1 10.1021/jm400195y
CHEMBL2334773 87534 None 0 Human Functional pEC50 = 7.3 7.3 -91 2
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 641 12 6 7 3.2 C=C(C(=O)O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)c1ccco1 10.1021/jm400195y
162668623 182723 None 0 Human Functional pEC50 = 7.3 7.3 1 5
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 1097 31 14 13 -2.2 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)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
CHEMBL4788431 182723 None 0 Human Functional pEC50 = 7.3 7.3 1 5
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 1097 31 14 13 -2.2 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)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
44253973 198998 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 376 4 1 3 4.1 CCN(CC)C(=O)c1ccc(C2=CC3(CCCNC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL563700 198998 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 376 4 1 3 4.1 CCN(CC)C(=O)c1ccc(C2=CC3(CCCNC3)Oc3ccccc32)cc1 10.1021/jm900773n
86711644 160491 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 7 1 6 3.7 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(NS(C)(=O)=O)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
CHEMBL4111233 160491 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
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 7 1 6 3.7 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(NS(C)(=O)=O)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
172442565 195027 None 0 Human Functional pEC50 = 6.3 6.3 -3 2
Inverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assayInverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
ChEMBL 608 11 1 8 7.3 COc1cccc(CNCc2nn(Cc3cccc(OC)c3)c3nc(-c4ccccc4Cl)c4cc(OC)c(OC)cc4c23)c1 10.1021/acs.jmedchem.3c00064
CHEMBL5395170 195027 None 0 Human Functional pEC50 = 6.3 6.3 -3 2
Inverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assayInverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
ChEMBL 608 11 1 8 7.3 COc1cccc(CNCc2nn(Cc3cccc(OC)c3)c3nc(-c4ccccc4Cl)c4cc(OC)c(OC)cc4c23)c1 10.1021/acs.jmedchem.3c00064
162668843 182695 None 0 Human Functional pEC50 = 6.3 6.3 -2 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4788060 182695 None 0 Human Functional pEC50 = 6.3 6.3 -2 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
1647 1313 None 34 Rat Functional pEC50 = 7.3 7.3 -70 9
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None None 10.1016/j.bmcl.2018.05.015
5462471 1313 None 34 Rat Functional pEC50 = 7.3 7.3 -70 9
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None None 10.1016/j.bmcl.2018.05.015
CHEMBL113995 1313 None 34 Rat Functional pEC50 = 7.3 7.3 -70 9
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None None 10.1016/j.bmcl.2018.05.015
CHEMBL38874 1313 None 34 Rat Functional pEC50 = 7.3 7.3 -70 9
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None None 10.1016/j.bmcl.2018.05.015
145961816 161705 None 0 Rat Functional pEC50 = 7.3 7.3 -1230 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 650 16 9 8 0.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1-c1ccsc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4129689 161705 None 0 Rat Functional pEC50 = 7.3 7.3 -1230 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 650 16 9 8 0.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1-c1ccsc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
162649449 180159 None 0 Human Functional pEC50 = 7.3 7.3 -29 3
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 421 8 1 4 5.1 CCOC(=O)CC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
CHEMBL4747769 180159 None 0 Human Functional pEC50 = 7.3 7.3 -29 3
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 421 8 1 4 5.1 CCOC(=O)CC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
162668623 182723 None 0 Human Functional pEC50 = 7.3 7.3 1 5
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 1097 31 14 13 -2.2 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)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
CHEMBL4788431 182723 None 0 Human Functional pEC50 = 7.3 7.3 1 5
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 1097 31 14 13 -2.2 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)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
56658044 65727 None 0 Human Functional pEC50 = 7.3 7.3 -9 4
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834413 65727 None 0 Human Functional pEC50 = 7.3 7.3 -9 4
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
172470496 197131 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Inverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assayInverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
ChEMBL 670 12 1 8 9.1 COc1cccc(Cn2nc(CNCc3cccc(Oc4ccccc4)c3)c3c4cc(OC)c(OC)cc4c(-c4ccccc4Cl)nc32)c1 10.1021/acs.jmedchem.3c00064
CHEMBL5439465 197131 None 0 Human Functional pEC50 = 7.3 7.3 -5 2
Inverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assayInverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
ChEMBL 670 12 1 8 9.1 COc1cccc(Cn2nc(CNCc3cccc(Oc4ccccc4)c3)c3c4cc(OC)c(OC)cc4c(-c4ccccc4Cl)nc32)c1 10.1021/acs.jmedchem.3c00064
162668843 182695 None 0 Human Functional pEC50 = 6.3 6.3 -2 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4788060 182695 None 0 Human Functional pEC50 = 6.3 6.3 -2 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
172439310 194978 None 0 Human Functional pEC50 = 6.3 6.3 -9 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 515 6 1 4 7.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CNC(=O)c4ccc(C(F)(F)F)o4)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
CHEMBL5394355 194978 None 0 Human Functional pEC50 = 6.3 6.3 -9 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 515 6 1 4 7.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CNC(=O)c4ccc(C(F)(F)F)o4)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
16188374 52194 None 5 Human Functional pEC50 = 4.3 4.3 -3 2
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 403 6 1 5 4.9 Cc1ccc(-n2cc(CNC(C)c3cnn(C)c3C)c(-c3ccc(F)cc3)n2)cc1 nan
CHEMBL1588202 52194 None 5 Human Functional pEC50 = 4.3 4.3 -3 2
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 403 6 1 5 4.9 Cc1ccc(-n2cc(CNC(C)c3cnn(C)c3C)c(-c3ccc(F)cc3)n2)cc1 nan
44380504 59085 None 0 Human Functional pEC50 = 8.3 8.3 -4 3
Activity was evaluated in human delta opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human delta opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay
ChEMBL 427 2 2 5 3.6 CO[C@@]12CCC3(C[C@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@H]2O5 10.1016/s0960-894x(99)00085-2
CHEMBL169552 59085 None 0 Human Functional pEC50 = 8.3 8.3 -4 3
Activity was evaluated in human delta opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human delta opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay
ChEMBL 427 2 2 5 3.6 CO[C@@]12CCC3(C[C@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@H]2O5 10.1016/s0960-894x(99)00085-2
44573249 192765 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 423 4 2 5 4.4 Nc1ccnc(N2CCC(C(=O)Nc3ccc4ccccc4n3)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL521830 192765 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 423 4 2 5 4.4 Nc1ccnc(N2CCC(C(=O)Nc3ccc4ccccc4n3)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2009.01.106
155546429 173640 None 0 Human Functional pEC50 = 8.3 8.3 -1 4
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 556 15 6 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)O 10.1021/acs.jmedchem.0c00530
CHEMBL4531563 173640 None 0 Human Functional pEC50 = 8.3 8.3 -1 4
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 556 15 6 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)O 10.1021/acs.jmedchem.0c00530
44177145 198184 None 0 Human Functional pEC50 = 8.3 8.3 4 4
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 1191 27 10 10 5.4 CCCC[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](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/jm900473p
CHEMBL557188 198184 None 0 Human Functional pEC50 = 8.3 8.3 4 4
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 1191 27 10 10 5.4 CCCC[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](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/jm900473p
16224613 103843 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 390 5 2 3 4.6 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3)c2ccc(O)cc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL308928 103843 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 390 5 2 3 4.6 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3)c2ccc(O)cc2)cc1 10.1016/j.bmcl.2004.02.051
11849360 204296 None 0 Human Functional pEC50 = 8.3 8.3 -5 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 478 4 1 5 3.5 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(Cl)cc5)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
CHEMBL607069 204296 None 0 Human Functional pEC50 = 8.3 8.3 -5 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 478 4 1 5 3.5 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(Cl)cc5)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
44177145 198184 None 0 Human Functional pEC50 = 8.3 8.3 4 4
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 1191 27 10 10 5.4 CCCC[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](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/jm900473p
CHEMBL557188 198184 None 0 Human Functional pEC50 = 8.3 8.3 4 4
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 1191 27 10 10 5.4 CCCC[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](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/jm900473p
46227963 14181 None 0 Human Functional pEC50 = 8.3 8.3 1 4
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 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198701 14181 None 0 Human Functional pEC50 = 8.3 8.3 1 4
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 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611929 14181 None 0 Human Functional pEC50 = 8.3 8.3 1 4
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 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
44551464 14183 None 0 Human Functional pEC50 = 8.3 8.3 -1 4
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 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198703 14183 None 0 Human Functional pEC50 = 8.3 8.3 -1 4
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 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611931 14183 None 0 Human Functional pEC50 = 8.3 8.3 -1 4
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 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
127049273 141102 None 0 Rat Functional pEC50 = 8.3 8.3 -2 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 511 7 3 4 4.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CCC2)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
CHEMBL3823787 141102 None 0 Rat Functional pEC50 = 8.3 8.3 -2 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 511 7 3 4 4.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CCC2)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.6b00308
11250396 145733 None 0 Human Functional pEC50 = 8.3 8.3 26 2
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 600 17 7 8 -1.1 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(C(N)=O)cc1)C(=O)O 10.1016/j.bmcl.2007.01.092
CHEMBL391580 145733 None 0 Human Functional pEC50 = 8.3 8.3 26 2
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 600 17 7 8 -1.1 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(C(N)=O)cc1)C(=O)O 10.1016/j.bmcl.2007.01.092
1639 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2014.05.065
1765 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2014.05.065
5360515 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2014.05.065
5360515.0 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2014.05.065
CHEMBL19019 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2014.05.065
DB00704 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
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 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2014.05.065
1639 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
1765 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
5360515 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
5360515.0 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
CHEMBL19019 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
DB00704 2726 None 32 Human Functional pEC50 = 8.3 8.3 -25 9
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
CHEMBL2419539 212899 None 0 Human Functional pEC50 = 8.3 8.3 1 3
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)NC(C)(C)C(=O)N[C@@H](CC(C)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.2013.06.065
71457292 82749 None 0 Human Functional pEC50 = 8.3 8.3 8 3
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 578 5 1 6 6.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2ncc(-c4ccc(Cl)cc4)cc2C[C@@]3(OC(=O)CCc2ccccc2)[C@H]1C5 10.1021/jm300686p
CHEMBL2179662 82749 None 0 Human Functional pEC50 = 8.3 8.3 8 3
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 578 5 1 6 6.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2ncc(-c4ccc(Cl)cc4)cc2C[C@@]3(OC(=O)CCc2ccccc2)[C@H]1C5 10.1021/jm300686p
44408483 169032 None 0 Human Functional pEC50 = 8.3 8.3 12 5
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 1212 31 12 15 3.7 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL438739 169032 None 0 Human Functional pEC50 = 8.3 8.3 12 5
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 1212 31 12 15 3.7 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
44408483 169032 None 0 Human Functional pEC50 = 8.3 8.3 12 5
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 1212 31 12 15 3.7 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL438739 169032 None 0 Human Functional pEC50 = 8.3 8.3 12 5
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 1212 31 12 15 3.7 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
73354966 90596 None 0 Human Functional pEC50 = 8.2 8.2 3 3
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 903 23 7 9 3.4 CC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
CHEMBL2387339 90596 None 0 Human Functional pEC50 = 8.2 8.2 3 3
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 903 23 7 9 3.4 CC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
155555053 176667 None 0 Rat Functional pEC50 = 8.2 8.2 -5 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 522 6 3 5 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cnc4ccccc4c3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL4550332 176667 None 0 Rat Functional pEC50 = 8.2 8.2 -5 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 522 6 3 5 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cnc4ccccc4c3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597317 176667 None 0 Rat Functional pEC50 = 8.2 8.2 -5 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 522 6 3 5 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cnc4ccccc4c3)ccc21 10.1021/acs.jmedchem.9b00378
145963297 161714 None 0 Rat Functional pEC50 = 8.2 8.2 -22 3
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 509 12 6 6 0.4 C=Cc1ccccc1C[C@H](NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4129901 161714 None 0 Rat Functional pEC50 = 8.2 8.2 -22 3
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 509 12 6 6 0.4 C=Cc1ccccc1C[C@H](NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
122182787 122378 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 414 2 2 5 3.6 CCCN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2nc4ccccc4cc2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2015.05.038
CHEMBL3596369 122378 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 414 2 2 5 3.6 CCCN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2nc4ccccc4cc2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2015.05.038
CHEMBL3598211 122378 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 414 2 2 5 3.6 CCCN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2nc4ccccc4cc2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2015.05.038
45486012 199870 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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(CCc3ccncc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL569529 199870 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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(CCc3ccncc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL262172 212987 None 0 Human Functional pEC50 = 8.2 8.2 7 5
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
CHEMBL262172 212987 None 0 Human Functional pEC50 = 8.2 8.2 7 5
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
16100407 82703 None 0 Human Functional pEC50 = 8.2 8.2 4 4
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
CHEMBL217957 82703 None 0 Human Functional pEC50 = 8.2 8.2 4 4
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
71625601 90598 None 0 Human Functional pEC50 = 8.2 8.2 -10 3
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 888 22 7 9 3.0 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)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
CHEMBL2387341 90598 None 0 Human Functional pEC50 = 8.2 8.2 -10 3
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 888 22 7 9 3.0 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)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
10809678 98809 None 0 Human Functional pEC50 = 8.2 8.2 1445 2
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)c2ccccc2OC)cc1 10.1021/jm000229p
CHEMBL278078 98809 None 0 Human Functional pEC50 = 8.2 8.2 1445 2
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)c2ccccc2OC)cc1 10.1021/jm000229p
168275900 190561 None 0 Human Functional pEC50 = 8.2 8.2 -1 3
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 5 2 4 3.7 O=C(Cc1ccccc1)N[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
CHEMBL5178511 190561 None 0 Human Functional pEC50 = 8.2 8.2 -1 3
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 5 2 4 3.7 O=C(Cc1ccccc1)N[C@@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2 10.1016/j.bmc.2021.116552
CHEMBL426363 215806 None 0 Human Functional pEC50 = 7.3 7.3 -18 4
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)CNC(=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
54756989 65724 None 0 Human Functional pEC50 = 7.3 7.3 -19 2
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 481 5 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834410 65724 None 0 Human Functional pEC50 = 7.3 7.3 -19 2
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 481 5 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL426363 215806 None 0 Human Functional pEC50 = 7.3 7.3 -18 4
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)CNC(=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
11361718 127618 None 0 Mouse Functional pEC50 = 6.3 6.3 1 2
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 404 5 3 4 3.7 Cc1[nH]c([C@@H]2CCCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1-c1ccccc1 10.1016/j.bmcl.2006.01.082
CHEMBL366311 127618 None 0 Mouse Functional pEC50 = 6.3 6.3 1 2
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 404 5 3 4 3.7 Cc1[nH]c([C@@H]2CCCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1-c1ccccc1 10.1016/j.bmcl.2006.01.082
1627 2594 None 9 Human Functional pEC50 = 6.3 6.3 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2013.06.084
1845 2594 None 9 Human Functional pEC50 = 6.3 6.3 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2013.06.084
5288826 2594 None 9 Human Functional pEC50 = 6.3 6.3 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2013.06.084
5288826.0 2594 None 9 Human Functional pEC50 = 6.3 6.3 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2013.06.084
CHEMBL70 2594 None 9 Human Functional pEC50 = 6.3 6.3 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2013.06.084
DB00295 2594 None 9 Human Functional pEC50 = 6.3 6.3 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2013.06.084
3556099 29033 None 4 Human Functional pEC50 = 4.3 4.3 -12 2
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 327 5 2 2 4.3 Cc1ccc(C)c(NC(S)=NCC(c2ccccc2)N(C)C)c1 nan
CHEMBL1380599 29033 None 4 Human Functional pEC50 = 4.3 4.3 -12 2
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 327 5 2 2 4.3 Cc1ccc(C)c(NC(S)=NCC(c2ccccc2)N(C)C)c1 nan
10279008 102832 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 506 8 0 2 7.6 CC(C)N(C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1)C(C)C 10.1016/j.bmcl.2004.02.051
CHEMBL305225 102832 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 506 8 0 2 7.6 CC(C)N(C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1)C(C)C 10.1016/j.bmcl.2004.02.051
46227360 205039 None 0 Human Functional pEC50 = 7.3 7.3 -4 5
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 18 10 12 4.6 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
CHEMBL611924 205039 None 0 Human Functional pEC50 = 7.3 7.3 -4 5
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 18 10 12 4.6 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
44233184 194880 None 0 Human Functional pEC50 = 7.3 7.3 -11 5
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 1343 32 15 16 1.7 CCCC[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](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=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/jm900473p
CHEMBL538131 194880 None 0 Human Functional pEC50 = 7.3 7.3 -11 5
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 1343 32 15 16 1.7 CCCC[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](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=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/jm900473p
46227360 205039 None 0 Human Functional pEC50 = 7.3 7.3 -4 5
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 18 10 12 4.6 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
CHEMBL611924 205039 None 0 Human Functional pEC50 = 7.3 7.3 -4 5
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 18 10 12 4.6 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
44233410 198050 None 0 Human Functional pEC50 = 7.3 7.3 -15 4
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 1327 28 14 16 1.0 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)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)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
CHEMBL555504 198050 None 0 Human Functional pEC50 = 7.3 7.3 -15 4
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 1327 28 14 16 1.0 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)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)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
CHEMBL3582487 214258 None 0 Human Functional pEC50 = 7.3 7.3 -85 6
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)cc2)C(=O)N1 10.1021/acsmedchemlett.5b00056
71720682 87533 None 0 Human Functional pEC50 = 7.3 7.3 -93 2
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 651 12 6 6 3.6 C=C(C(=O)O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)c1ccccc1 10.1021/jm400195y
CHEMBL2334772 87533 None 0 Human Functional pEC50 = 7.3 7.3 -93 2
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 651 12 6 6 3.6 C=C(C(=O)O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)c1ccccc1 10.1021/jm400195y
168296853 192551 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
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 444 4 2 4 3.8 O=C(N[C@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2)c1ccccc1 10.1016/j.bmc.2021.116552
CHEMBL5208385 192551 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
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 444 4 2 4 3.8 O=C(N[C@H]1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]32CC[C@@H]1O2)c1ccccc1 10.1016/j.bmc.2021.116552
23635163 88539 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
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 642 15 6 7 1.4 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NC1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
CHEMBL235106 88539 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
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 642 15 6 7 1.4 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NC1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
162670510 183084 None 0 Human Functional pEC50 = 6.3 6.3 -29 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4793250 183084 None 0 Human Functional pEC50 = 6.3 6.3 -29 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
23635163 88539 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
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 642 15 6 7 1.4 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NC1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
CHEMBL235106 88539 None 0 Human Functional pEC50 = 6.3 6.3 -2 3
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 642 15 6 7 1.4 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NC1CCN(CCc2ccccc2)CC1 10.1021/jm061465o
3730844 51592 None 11 Human Functional pEC50 = 4.3 4.3 - 1
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 369 4 0 4 5.0 Clc1ccc(-c2nc3ncccc3n2OCc2ccccc2)c(Cl)c1 nan
CHEMBL1583291 51592 None 11 Human Functional pEC50 = 4.3 4.3 - 1
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 369 4 0 4 5.0 Clc1ccc(-c2nc3ncccc3n2OCc2ccccc2)c(Cl)c1 nan
162670510 183084 None 0 Human Functional pEC50 = 6.3 6.3 -29 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4793250 183084 None 0 Human Functional pEC50 = 6.3 6.3 -29 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
25208097 184028 None 1 Human Functional pEC50 = 6.3 6.3 -61 4
Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481366 184028 None 1 Human Functional pEC50 = 6.3 6.3 -61 4
Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
44573405 187493 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 403 5 1 6 3.4 COc1cccc(C(=O)N(c2ccccn2)C2CCN(c3cc(N)ccn3)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL493517 187493 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 403 5 1 6 3.4 COc1cccc(C(=O)N(c2ccccn2)C2CCN(c3cc(N)ccn3)CC2)c1 10.1016/j.bmcl.2009.01.106
44233410 198050 None 0 Human Functional pEC50 = 7.3 7.3 -15 4
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 1327 28 14 16 1.0 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)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)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
CHEMBL555504 198050 None 0 Human Functional pEC50 = 7.3 7.3 -15 4
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 1327 28 14 16 1.0 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)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)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
11015676 204226 None 0 Mouse Functional pEC50 = 7.3 7.3 - 1
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 440 4 3 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc2ccccc2[nH]1 10.1021/jm010449i
CHEMBL606737 204226 None 0 Mouse Functional pEC50 = 7.3 7.3 - 1
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 440 4 3 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc2ccccc2[nH]1 10.1021/jm010449i
91801212 114835 None 0 Human Functional pEC50 = 7.3 7.3 -5 3
Agonist activity at human DOR expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 355 2 2 6 2.6 C[C@@]1(c2ccccc2O)O[C@@H]2N3[C@H](CO[C@H]31)O[C@]2(C)c1ccccc1O 10.1016/j.bmcl.2014.08.012
CHEMBL3338874 114835 None 0 Human Functional pEC50 = 7.3 7.3 -5 3
Agonist activity at human DOR expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 355 2 2 6 2.6 C[C@@]1(c2ccccc2O)O[C@@H]2N3[C@H](CO[C@H]31)O[C@]2(C)c1ccccc1O 10.1016/j.bmcl.2014.08.012
118725848 117236 None 0 Human Functional pEC50 = 5.3 5.3 -239 3
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 390 5 1 5 4.6 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1cc2ccccc2s1 10.1016/j.bmcl.2014.12.064
CHEMBL3393998 117236 None 0 Human Functional pEC50 = 5.3 5.3 -239 3
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 390 5 1 5 4.6 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1cc2ccccc2s1 10.1016/j.bmcl.2014.12.064
86711651 160715 None 0 Human Functional pEC50 = 6.3 6.3 -61 3
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 500 8 1 5 4.7 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CNCc1ccccc1)C2 nan
CHEMBL4113058 160715 None 0 Human Functional pEC50 = 6.3 6.3 -61 3
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 500 8 1 5 4.7 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CNCc1ccccc1)C2 nan
9820950 205501 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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
CHEMBL63477 205501 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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
CHEMBL3759179 214689 None 0 Human Functional pEC50 = 7.3 7.3 -14 3
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2015.12.012
49863733 15338 None 0 Human Functional pEC50 = 6.3 6.3 -3 5
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
CHEMBL1214026 15338 None 0 Human Functional pEC50 = 6.3 6.3 -3 5
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
49863733 15338 None 0 Human Functional pEC50 = 6.3 6.3 -3 5
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
CHEMBL1214026 15338 None 0 Human Functional pEC50 = 6.3 6.3 -3 5
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
44408525 169531 None 0 Human Functional pEC50 = 7.3 7.3 -1 4
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 1075 30 12 14 1.5 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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
CHEMBL442483 169531 None 0 Human Functional pEC50 = 7.3 7.3 -1 4
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 1075 30 12 14 1.5 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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
23723457 54842 None 39 Human Functional pEC50 = 7.3 7.3 -1 2
Inhibition of delta opioid receptor (unknown origin) expressed in human UO5S cells by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) expressed in human UO5S cells by [35S]-GTPgammaS binding assay
ChEMBL 408 8 1 4 4.4 CCOC(=O)C1(CCc2ccccc2)CCN(Cc2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2019.111701
CHEMBL1612697 54842 None 39 Human Functional pEC50 = 7.3 7.3 -1 2
Inhibition of delta opioid receptor (unknown origin) expressed in human UO5S cells by [35S]-GTPgammaS binding assayInhibition of delta opioid receptor (unknown origin) expressed in human UO5S cells by [35S]-GTPgammaS binding assay
ChEMBL 408 8 1 4 4.4 CCOC(=O)C1(CCc2ccccc2)CCN(Cc2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2019.111701
168269548 190054 None 0 Human Functional pEC50 = 7.3 7.3 -8 3
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
CHEMBL5170301 190054 None 0 Human Functional pEC50 = 7.3 7.3 -8 3
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
44408525 169531 None 0 Human Functional pEC50 = 7.3 7.3 -1 4
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 1075 30 12 14 1.5 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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
CHEMBL442483 169531 None 0 Human Functional pEC50 = 7.3 7.3 -1 4
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 1075 30 12 14 1.5 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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
11361718 127618 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 404 5 3 4 3.7 Cc1[nH]c([C@@H]2CCCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1-c1ccccc1 10.1021/jm030548r
CHEMBL366311 127618 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 404 5 3 4 3.7 Cc1[nH]c([C@@H]2CCCCN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1-c1ccccc1 10.1021/jm030548r
CHEMBL5085455 217457 None 0 Human Functional pEC50 = 6.3 6.3 -14 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
16224211 206178 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 494 9 1 3 5.8 CCN(CCO)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL67673 206178 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 494 9 1 3 5.8 CCN(CCO)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL5085455 217457 None 0 Human Functional pEC50 = 6.3 6.3 -14 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
16094344 169045 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 335 2 1 2 4.9 C[C@H]1[C@@H]2CC[C@@H](c3ccccc3)CN2CC[C@@]1(C)c1cccc(O)c1 10.1021/jm060486f
CHEMBL438821 169045 None 0 Human Functional pEC50 = 7.3 7.3 -1 3
Agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 335 2 1 2 4.9 C[C@H]1[C@@H]2CC[C@@H](c3ccccc3)CN2CC[C@@]1(C)c1cccc(O)c1 10.1021/jm060486f
44367182 44094 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity tested in [35S]GTP-gamma-S, Recombinant Human Opioid receptor delta 1 transfected in to CHO cells for the displacement of [3H]Cl-DPDPE (delta)Partial agonist activity tested in [35S]GTP-gamma-S, Recombinant Human Opioid receptor delta 1 transfected in to CHO cells for the displacement of [3H]Cl-DPDPE (delta)
ChEMBL 490 3 2 5 4.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c(-c4ccccc4)cn2Cc2ccccc2)C[C@@]3(O)C1C5 10.1021/jm010841w
CHEMBL151476 44094 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Partial agonist activity tested in [35S]GTP-gamma-S, Recombinant Human Opioid receptor delta 1 transfected in to CHO cells for the displacement of [3H]Cl-DPDPE (delta)Partial agonist activity tested in [35S]GTP-gamma-S, Recombinant Human Opioid receptor delta 1 transfected in to CHO cells for the displacement of [3H]Cl-DPDPE (delta)
ChEMBL 490 3 2 5 4.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c(-c4ccccc4)cn2Cc2ccccc2)C[C@@]3(O)C1C5 10.1021/jm010841w
118725745 117219 None 0 Human Functional pEC50 = 5.3 5.3 -75 3
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 359 5 1 5 3.3 N#Cc1cccc(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)c1 10.1016/j.bmcl.2014.12.064
CHEMBL3393885 117219 None 0 Human Functional pEC50 = 5.3 5.3 -75 3
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 359 5 1 5 3.3 N#Cc1cccc(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)c1 10.1016/j.bmcl.2014.12.064
5311353 204332 None 2 Human Functional pEC50 = 6.3 6.3 - 1
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 321 3 1 2 4.2 CC1[C@H]2Cc3ccc(O)cc3[C@]1(C)CCN2CCc1ccccc1 nan
CHEMBL1604493 204332 None 2 Human Functional pEC50 = 6.3 6.3 - 1
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 321 3 1 2 4.2 CC1[C@H]2Cc3ccc(O)cc3[C@]1(C)CCN2CCc1ccccc1 nan
CHEMBL607317 204332 None 2 Human Functional pEC50 = 6.3 6.3 - 1
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 321 3 1 2 4.2 CC1[C@H]2Cc3ccc(O)cc3[C@]1(C)CCN2CCc1ccccc1 nan
89978553 160058 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
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 520 5 0 7 5.5 COc1ccc2c3c1O[C@@H]1[C@]34CCN(C)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CSc1nc3ccccc3s1)C2 nan
CHEMBL4107470 160058 None 0 Human Functional pEC50 = 6.3 6.3 -1 3
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 520 5 0 7 5.5 COc1ccc2c3c1O[C@@H]1[C@]34CCN(C)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CSc1nc3ccccc3s1)C2 nan
145960967 161712 None 0 Rat Functional pEC50 = 7.3 7.3 -1 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 565 12 6 7 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1-c1ccsc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4129753 161712 None 0 Rat Functional pEC50 = 7.3 7.3 -1 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 565 12 6 7 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1-c1ccsc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
172466389 196630 None 0 Human Functional pEC50 = 7.3 7.3 -21 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5428360 196630 None 0 Human Functional pEC50 = 7.3 7.3 -21 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
162665640 182428 None 0 Human Functional pEC50 = 7.3 7.3 10 3
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 1097 31 14 13 -2.2 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)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
CHEMBL4784329 182428 None 0 Human Functional pEC50 = 7.3 7.3 10 3
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 1097 31 14 13 -2.2 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)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
162665640 182428 None 0 Human Functional pEC50 = 7.3 7.3 10 3
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 1097 31 14 13 -2.2 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)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
CHEMBL4784329 182428 None 0 Human Functional pEC50 = 7.3 7.3 10 3
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 1097 31 14 13 -2.2 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)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
86711648 160820 None 0 Human Functional pEC50 = 5.3 5.3 -1 2
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 553 8 0 7 5.2 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COc1ccc(-n3ccnc3)cc1)C2 nan
CHEMBL4113804 160820 None 0 Human Functional pEC50 = 5.3 5.3 -1 2
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 553 8 0 7 5.2 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COc1ccc(-n3ccnc3)cc1)C2 nan
3983975 55954 None 4 Human Functional pEC50 = 4.3 4.3 -1 2
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 458 7 1 4 4.4 CCOC(=O)C1(c2ccccc2)CCN(CCC(=O)Nc2cccc(Br)c2)CC1 nan
CHEMBL1513567 55954 None 4 Human Functional pEC50 = 4.3 4.3 -1 2
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 458 7 1 4 4.4 CCOC(=O)C1(c2ccccc2)CCN(CCC(=O)Nc2cccc(Br)c2)CC1 nan
CHEMBL1623859 55954 None 4 Human Functional pEC50 = 4.3 4.3 -1 2
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 458 7 1 4 4.4 CCOC(=O)C1(c2ccccc2)CCN(CCC(=O)Nc2cccc(Br)c2)CC1 nan
44433402 88572 None 0 Human Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assay
ChEMBL 387 2 3 6 1.2 CO[C@]12CC(O)[C@@]3(C[C@@H]1[C@@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1016/j.bmcl.2007.06.050
CHEMBL235239 88572 None 0 Human Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assay
ChEMBL 387 2 3 6 1.2 CO[C@]12CC(O)[C@@]3(C[C@@H]1[C@@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1016/j.bmcl.2007.06.050
66827067 160476 None 0 Human Functional pEC50 = 7.2 7.2 -5 3
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 633 17 0 8 5.2 COCCOCCOCCOc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
CHEMBL4111124 160476 None 0 Human Functional pEC50 = 7.2 7.2 -5 3
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 633 17 0 8 5.2 COCCOCCOCCOc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
66825501 160075 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 558 9 1 7 4.0 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COC(=O)[C@@H](N)Cc1ccccc1)C2 nan
CHEMBL4107627 160075 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 558 9 1 7 4.0 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COC(=O)[C@@H](N)Cc1ccccc1)C2 nan
132941097 183374 None 0 Human Functional pEC50 = 6.2 6.2 -14 5
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 1055 29 13 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCC(=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
CHEMBL4796596 183374 None 0 Human Functional pEC50 = 6.2 6.2 -14 5
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 1055 29 13 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCC(=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
CHEMBL5086463 217519 None 0 Human Functional pEC50 = 6.2 6.2 -3 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
132941097 183374 None 0 Human Functional pEC50 = 6.2 6.2 -14 5
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 1055 29 13 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCC(=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
CHEMBL4796596 183374 None 0 Human Functional pEC50 = 6.2 6.2 -14 5
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 1055 29 13 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCC(=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
172439679 195348 None 0 Human Functional pEC50 = 7.2 7.2 3 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1150 24 13 13 -0.4 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5401796 195348 None 0 Human Functional pEC50 = 7.2 7.2 3 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1150 24 13 13 -0.4 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL247759 212966 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc2nc(N)sc2c1)C(=O)O 10.1016/j.bmcl.2007.01.092
CHEMBL5086463 217519 None 0 Human Functional pEC50 = 6.2 6.2 -3 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
162647830 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
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 1112 32 15 14 -3.9 C[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
CHEMBL4745148 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
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 1112 32 15 14 -3.9 C[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
162647830 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[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.0c01367
CHEMBL4745148 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[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.0c01367
162647830 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[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.0c01367
CHEMBL4745148 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
Agonist activity at delta opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated 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 inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[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.0c01367
162647830 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
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 1112 32 15 14 -3.9 C[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
CHEMBL4745148 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
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 1112 32 15 14 -3.9 C[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
162647830 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
Agonist activity at delta-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at delta-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 1112 32 15 14 -3.9 C[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.0c00643
CHEMBL4745148 179947 None 0 Human Functional pEC50 = 6.2 6.2 -3 5
Agonist activity at delta-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at delta-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 1112 32 15 14 -3.9 C[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.0c00643
44573293 187302 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 436 5 2 5 4.3 COc1ccc(C(=O)NC2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)cc1Cl 10.1016/j.bmcl.2009.01.106
CHEMBL492330 187302 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 436 5 2 5 4.3 COc1ccc(C(=O)NC2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)cc1Cl 10.1016/j.bmcl.2009.01.106
16730656 187335 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 357 2 1 4 4.3 Nc1ccnc(N2CCC3(CC2)OC(c2ccccc2)c2ccccc23)c1 10.1016/j.bmcl.2009.01.106
CHEMBL492553 187335 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 357 2 1 4 4.3 Nc1ccnc(N2CCC3(CC2)OC(c2ccccc2)c2ccccc23)c1 10.1016/j.bmcl.2009.01.106
CHEMBL5084538 218035 None 2 Human Functional pEC50 = 7.2 7.2 -134 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccs1 10.1021/acs.jmedchem.2c00087
CHEMBL5095817 218035 None 2 Human Functional pEC50 = 7.2 7.2 -134 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccs1 10.1021/acs.jmedchem.2c00087
127028436 138365 None 0 Rat Functional pEC50 = 5.2 5.2 -151 3
Agonist activity at rat DOR expressed in rat C6 cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in rat C6 cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 429 6 4 4 4.1 Cc1cc(C[C@H](N)C(=O)N[C@@H]2CCNc3ccc(Cc4ccccc4)cc32)c(C)cc1O 10.1021/acsmedchemlett.5b00344
CHEMBL3770677 138365 None 0 Rat Functional pEC50 = 5.2 5.2 -151 3
Agonist activity at rat DOR expressed in rat C6 cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in rat C6 cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 429 6 4 4 4.1 Cc1cc(C[C@H](N)C(=O)N[C@@H]2CCNc3ccc(Cc4ccccc4)cc32)c(C)cc1O 10.1021/acsmedchemlett.5b00344
145982510 165503 None 0 Rat Functional pEC50 = 6.2 6.2 -8 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 529 7 0 6 5.2 COc1ccc(C(=O)[C@@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1 10.1016/j.bmc.2018.07.020
CHEMBL4238289 165503 None 0 Rat Functional pEC50 = 6.2 6.2 -8 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 529 7 0 6 5.2 COc1ccc(C(=O)[C@@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1 10.1016/j.bmc.2018.07.020
172450838 195593 None 0 Human Functional pEC50 = 8.2 8.2 -7 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1150 24 13 13 -0.4 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5406732 195593 None 0 Human Functional pEC50 = 8.2 8.2 -7 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1150 24 13 13 -0.4 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
72735388 106363 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 440 1 2 4 3.9 Oc1ccc2c(c1)[C@]13CCN(CC(F)(F)F)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL3139080 106363 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 440 1 2 4 3.9 Oc1ccc2c(c1)[C@]13CCN(CC(F)(F)F)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL4296724 106363 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 440 1 2 4 3.9 Oc1ccc2c(c1)[C@]13CCN(CC(F)(F)F)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
44279592 162608 None 0 Human Functional pEC50 = 8.2 8.2 -1 3
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 395 1 2 5 2.5 CO[C@]12C=CC3(CC14CCC[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm991165p
CHEMBL416765 162608 None 0 Human Functional pEC50 = 8.2 8.2 -1 3
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 395 1 2 5 2.5 CO[C@]12C=CC3(CC14CCC[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm991165p
CHEMBL5083572 218022 None 0 Human Functional pEC50 = 8.2 8.2 -2 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(Cc1ccco1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/acs.jmedchem.2c00087
CHEMBL5095617 218022 None 0 Human Functional pEC50 = 8.2 8.2 -2 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(Cc1ccco1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/acs.jmedchem.2c00087
71454362 84207 None 0 Human Functional pEC50 = 8.2 8.2 -6 3
Partial agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 538 9 1 4 6.3 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1OC 10.1016/j.bmcl.2012.10.081
CHEMBL2208350 84207 None 0 Human Functional pEC50 = 8.2 8.2 -6 3
Partial agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 538 9 1 4 6.3 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1OC 10.1016/j.bmcl.2012.10.081
CHEMBL294616 213353 None 0 Human Functional pEC50 = 8.2 8.2 -2 7
Agonist activity at human delta opioid receptor transfected in CHOK1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor transfected in CHOK1 cells after 60 mins 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/np300653d
104787 1473 None 17 Human Functional pEC50 = 8.2 8.2 -2 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
1608 1473 None 17 Human Functional pEC50 = 8.2 8.2 -2 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
CHEMBL31421 1473 None 17 Human Functional pEC50 = 8.2 8.2 -2 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
DB08861 1473 None 17 Human Functional pEC50 = 8.2 8.2 -2 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
90655826 111269 None 0 Human Functional pEC50 = 8.2 8.2 1 3
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 4 1 6 3.1 C=CCN1CC[C@@]23c4c5ccc(O)c4OCO[C@]46CC[C@@]2(O[C@H](C(=O)N4Cc2ccccc2)[C@H]63)[C@H]1C5 10.1021/ml400491k
CHEMBL3264745 111269 None 0 Human Functional pEC50 = 8.2 8.2 1 3
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 4 1 6 3.1 C=CCN1CC[C@@]23c4c5ccc(O)c4OCO[C@]46CC[C@@]2(O[C@H](C(=O)N4Cc2ccccc2)[C@H]63)[C@H]1C5 10.1021/ml400491k
72735566 106426 None 0 Human Functional pEC50 = 8.2 8.2 38 2
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
CHEMBL3139249 106426 None 0 Human Functional pEC50 = 8.2 8.2 38 2
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
CHEMBL4296739 106426 None 0 Human Functional pEC50 = 8.2 8.2 38 2
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
CHEMBL3609618 214292 None 0 Human Functional pEC50 = 8.2 8.2 1 3
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 None None None C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2015.06.030
122182785 122386 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 400 1 2 5 3.2 CCN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2nc4ccccc4cc2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2015.05.038
CHEMBL3596368 122386 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 400 1 2 5 3.2 CCN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2nc4ccccc4cc2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2015.05.038
CHEMBL3598304 122386 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 400 1 2 5 3.2 CCN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2nc4ccccc4cc2C[C@@]3(O)[C@H]1C5 10.1016/j.bmcl.2015.05.038
1647 1313 None 34 Human Functional pEC50 = 8.2 8.2 -19 9
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
5462471 1313 None 34 Human Functional pEC50 = 8.2 8.2 -19 9
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL113995 1313 None 34 Human Functional pEC50 = 8.2 8.2 -19 9
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL38874 1313 None 34 Human Functional pEC50 = 8.2 8.2 -19 9
Partial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human DOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
16083041 78091 None 0 Human Functional pEC50 = 8.2 8.2 -2 3
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTP-gamma-S bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTP-gamma-S binding
ChEMBL 478 7 1 2 6.3 C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5)cc4)cc3[C@]1(C)CCN2CC1CC1 10.1021/jm060278n
CHEMBL210005 78091 None 0 Human Functional pEC50 = 8.2 8.2 -2 3
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTP-gamma-S bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTP-gamma-S binding
ChEMBL 478 7 1 2 6.3 C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5)cc4)cc3[C@]1(C)CCN2CC1CC1 10.1021/jm060278n
44573294 193163 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 373 4 2 5 3.0 Nc1ccnc(N2CCC(NC(=O)c3ccccn3)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL522317 193163 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 373 4 2 5 3.0 Nc1ccnc(N2CCC(NC(=O)c3ccccn3)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2009.01.106
16046123 80322 None 0 Human Functional pEC50 = 7.2 7.2 2 3
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 789 19 6 8 2.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
CHEMBL214022 80322 None 0 Human Functional pEC50 = 7.2 7.2 2 3
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 789 19 6 8 2.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
CHEMBL2387337 80322 None 0 Human Functional pEC50 = 7.2 7.2 2 3
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 789 19 6 8 2.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
86711647 160420 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 539 7 1 7 4.9 CO[C@]12CC[C@@]3(C[C@@H]1COc1ccc(-n4ccnc4)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL4110639 160420 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 539 7 1 7 4.9 CO[C@]12CC[C@@]3(C[C@@H]1COc1ccc(-n4ccnc4)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
162664997 182211 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 485 9 1 4 5.2 CCC(=O)N(c1ccccc1)C1(C(=O)Nc2ccc(OC)cc2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
CHEMBL4781906 182211 None 0 Human Functional pEC50 = 7.2 7.2 1 2
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 485 9 1 4 5.2 CCC(=O)N(c1ccccc1)C1(C(=O)Nc2ccc(OC)cc2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
168277847 190548 None 0 Rat Functional pEC50 = 7.2 7.2 -3 2
Agonist activity at recombinant rat DOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at recombinant rat DOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding
ChEMBL 434 5 2 7 2.6 CC[C@@H]1CN2CC[C@]3(O)c4c(ccc(F)c4OC)N[C@@H]3[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.0c01915
CHEMBL5178271 190548 None 0 Rat Functional pEC50 = 7.2 7.2 -3 2
Agonist activity at recombinant rat DOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS bindingAgonist activity at recombinant rat DOP stably expressed in CHO-K1 cell membrane assessed as [35S]GTPgammaS binding
ChEMBL 434 5 2 7 2.6 CC[C@@H]1CN2CC[C@]3(O)c4c(ccc(F)c4OC)N[C@@H]3[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.0c01915
44341722 9983 None 0 Human Functional pEC50 = 7.2 7.2 1 3
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 353 0 3 7 0.8 CN1CCC23c4c5ccc(O)c4OC2c2nc(O)ncc2CC3(O)C1C5 10.1016/s0960-894x(99)00608-3
CHEMBL114803 9983 None 0 Human Functional pEC50 = 7.2 7.2 1 3
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 353 0 3 7 0.8 CN1CCC23c4c5ccc(O)c4OC2c2nc(O)ncc2CC3(O)C1C5 10.1016/s0960-894x(99)00608-3
1607 1306 None 30 Human Functional pEC50 = 5.2 5.2 -22 6
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assay
ChEMBL None None None None 10.1016/j.ejmech.2022.114728
6917707 1306 None 30 Human Functional pEC50 = 5.2 5.2 -22 6
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assay
ChEMBL None None None None 10.1016/j.ejmech.2022.114728
CHEMBL340032 1306 None 30 Human Functional pEC50 = 5.2 5.2 -22 6
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assay
ChEMBL None None None None 10.1016/j.ejmech.2022.114728
DB08856 1306 None 30 Human Functional pEC50 = 5.2 5.2 -22 6
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as reduction in beta-arrestin 2 recruitment measured after 1.5 hrs by PathHunter assay
ChEMBL None None None None 10.1016/j.ejmech.2022.114728
172466389 196630 None 0 Human Functional pEC50 = 7.2 7.2 -21 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5428360 196630 None 0 Human Functional pEC50 = 7.2 7.2 -21 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
132079918 179967 None 0 Human Functional pEC50 = 6.2 6.2 -13 2
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)c2cccc(OC)c2)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
CHEMBL4745430 179967 None 0 Human Functional pEC50 = 6.2 6.2 -13 2
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)c2cccc(OC)c2)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
172464002 196592 None 0 Human Functional pEC50 = 6.2 6.2 -1 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)C/C=C/CCCC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5427400 196592 None 0 Human Functional pEC50 = 6.2 6.2 -1 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)C/C=C/CCCC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
10228465 205817 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 494 9 0 3 6.7 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCOc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL65151 205817 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 494 9 0 3 6.7 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCOc2ccccc2)c2ccccc2)cc1 10.1016/j.bmcl.2004.02.051
132961503 161132 None 0 Rat Functional pEC50 = 6.2 6.2 -851 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 382 5 2 5 3.4 O=[N+]([O-])c1ccc(CCN2CC[C@@]3(c4cccc(O)c4)CCC[C@@H]2[C@H]3O)cc1 10.1016/j.bmc.2017.02.064
CHEMBL4085431 161132 None 0 Rat Functional pEC50 = 6.2 6.2 -851 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 382 5 2 5 3.4 O=[N+]([O-])c1ccc(CCN2CC[C@@]3(c4cccc(O)c4)CCC[C@@H]2[C@H]3O)cc1 10.1016/j.bmc.2017.02.064
CHEMBL4116456 161132 None 0 Rat Functional pEC50 = 6.2 6.2 -851 2
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 382 5 2 5 3.4 O=[N+]([O-])c1ccc(CCN2CC[C@@]3(c4cccc(O)c4)CCC[C@@H]2[C@H]3O)cc1 10.1016/j.bmc.2017.02.064
2946860 23659 None 17 Human Functional pEC50 = 4.2 4.2 - 1
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 403 4 0 5 3.9 Cc1ccc2c(C)c(C(=O)N(Cc3cccs3)C3CCS(=O)(=O)C3)oc2c1 nan
CHEMBL1334918 23659 None 17 Human Functional pEC50 = 4.2 4.2 - 1
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 403 4 0 5 3.9 Cc1ccc2c(C)c(C(=O)N(Cc3cccs3)C3CCS(=O)(=O)C3)oc2c1 nan
122181051 121864 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assayAgonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
ChEMBL 430 6 2 5 3.8 CC(C)C[C@H]1CN2C(=CC3=NC[C@H](Cc4ccccc4)N3C[C@@H]2Cc2ccc(O)cc2)N1 10.1021/jm501637c
CHEMBL3589704 121864 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assayAgonist activity at delta opioid receptor (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay
ChEMBL 430 6 2 5 3.8 CC(C)C[C@H]1CN2C(=CC3=NC[C@H](Cc4ccccc4)N3C[C@@H]2Cc2ccc(O)cc2)N1 10.1021/jm501637c
CHEMBL3759167 214688 None 0 Human Functional pEC50 = 7.2 7.2 -11 3
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysisAgonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2015.12.012
89978655 160513 None 0 Human Functional pEC50 = 6.2 6.2 1 2
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 525 7 0 8 4.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CSc1nc(C)ns1)C2 nan
CHEMBL4111378 160513 None 0 Human Functional pEC50 = 6.2 6.2 1 2
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 525 7 0 8 4.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](CSc1nc(C)ns1)C2 nan
1795 1591 None 47 Human Functional pEC50 = 4.2 4.2 -8 4
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 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
4186 1591 None 47 Human Functional pEC50 = 4.2 4.2 -8 4
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 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
CHEMBL517986 1591 None 47 Human Functional pEC50 = 4.2 4.2 -8 4
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 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
44235488 198255 None 0 Human Functional pEC50 = 7.2 7.2 -1 3
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 358 0 1 3 3.8 CN1CC[C@]23Cc4c(c5ccccc5n4C)C[C@]2(Cc2ccc(O)cc23)C1 10.1016/j.bmcl.2009.06.093
CHEMBL557937 198255 None 0 Human Functional pEC50 = 7.2 7.2 -1 3
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 358 0 1 3 3.8 CN1CC[C@]23Cc4c(c5ccccc5n4C)C[C@]2(Cc2ccc(O)cc23)C1 10.1016/j.bmcl.2009.06.093
44306987 103120 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 418 6 0 3 5.2 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL307327 103120 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 418 6 0 3 5.2 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.02.051
5573 67602 None 59 Human Functional pEC50 = 4.2 4.2 -85 6
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 387 9 0 6 3.7 CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C nan
5573.0 67602 None 59 Human Functional pEC50 = 4.2 4.2 -85 6
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 387 9 0 6 3.7 CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C nan
CHEMBL1325297 67602 None 59 Human Functional pEC50 = 4.2 4.2 -85 6
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 387 9 0 6 3.7 CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C nan
CHEMBL190044 67602 None 59 Human Functional pEC50 = 4.2 4.2 -85 6
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 387 9 0 6 3.7 CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C nan
DB09089 67602 None 59 Human Functional pEC50 = 4.2 4.2 -85 6
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 387 9 0 6 3.7 CCC(COC(=O)c1cc(OC)c(OC)c(OC)c1)(c1ccccc1)N(C)C nan
CHEMBL5094675 217999 None 0 Human Functional pEC50 = 6.2 6.2 -5 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
162651945 180466 None 0 Human Functional pEC50 = 6.2 6.2 6 2
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 505 10 1 5 5.2 CCC(=O)N(Cc1cccs1)C1(C(=O)Nc2ccc(OC)cc2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
CHEMBL4751491 180466 None 0 Human Functional pEC50 = 6.2 6.2 6 2
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 505 10 1 5 5.2 CCC(=O)N(Cc1cccs1)C1(C(=O)Nc2ccc(OC)cc2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
44255044 198870 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 394 4 1 3 4.3 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1F 10.1021/jm900773n
CHEMBL562873 198870 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 394 4 1 3 4.3 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1F 10.1021/jm900773n
44596170 14182 None 0 Human Functional pEC50 = 7.2 7.2 -36 4
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 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 14182 None 0 Human Functional pEC50 = 7.2 7.2 -36 4
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 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 14182 None 0 Human Functional pEC50 = 7.2 7.2 -36 4
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 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
44341920 114250 None 0 Human Functional pEC50 = 7.2 7.2 1 3
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 352 0 3 7 0.7 CN1CCC23c4c5ccc(O)c4OC2c2nc(N)ncc2CC3(O)C1C5 10.1016/s0960-894x(99)00608-3
CHEMBL332947 114250 None 0 Human Functional pEC50 = 7.2 7.2 1 3
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 352 0 3 7 0.7 CN1CCC23c4c5ccc(O)c4OC2c2nc(N)ncc2CC3(O)C1C5 10.1016/s0960-894x(99)00608-3
89978762 160238 None 0 Human Functional pEC50 = 7.2 7.2 -26 3
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 10 1 6 4.0 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OCC(N)=O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL4109061 160238 None 0 Human Functional pEC50 = 7.2 7.2 -26 3
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 10 1 6 4.0 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(OCC(N)=O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
86711652 160116 None 0 Human Functional pEC50 = 7.2 7.2 -43 3
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 489 7 0 4 5.3 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(F)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL4108017 160116 None 0 Human Functional pEC50 = 7.2 7.2 -43 3
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 489 7 0 4 5.3 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(F)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL5094675 217999 None 0 Human Functional pEC50 = 6.2 6.2 -5 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
168274425 190242 None 0 Human Functional pEC50 = 6.2 6.2 -15 4
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 569 15 6 6 1.6 CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1 10.1039/D1MD00025J
CHEMBL5173456 190242 None 0 Human Functional pEC50 = 6.2 6.2 -15 4
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 569 15 6 6 1.6 CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1 10.1039/D1MD00025J
127034976 136555 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 476 11 2 4 8.0 COc1cc(/C=C/c2ccc(O)c(O)c2CC=C(C)C)c(C/C=C(\C)CCC=C(C)C)c(OC)c1 10.1016/j.bmcl.2015.10.059
CHEMBL3735897 136555 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor over-expressed in CHO cell membrane after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 476 11 2 4 8.0 COc1cc(/C=C/c2ccc(O)c(O)c2CC=C(C)C)c(C/C=C(\C)CCC=C(C)C)c(OC)c1 10.1016/j.bmcl.2015.10.059
168274425 190242 None 0 Human Functional pEC50 = 6.2 6.2 -15 4
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 569 15 6 6 1.6 CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1 10.1039/D1MD00025J
CHEMBL5173456 190242 None 0 Human Functional pEC50 = 6.2 6.2 -15 4
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 569 15 6 6 1.6 CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1 10.1039/D1MD00025J
127049275 141037 None 0 Rat Functional pEC50 = 7.2 7.2 -22 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 501 8 3 5 3.7 COCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
CHEMBL3822963 141037 None 0 Rat Functional pEC50 = 7.2 7.2 -22 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 501 8 3 5 3.7 COCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
89981528 160103 None 0 Human Functional pEC50 = 7.2 7.2 -8 3
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 449 5 0 4 4.5 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(F)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
CHEMBL4107906 160103 None 0 Human Functional pEC50 = 7.2 7.2 -8 3
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 449 5 0 4 4.5 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(F)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
16187807 20399 None 1 Human Functional pEC50 = 4.2 4.2 1 2
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 393 7 1 4 4.2 COc1ccc2c(c1)C=C(CN1CCC(CO)(CCc3ccccc3)CC1)CO2 nan
CHEMBL1306479 20399 None 1 Human Functional pEC50 = 4.2 4.2 1 2
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 393 7 1 4 4.2 COc1ccc2c(c1)C=C(CN1CCC(CO)(CCc3ccccc3)CC1)CO2 nan
145984332 165968 None 0 Rat Functional pEC50 = 6.2 6.2 -676 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 483 6 0 5 4.6 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42C=C[C@@]1(OC)[C@@H](C(=O)c1ccccc1)C2 10.1016/j.bmc.2018.07.020
CHEMBL4249256 165968 None 0 Rat Functional pEC50 = 6.2 6.2 -676 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 483 6 0 5 4.6 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42C=C[C@@]1(OC)[C@@H](C(=O)c1ccccc1)C2 10.1016/j.bmc.2018.07.020
122195953 124274 None 0 Rat Functional pEC50 = 7.2 7.2 -11 2
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 471 6 3 4 4.1 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.5b01270
CHEMBL3634247 124274 None 0 Rat Functional pEC50 = 7.2 7.2 -11 2
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 471 6 3 4 4.1 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.5b01270
44421403 141727 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
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 514 4 2 5 5.4 Oc1ccc2c3c1O[C@H]1c4c(c5c(n4CC4CCCCC4)CCCC5)C[C@@]4(O)C(C2)N(CC2CC2)CC[C@]314 10.1021/jm040817t
CHEMBL385316 141727 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
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 514 4 2 5 5.4 Oc1ccc2c3c1O[C@H]1c4c(c5c(n4CC4CCCCC4)CCCC5)C[C@@]4(O)C(C2)N(CC2CC2)CC[C@]314 10.1021/jm040817t
44254058 197635 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 382 4 1 4 4.2 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)s1 10.1021/jm900773n
CHEMBL550472 197635 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 382 4 1 4 4.2 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)s1 10.1021/jm900773n
71720457 86878 None 0 Rat Functional pEC50 = 7.2 7.2 -83 2
Agonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21 10.1021/jm400050y
CHEMBL2322561 86878 None 0 Rat Functional pEC50 = 7.2 7.2 -83 2
Agonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat DOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21 10.1021/jm400050y
71720457 86878 None 0 Rat Functional pEC50 = 7.2 7.2 -83 2
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21 10.1021/acs.jmedchem.5b01270
CHEMBL2322561 86878 None 0 Rat Functional pEC50 = 7.2 7.2 -83 2
Agonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat delta-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21 10.1021/acs.jmedchem.5b01270
162666316 182362 None 0 Human Functional pEC50 = 6.2 6.2 -16 2
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 493 4 1 7 4.0 CC(=O)O[C@@H]1C[C@H](NC(=O)c2ccccc2)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
CHEMBL4783674 182362 None 0 Human Functional pEC50 = 6.2 6.2 -16 2
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 493 4 1 7 4.0 CC(=O)O[C@@H]1C[C@H](NC(=O)c2ccccc2)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
172463159 196666 None 0 Human Functional pEC50 = 6.2 6.2 -10 2
Inverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assayInverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
ChEMBL 642 11 1 7 8.5 COc1cccc(Cn2nc(CNCCc3ccc4ccccc4c3)c3c4cc(OC)c(OC)cc4c(-c4ccccc4Cl)nc32)c1 10.1021/acs.jmedchem.3c00064
CHEMBL5429274 196666 None 0 Human Functional pEC50 = 6.2 6.2 -10 2
Inverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assayInverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
ChEMBL 642 11 1 7 8.5 COc1cccc(Cn2nc(CNCCc3ccc4ccccc4c3)c3c4cc(OC)c(OC)cc4c(-c4ccccc4Cl)nc32)c1 10.1021/acs.jmedchem.3c00064
168269903 190187 None 0 Human Functional pEC50 = 6.2 6.2 -5 4
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 595 16 6 6 2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)NC1CC1 10.1039/D1MD00025J
CHEMBL5172639 190187 None 0 Human Functional pEC50 = 6.2 6.2 -5 4
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 595 16 6 6 2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)NC1CC1 10.1039/D1MD00025J
168287282 191896 None 0 Human Functional pEC50 = 6.2 6.2 -10 4
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 583 16 6 6 2.0 CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1 10.1039/D1MD00025J
CHEMBL5198168 191896 None 0 Human Functional pEC50 = 6.2 6.2 -10 4
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 583 16 6 6 2.0 CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1 10.1039/D1MD00025J
24891946 55859 None 1 Human Functional pEC50 = 4.2 4.2 -14 2
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 532 9 0 6 5.0 CN(C)CCCN(C(=O)c1ccc(S(=O)(=O)N(C)C2CCCCC2)cc1)c1nc2ccc(F)cc2s1 nan
CHEMBL1522542 55859 None 1 Human Functional pEC50 = 4.2 4.2 -14 2
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 532 9 0 6 5.0 CN(C)CCCN(C(=O)c1ccc(S(=O)(=O)N(C)C2CCCCC2)cc1)c1nc2ccc(F)cc2s1 nan
CHEMBL1623168 55859 None 1 Human Functional pEC50 = 4.2 4.2 -14 2
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 532 9 0 6 5.0 CN(C)CCCN(C(=O)c1ccc(S(=O)(=O)N(C)C2CCCCC2)cc1)c1nc2ccc(F)cc2s1 nan
168269903 190187 None 0 Human Functional pEC50 = 6.2 6.2 -5 4
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 595 16 6 6 2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)NC1CC1 10.1039/D1MD00025J
CHEMBL5172639 190187 None 0 Human Functional pEC50 = 6.2 6.2 -5 4
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 595 16 6 6 2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)NC1CC1 10.1039/D1MD00025J
168287282 191896 None 0 Human Functional pEC50 = 6.2 6.2 -10 4
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 583 16 6 6 2.0 CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1 10.1039/D1MD00025J
CHEMBL5198168 191896 None 0 Human Functional pEC50 = 6.2 6.2 -10 4
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 583 16 6 6 2.0 CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1 10.1039/D1MD00025J
145961883 161459 None 0 Rat Functional pEC50 = 8.2 8.2 -588 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 594 16 9 7 -0.4 C=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4126102 161459 None 0 Rat Functional pEC50 = 8.2 8.2 -588 4
Agonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assayAgonist activity at rat delta-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 594 16 9 7 -0.4 C=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
44177669 61281 None 0 Human Functional pEC50 = 8.2 8.2 -5 5
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 1233 27 9 10 6.3 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)N(C)Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766205 61281 None 0 Human Functional pEC50 = 8.2 8.2 -5 5
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 1233 27 9 10 6.3 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)N(C)Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
118713810 114480 None 0 Mouse Functional pEC50 = 8.2 8.2 10 3
Agonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 1026 12 12 14 0.3 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)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/ml500241n
CHEMBL3331510 114480 None 0 Mouse Functional pEC50 = 8.2 8.2 10 3
Agonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 1026 12 12 14 0.3 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)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/ml500241n
9005 474 None 17 Human Functional pEC50 = 8.1 8.1 2137 3
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 348 5 1 2 4.4 CCN(C(=O)c1ccc(cc1)C(=C1CCNCC1)c1ccccc1)CC 10.1021/jm000229p
9841259 474 None 17 Human Functional pEC50 = 8.1 8.1 2137 3
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 348 5 1 2 4.4 CCN(C(=O)c1ccc(cc1)C(=C1CCNCC1)c1ccccc1)CC 10.1021/jm000229p
CHEMBL415521 474 None 17 Human Functional pEC50 = 8.1 8.1 2137 3
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 348 5 1 2 4.4 CCN(C(=O)c1ccc(cc1)C(=C1CCNCC1)c1ccccc1)CC 10.1021/jm000229p
127032210 139280 None 0 Human Functional pEC50 = 8.1 8.1 1 3
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 426 2 2 4 4.1 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)CCc1cc2ccccc2nc1C3 10.1016/j.bmc.2016.03.040
CHEMBL3787663 139280 None 0 Human Functional pEC50 = 8.1 8.1 1 3
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 426 2 2 4 4.1 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)CCc1cc2ccccc2nc1C3 10.1016/j.bmc.2016.03.040
71450766 84211 None 0 Human Functional pEC50 = 8.1 8.1 -5 3
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 482 7 1 3 5.8 COc1ccc2cc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)ccc2c1 10.1016/j.bmcl.2012.10.081
CHEMBL2208354 84211 None 0 Human Functional pEC50 = 8.1 8.1 -5 3
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 482 7 1 3 5.8 COc1ccc2cc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)ccc2c1 10.1016/j.bmcl.2012.10.081
11566769 112725 None 0 Human Functional pEC50 = 8.1 8.1 2 2
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 364 5 2 3 4.1 C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N)C[C@]1(c1cccc(O)c1)C2 10.1021/jm401250s
CHEMBL3216611 112725 None 0 Human Functional pEC50 = 8.1 8.1 2 2
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 364 5 2 3 4.1 C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N)C[C@]1(c1cccc(O)c1)C2 10.1021/jm401250s
CHEMBL3303515 112725 None 0 Human Functional pEC50 = 8.1 8.1 2 2
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 364 5 2 3 4.1 C[C@@H]1CN(CCCc2ccccc2)[C@H]2C[C@H](N)C[C@]1(c1cccc(O)c1)C2 10.1021/jm401250s
71461668 79209 None 0 Human Functional pEC50 = 8.1 8.1 2 3
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 476 4 2 3 6.1 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(CCCc2ccccc2)C1C5 10.1021/jm021073r
CHEMBL2113380 79209 None 0 Human Functional pEC50 = 8.1 8.1 2 3
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 476 4 2 3 6.1 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(CCCc2ccccc2)C1C5 10.1021/jm021073r
123924 3633 None 34 Human Functional pEC50 = 8.1 8.1 1 9
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
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/acsmedchemlett.9b00569
1611 3633 None 34 Human Functional pEC50 = 8.1 8.1 1 9
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
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/acsmedchemlett.9b00569
CHEMBL13470 3633 None 34 Human Functional pEC50 = 8.1 8.1 1 9
Agonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
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/acsmedchemlett.9b00569
CHEMBL3331509 213849 None 0 Mouse Functional pEC50 = 8.1 8.1 - 1
Agonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/ml500241n
172465082 196717 None 0 Human Functional pEC50 = 8.1 8.1 -1 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5430632 196717 None 0 Human Functional pEC50 = 8.1 8.1 -1 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCC/C=C/CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
44233185 194934 None 0 Human Functional pEC50 = 8.1 8.1 -44 5
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 1327 29 14 16 1.1 CCCC[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](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
CHEMBL539193 194934 None 0 Human Functional pEC50 = 8.1 8.1 -44 5
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 1327 29 14 16 1.1 CCCC[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](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
44339475 110634 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
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 445 7 1 4 4.8 O=C1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4cccc(O)c4C2(CCN3CC2CC2)C1 10.1021/jm031126k
CHEMBL325347 110634 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
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 445 7 1 4 4.8 O=C1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4cccc(O)c4C2(CCN3CC2CC2)C1 10.1021/jm031126k
44233185 194934 None 0 Human Functional pEC50 = 8.1 8.1 -44 5
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 1327 29 14 16 1.1 CCCC[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](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
CHEMBL539193 194934 None 0 Human Functional pEC50 = 8.1 8.1 -44 5
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 1327 29 14 16 1.1 CCCC[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](CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm900473p
25129133 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](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/jm800389v
CHEMBL507340 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](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/jm800389v
CHEMBL5075108 218018 None 2 Human Functional pEC50 = 7.2 7.2 -131 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccs1 10.1021/acs.jmedchem.2c00087
CHEMBL5095555 218018 None 2 Human Functional pEC50 = 7.2 7.2 -131 3
Antagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting methodAntagonist activity against human delta opioid receptor expressed in CHO cell membrane assessed as reduction in SNC80 induced [35S]GTPgammaS binding incubated for 1.5 hrs by liquid scintillation counting method
ChEMBL None None None O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccs1 10.1021/acs.jmedchem.2c00087
1422958 35633 None 7 Human Functional pEC50 = 4.2 4.2 - 1
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 406 5 1 6 3.9 CN1CCN(c2ccc(NC(=O)c3ccc(-c4cccc([N+](=O)[O-])c4)o3)cc2)CC1 nan
CHEMBL1439686 35633 None 7 Human Functional pEC50 = 4.2 4.2 - 1
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 406 5 1 6 3.9 CN1CCN(c2ccc(NC(=O)c3ccc(-c4cccc([N+](=O)[O-])c4)o3)cc2)CC1 nan
4796915 49777 None 2 Human Functional pEC50 = 4.2 4.2 - 1
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 356 6 1 6 4.0 COc1ccc(C(CNc2ncnc3sc(C)c(C)c23)N(C)C)cc1 nan
CHEMBL1567143 49777 None 2 Human Functional pEC50 = 4.2 4.2 - 1
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 356 6 1 6 4.0 COc1ccc(C(CNc2ncnc3sc(C)c(C)c23)N(C)C)cc1 nan
118725854 117243 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 401 6 2 6 2.1 CS(=O)(=O)c1c[nH]c(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)c1 10.1016/j.bmcl.2014.12.064
CHEMBL3394004 117243 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 401 6 2 6 2.1 CS(=O)(=O)c1c[nH]c(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)c1 10.1016/j.bmcl.2014.12.064
44337683 9163 None 0 Human Functional pEC50 = 7.1 7.1 -21 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 429 2 1 4 4.7 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@]12CCC(=O)[C@H]3/C(=C(\C)c1ccccc1)C2 10.1021/jm030801n
CHEMBL110124 9163 None 0 Human Functional pEC50 = 7.1 7.1 -21 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 429 2 1 4 4.7 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@]12CCC(=O)[C@H]3/C(=C(\C)c1ccccc1)C2 10.1021/jm030801n
11742693 75944 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
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 417 6 3 4 2.8 NC(=O)c1ccc(C[C@H](N)C(=O)N2CCCC[C@H]2c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/j.bmcl.2006.01.082
CHEMBL204996 75944 None 0 Mouse Functional pEC50 = 6.1 6.1 - 1
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 417 6 3 4 2.8 NC(=O)c1ccc(C[C@H](N)C(=O)N2CCCC[C@H]2c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/j.bmcl.2006.01.082
44439901 148629 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 713 20 10 10 -2.5 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cccc(C(N)=O)c1)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1016/j.bmcl.2007.01.092
CHEMBL393867 148629 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 713 20 10 10 -2.5 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cccc(C(N)=O)c1)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1016/j.bmcl.2007.01.092
16288533 59968 None 3 Human Functional pEC50 = 5.1 5.1 -14 2
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 338 6 1 3 3.2 COc1ccc(C(CNC(=O)c2ccc3c(c2)CCC3)N(C)C)cc1 nan
CHEMBL1732484 59968 None 3 Human Functional pEC50 = 5.1 5.1 -14 2
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 338 6 1 3 3.2 COc1ccc(C(CNC(=O)c2ccc3c(c2)CCC3)N(C)C)cc1 nan
44418923 161879 None 0 Human Functional pEC50 = 7.1 7.1 -3 5
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=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
CHEMBL414087 161879 None 0 Human Functional pEC50 = 7.1 7.1 -3 5
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=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
CHEMBL247363 212964 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 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(N)cc1)C(=O)O 10.1016/j.bmcl.2007.01.092
132079904 182575 None 0 Human Functional pEC50 = 7.1 7.1 -5 2
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 492 4 0 8 4.4 COC(=O)[C@@H]1C=C(OC(=O)c2ccccc2)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
CHEMBL4786506 182575 None 0 Human Functional pEC50 = 7.1 7.1 -5 2
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 492 4 0 8 4.4 COC(=O)[C@@H]1C=C(OC(=O)c2ccccc2)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
44408590 161820 None 0 Human Functional pEC50 = 7.1 7.1 -3 5
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 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL413644 161820 None 0 Human Functional pEC50 = 7.1 7.1 -3 5
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 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
1651 2719 None 23 Human Functional pEC50 = 7.1 7.1 -186 5
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 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
4673 2719 None 23 Human Functional pEC50 = 7.1 7.1 -186 5
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 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
6445230 2719 None 23 Human Functional pEC50 = 7.1 7.1 -186 5
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 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
CHEMBL267495 2719 None 23 Human Functional pEC50 = 7.1 7.1 -186 5
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 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
DB13471 2719 None 23 Human Functional pEC50 = 7.1 7.1 -186 5
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 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
CHEMBL5090298 217746 None 0 Human Functional pEC50 = 7.1 7.1 -1 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
44408590 161820 None 0 Human Functional pEC50 = 7.1 7.1 -3 5
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 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL413644 161820 None 0 Human Functional pEC50 = 7.1 7.1 -3 5
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 1134 30 12 15 2.6 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL5090298 217746 None 0 Human Functional pEC50 = 7.1 7.1 -1 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
785909 41061 None 4 Human Functional pEC50 = 4.1 4.1 -1 2
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 336 4 1 3 4.1 COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C nan
CHEMBL1487650 41061 None 4 Human Functional pEC50 = 4.1 4.1 -1 2
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 336 4 1 3 4.1 COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C nan
5113115 20637 None 4 Human Functional pEC50 = 4.1 4.1 -5 2
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 314 5 2 3 3.4 Cc1ccccc1NC(S)=NCC(c1cccnc1)N(C)C nan
CHEMBL1308389 20637 None 4 Human Functional pEC50 = 4.1 4.1 -5 2
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 314 5 2 3 3.4 Cc1ccccc1NC(S)=NCC(c1cccnc1)N(C)C nan
1859830 55693 None 10 Human Functional pEC50 = 4.1 4.1 - 1
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 435 9 3 7 3.0 Nc1nonc1C(=O)NCCNCc1c(OCc2ccccc2F)ccc2ccccc12 nan
CHEMBL1445858 55693 None 10 Human Functional pEC50 = 4.1 4.1 - 1
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 435 9 3 7 3.0 Nc1nonc1C(=O)NCCNCc1c(OCc2ccccc2F)ccc2ccccc12 nan
CHEMBL1621801 55693 None 10 Human Functional pEC50 = 4.1 4.1 - 1
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 435 9 3 7 3.0 Nc1nonc1C(=O)NCCNCc1c(OCc2ccccc2F)ccc2ccccc12 nan
44541250 200688 None 0 Human Functional pEC50 = 7.1 7.1 -23 2
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 482 4 1 5 3.0 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)C#Cc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm901074a
CHEMBL575451 200688 None 0 Human Functional pEC50 = 7.1 7.1 -23 2
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human delta opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 482 4 1 5 3.0 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)C#Cc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm901074a
66827012 160975 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 499 5 1 7 4.1 CO[C@]12CC[C@@]3(C[C@@H]1COc1ccc(-n4ccnc4)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
CHEMBL4115091 160975 None 0 Human Functional pEC50 = 7.1 7.1 -8 3
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 499 5 1 7 4.1 CO[C@]12CC[C@@]3(C[C@@H]1COc1ccc(-n4ccnc4)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
CHEMBL336381 214042 None 0 Human Functional pEC50 = 7.1 7.1 -10 4
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)CNC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
72712370 93214 None 2 Human Functional pEC50 = 6.1 6.1 -12 3
Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay
ChEMBL 356 6 1 4 4.7 c1ccc([C@]2(CCNCc3cccs3)CCOC3(CCCC3)C2)nc1 10.1021/jm4010829
CHEMBL2443278 93214 None 2 Human Functional pEC50 = 6.1 6.1 -12 3
Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assayAgonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay
ChEMBL 356 6 1 4 4.7 c1ccc([C@]2(CCNCc3cccs3)CCOC3(CCCC3)C2)nc1 10.1021/jm4010829
11950654 114511 None 0 Human Functional pEC50 = 5.1 5.1 2 2
Agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP[gammaS] bindingAgonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding
ChEMBL 364 5 2 3 4.1 CC1CN(CCCc2ccccc2)C2C[C@H](N)CC1(c1cccc(O)c1)C2 10.1016/j.bmcl.2014.03.040
CHEMBL333342 114511 None 0 Human Functional pEC50 = 5.1 5.1 2 2
Agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP[gammaS] bindingAgonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding
ChEMBL 364 5 2 3 4.1 CC1CN(CCCc2ccccc2)C2C[C@H](N)CC1(c1cccc(O)c1)C2 10.1016/j.bmcl.2014.03.040
155546429 173640 None 0 Human Functional pEC50 = 6.1 6.1 -1 4
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 556 15 6 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)O 10.1039/D1MD00025J
CHEMBL4531563 173640 None 0 Human Functional pEC50 = 6.1 6.1 -1 4
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 556 15 6 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)O 10.1039/D1MD00025J
CHEMBL336381 214042 None 0 Human Functional pEC50 = 7.1 7.1 -10 4
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)CNC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
CHEMBL2419543 212903 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=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
11849283 204309 None 0 Human Functional pEC50 = 7.1 7.1 -30 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 458 4 1 5 3.2 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(C)cc5)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
CHEMBL607127 204309 None 0 Human Functional pEC50 = 7.1 7.1 -30 3
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
ChEMBL 458 4 1 5 3.2 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(C)cc5)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
123924 3633 None 34 Human Functional pEC50 = 6.1 6.1 1 9
Agonistic activity towards opioid receptor delta 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudateAgonistic activity towards opioid receptor delta 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate
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/jm030311v
1611 3633 None 34 Human Functional pEC50 = 6.1 6.1 1 9
Agonistic activity towards opioid receptor delta 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudateAgonistic activity towards opioid receptor delta 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate
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/jm030311v
CHEMBL13470 3633 None 34 Human Functional pEC50 = 6.1 6.1 1 9
Agonistic activity towards opioid receptor delta 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudateAgonistic activity towards opioid receptor delta 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate
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/jm030311v
155546429 173640 None 0 Human Functional pEC50 = 6.1 6.1 -1 4
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 556 15 6 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)O 10.1039/D1MD00025J
CHEMBL4531563 173640 None 0 Human Functional pEC50 = 6.1 6.1 -1 4
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 556 15 6 6 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(=O)O 10.1039/D1MD00025J
132079916 181275 None 0 Human Functional pEC50 = 6.1 6.1 -7 2
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 537 5 0 10 4.3 COC(=O)[C@@H]1C=C(OC(=O)c2ccc([N+](=O)[O-])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
CHEMBL4760942 181275 None 0 Human Functional pEC50 = 6.1 6.1 -7 2
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 537 5 0 10 4.3 COC(=O)[C@@H]1C=C(OC(=O)c2ccc([N+](=O)[O-])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
44406285 72650 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 450 5 0 3 5.6 CN(C(=O)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2005.09.025
CHEMBL199433 72650 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 450 5 0 3 5.6 CN(C(=O)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2005.09.025
89978607 160564 None 0 Human Functional pEC50 = 6.1 6.1 -8 2
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 589 11 0 8 4.7 COC(=O)COc1ccc(COC[C@H]2C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1 nan
CHEMBL4111803 160564 None 0 Human Functional pEC50 = 6.1 6.1 -8 2
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 589 11 0 8 4.7 COC(=O)COc1ccc(COC[C@H]2C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1 nan
155519089 170446 None 0 Rat Functional pEC50 = 7.1 7.1 17 2
Agonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting
ChEMBL 562 8 1 5 6.7 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NCc3ccccc3)cc1)C2 10.1021/acs.jmedchem.9b00857
CHEMBL4447249 170446 None 0 Rat Functional pEC50 = 7.1 7.1 17 2
Agonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting
ChEMBL 562 8 1 5 6.7 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NCc3ccccc3)cc1)C2 10.1021/acs.jmedchem.9b00857
1627 2594 None 9 Human Functional pEC50 = 6.1 6.1 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/acs.jmedchem.6b01235
1845 2594 None 9 Human Functional pEC50 = 6.1 6.1 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/acs.jmedchem.6b01235
5288826 2594 None 9 Human Functional pEC50 = 6.1 6.1 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/acs.jmedchem.6b01235
5288826.0 2594 None 9 Human Functional pEC50 = 6.1 6.1 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/acs.jmedchem.6b01235
CHEMBL70 2594 None 9 Human Functional pEC50 = 6.1 6.1 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/acs.jmedchem.6b01235
DB00295 2594 None 9 Human Functional pEC50 = 6.1 6.1 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/acs.jmedchem.6b01235
780684 41241 None 8 Human Functional pEC50 = 5.1 5.1 -199 4
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 348 5 1 4 3.7 Cc1ccc(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)cc1 10.1016/j.bmcl.2014.12.064
CHEMBL1488893 41241 None 8 Human Functional pEC50 = 5.1 5.1 -199 4
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 348 5 1 4 3.7 Cc1ccc(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)cc1 10.1016/j.bmcl.2014.12.064
24892091 55566 None 2 Human Functional pEC50 = 4.1 4.1 -1 2
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 564 11 0 6 5.7 CCN(Cc1ccccc1)S(=O)(=O)c1ccc(C(=O)N(CCCN(C)C)c2nc3c(C)c(C)ccc3s2)cc1 nan
CHEMBL1437660 55566 None 2 Human Functional pEC50 = 4.1 4.1 -1 2
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 564 11 0 6 5.7 CCN(Cc1ccccc1)S(=O)(=O)c1ccc(C(=O)N(CCCN(C)C)c2nc3c(C)c(C)ccc3s2)cc1 nan
CHEMBL1620637 55566 None 2 Human Functional pEC50 = 4.1 4.1 -1 2
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 564 11 0 6 5.7 CCN(Cc1ccccc1)S(=O)(=O)c1ccc(C(=O)N(CCCN(C)C)c2nc3c(C)c(C)ccc3s2)cc1 nan
71819404 92087 None 0 Human Functional pEC50 = 4.1 4.1 -10 3
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 319 1 1 4 1.7 COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](F)C[C@H]4[C@@H](C2)N(C)CC[C@@]341 10.1016/j.bmcl.2013.06.084
CHEMBL2418742 92087 None 0 Human Functional pEC50 = 4.1 4.1 -10 3
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 319 1 1 4 1.7 COc1ccc2c3c1O[C@H]1[C@@H](O)[C@H](F)C[C@H]4[C@@H](C2)N(C)CC[C@@]341 10.1016/j.bmcl.2013.06.084
155520586 170595 None 0 Rat Functional pEC50 = 6.1 6.1 -398 2
Agonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting
ChEMBL 576 7 1 5 6.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NC(=O)c3ccccc3)cc1)C2 10.1021/acs.jmedchem.9b00857
CHEMBL4449252 170595 None 0 Rat Functional pEC50 = 6.1 6.1 -398 2
Agonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation countingAgonist activity at rat DOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting
ChEMBL 576 7 1 5 6.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NC(=O)c3ccccc3)cc1)C2 10.1021/acs.jmedchem.9b00857
155520586 170595 None 0 Rat Functional pEC50 = 6.1 6.1 -398 2
Agonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 576 7 1 5 6.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NC(=O)c3ccccc3)cc1)C2 10.1021/acs.jmedchem.1c01082
CHEMBL4449252 170595 None 0 Rat Functional pEC50 = 6.1 6.1 -398 2
Agonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 576 7 1 5 6.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1ccc(NC(=O)c3ccccc3)cc1)C2 10.1021/acs.jmedchem.1c01082
16193682 59749 None 4 Human Functional pEC50 = 4.1 4.1 - 1
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 342 6 2 3 3.8 CCc1cccc(C)c1N=C(S)NCC(c1cccnc1)N(C)C nan
CHEMBL1724267 59749 None 4 Human Functional pEC50 = 4.1 4.1 - 1
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 342 6 2 3 3.8 CCc1cccc(C)c1N=C(S)NCC(c1cccnc1)N(C)C nan
104787 1473 None 17 Human Functional pEC50 = 8.1 8.1 -2 4
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 None 10.1016/j.bmcl.2015.05.038
1608 1473 None 17 Human Functional pEC50 = 8.1 8.1 -2 4
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 None 10.1016/j.bmcl.2015.05.038
CHEMBL31421 1473 None 17 Human Functional pEC50 = 8.1 8.1 -2 4
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 None 10.1016/j.bmcl.2015.05.038
DB08861 1473 None 17 Human Functional pEC50 = 8.1 8.1 -2 4
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 None 10.1016/j.bmcl.2015.05.038
155549998 176565 None 0 Human Functional pEC50 = 8.1 8.1 5 2
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1166 12 12 14 2.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSCc2ccccc2CSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
CHEMBL4539430 176565 None 0 Human Functional pEC50 = 8.1 8.1 5 2
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1166 12 12 14 2.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSCc2ccccc2CSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
CHEMBL4596465 176565 None 0 Human Functional pEC50 = 8.1 8.1 5 2
Agonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay
ChEMBL 1166 12 12 14 2.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CSCc2ccccc2CSC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C(=O)NCC(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC1=O 10.1021/acs.jmedchem.9b01963
73355099 91662 None 0 Human Functional pEC50 = 8.1 8.1 -3 3
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 729 11 3 6 5.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
CHEMBL2408014 91662 None 0 Human Functional pEC50 = 8.1 8.1 -3 3
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 729 11 3 6 5.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
127051732 141126 None 0 Rat Functional pEC50 = 8.1 8.1 -2 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 499 8 3 4 4.9 CCCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
CHEMBL3824052 141126 None 0 Rat Functional pEC50 = 8.1 8.1 -2 2
Agonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat DOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 499 8 3 4 4.9 CCCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
73355099 91662 None 0 Human Functional pEC50 = 8.1 8.1 -3 3
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 729 11 3 6 5.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
CHEMBL2408014 91662 None 0 Human Functional pEC50 = 8.1 8.1 -3 3
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 729 11 3 6 5.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
CHEMBL389651 214889 None 0 Human Functional pEC50 = 8.1 8.1 -3 4
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(C)C)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
CHEMBL2387216 212864 None 0 Human Functional pEC50 = 8.1 8.1 -5 3
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](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)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)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2013.03.065
16100408 141878 None 0 Human Functional pEC50 = 8.1 8.1 -2 4
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=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
CHEMBL386186 141878 None 0 Human Functional pEC50 = 8.1 8.1 -2 4
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=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
16720649 85395 None 0 Human Functional pEC50 = 8.1 8.1 2 3
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 327 0 2 5 2.3 CN1CC[C@]23Cc4nc(N)sc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1021/jm0701674
CHEMBL226167 85395 None 0 Human Functional pEC50 = 8.1 8.1 2 3
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 327 0 2 5 2.3 CN1CC[C@]23Cc4nc(N)sc4C[C@H]2[C@H]1Cc1ccc(O)cc13 10.1021/jm0701674
25129133 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
CHEMBL507340 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
25129133 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](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/jm100157m
CHEMBL507340 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](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/jm100157m
44421407 136983 None 0 Human Functional pEC50 = 8.1 8.1 11 3
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 392 0 2 5 2.5 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2C)CCCC4)C[C@@]3(O)C1C5 10.1021/jm040817t
CHEMBL374228 136983 None 0 Human Functional pEC50 = 8.1 8.1 11 3
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 392 0 2 5 2.5 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2C)CCCC4)C[C@@]3(O)C1C5 10.1021/jm040817t
25129133 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
CHEMBL507340 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
25129133 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](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/jm800389v
CHEMBL507340 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](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/jm800389v
25129133 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](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/jm100157m
CHEMBL507340 188995 None 0 Human Functional pEC50 = 8.1 8.1 -281 6
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 1208 27 10 11 4.9 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](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/jm100157m
10572649 117737 None 0 Human Functional pEC50 = 8.1 8.1 912 2
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 393 6 1 4 4.3 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc([N+](=O)[O-])c2)cc1 10.1021/jm000229p
CHEMBL340131 117737 None 0 Human Functional pEC50 = 8.1 8.1 912 2
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 393 6 1 4 4.3 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc([N+](=O)[O-])c2)cc1 10.1021/jm000229p
71461667 79205 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 373 0 3 4 2.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(N)C1C5 10.1021/jm021073r
CHEMBL2113376 79205 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 373 0 3 4 2.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(N)C1C5 10.1021/jm021073r
CHEMBL3580749 214236 None 0 Human Functional pEC50 = 8.1 8.1 -28 6
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 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(F)cc2F)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acsmedchemlett.5b00056
90656668 111017 None 0 Human Functional pEC50 = 8.1 8.1 2 3
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 501 6 2 5 4.9 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
CHEMBL3262091 111017 None 0 Human Functional pEC50 = 8.1 8.1 2 3
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 501 6 2 5 4.9 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
11796211 18115 None 0 Human Functional pEC50 = 8.1 8.1 575 3
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 416 5 1 2 5.7 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(Cl)c(Cl)c2)cc1 10.1021/jm000229p
CHEMBL126857 18115 None 0 Human Functional pEC50 = 8.1 8.1 575 3
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 416 5 1 2 5.7 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(Cl)c(Cl)c2)cc1 10.1021/jm000229p
71819401 92084 None 0 Human Functional pEC50 = 7.1 7.1 -7 5
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 301 0 2 4 1.7 C[C@@H]1C[C@H]2[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@@H](O5)[C@H]1O 10.1016/j.bmcl.2013.06.084
CHEMBL2418739 92084 None 0 Human Functional pEC50 = 7.1 7.1 -7 5
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 301 0 2 4 1.7 C[C@@H]1C[C@H]2[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@@H](O5)[C@H]1O 10.1016/j.bmcl.2013.06.084
24768355 168998 None 0 Human Functional pEC50 = 7.1 7.1 -4 4
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 1077 22 9 9 4.7 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm070332f
CHEMBL438389 168998 None 0 Human Functional pEC50 = 7.1 7.1 -4 4
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 1077 22 9 9 4.7 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm070332f
156043182 183244 None 0 Human Functional pEC50 = 7.1 7.1 -67 2
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 379 7 2 3 4.5 OCCC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
CHEMBL4795160 183244 None 0 Human Functional pEC50 = 7.1 7.1 -67 2
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 379 7 2 3 4.5 OCCC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
179340 495 None 33 Human Functional pEC50 = 5.1 5.1 -15848 3
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 414 7 1 3 4.1 O[C@H]1CCN(C1)C[C@@H](N(C(=O)C(c1ccccc1)c1ccccc1)C)c1ccccc1 10.1016/j.bmcl.2014.12.064
9279 495 None 33 Human Functional pEC50 = 5.1 5.1 -15848 3
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 414 7 1 3 4.1 O[C@H]1CCN(C1)C[C@@H](N(C(=O)C(c1ccccc1)c1ccccc1)C)c1ccccc1 10.1016/j.bmcl.2014.12.064
CHEMBL1190199 495 None 33 Human Functional pEC50 = 5.1 5.1 -15848 3
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 414 7 1 3 4.1 O[C@H]1CCN(C1)C[C@@H](N(C(=O)C(c1ccccc1)c1ccccc1)C)c1ccccc1 10.1016/j.bmcl.2014.12.064
DB05104 495 None 33 Human Functional pEC50 = 5.1 5.1 -15848 3
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 414 7 1 3 4.1 O[C@H]1CCN(C1)C[C@@H](N(C(=O)C(c1ccccc1)c1ccccc1)C)c1ccccc1 10.1016/j.bmcl.2014.12.064
164617754 184693 None 0 Rat Functional pEC50 = 6.1 6.1 -190 2
Agonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 592 9 1 6 6.7 COc1ccc(CNc2cccc([C@H]3C[C@@]45CC[C@]3(OC)[C@@H]3Oc6c(OC)ccc7c6[C@@]34CCN(CC3CC3)[C@@H]5C7)c2)cc1 10.1021/acs.jmedchem.1c01082
CHEMBL4848808 184693 None 0 Rat Functional pEC50 = 6.1 6.1 -190 2
Agonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 592 9 1 6 6.7 COc1ccc(CNc2cccc([C@H]3C[C@@]45CC[C@]3(OC)[C@@H]3Oc6c(OC)ccc7c6[C@@]34CCN(CC3CC3)[C@@H]5C7)c2)cc1 10.1021/acs.jmedchem.1c01082
44254505 198708 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 348 2 1 3 3.3 CN(C)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL561805 198708 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 348 2 1 3 3.3 CN(C)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
25129435 187609 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 335 2 1 4 3.4 COC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
CHEMBL494265 187609 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 335 2 1 4 3.4 COC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
25129090 187326 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 291 1 1 2 3.9 Cc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
CHEMBL492448 187326 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 291 1 1 2 3.9 Cc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm8008986
162669476 182848 None 0 Human Functional pEC50 = 6.1 6.1 -3 3
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 1055 29 14 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C)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
CHEMBL4790011 182848 None 0 Human Functional pEC50 = 6.1 6.1 -3 3
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 1055 29 14 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C)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
89978858 159996 None 0 Human Functional pEC50 = 5.1 5.1 -1071 3
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 587 10 1 7 5.7 CO[C@]12CC[C@@]3(C[C@@H]1COCc1cc4ccccc4s1)[C@H]1Cc4ccc(OCCO)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL4106985 159996 None 0 Human Functional pEC50 = 5.1 5.1 -1071 3
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 587 10 1 7 5.7 CO[C@]12CC[C@@]3(C[C@@H]1COCc1cc4ccccc4s1)[C@H]1Cc4ccc(OCCO)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
162669476 182848 None 0 Human Functional pEC50 = 6.1 6.1 -3 3
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 1055 29 14 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C)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
CHEMBL4790011 182848 None 0 Human Functional pEC50 = 6.1 6.1 -3 3
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 1055 29 14 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C)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
118725855 117244 None 0 Human Functional pEC50 = 7.1 7.1 -40 3
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 373 5 2 4 3.9 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1cc2ccccc2[nH]1 10.1016/j.bmcl.2014.12.064
CHEMBL3394005 117244 None 0 Human Functional pEC50 = 7.1 7.1 -40 3
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 373 5 2 4 3.9 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1cc2ccccc2[nH]1 10.1016/j.bmcl.2014.12.064
44396503 67369 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 443 7 3 4 2.6 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCCc1ccccc1 10.1021/jm030548r
CHEMBL188558 67369 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 443 7 3 4 2.6 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCCc1ccccc1 10.1021/jm030548r
44573291 187820 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 416 6 2 5 3.5 COc1ccc(CNC(=O)C2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)cc1 10.1016/j.bmcl.2009.01.106
CHEMBL495345 187820 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 416 6 2 5 3.5 COc1ccc(CNC(=O)C2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)cc1 10.1016/j.bmcl.2009.01.106
101806592 114063 None 0 Human Functional pEC50 = 7.1 7.1 -1 2
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 355 2 2 6 2.6 C[C@@]1(c2cccc(O)c2)O[C@H]2CO[C@@H]3N2[C@H]1O[C@]3(C)c1cccc(O)c1 10.1021/ml5000542
CHEMBL3326354 114063 None 0 Human Functional pEC50 = 7.1 7.1 -1 2
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 355 2 2 6 2.6 C[C@@]1(c2cccc(O)c2)O[C@H]2CO[C@@H]3N2[C@H]1O[C@]3(C)c1cccc(O)c1 10.1021/ml5000542
23723457 54842 None 39 Human Functional pEC50 = 5.1 5.1 -1 2
Inhibition of delta opioid receptor (unknown origin) expressed in human UO5S cells assessed as increase in beta arrestin recruitmentInhibition of delta opioid receptor (unknown origin) expressed in human UO5S cells assessed as increase in beta arrestin recruitment
ChEMBL 408 8 1 4 4.4 CCOC(=O)C1(CCc2ccccc2)CCN(Cc2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2019.111701
CHEMBL1612697 54842 None 39 Human Functional pEC50 = 5.1 5.1 -1 2
Inhibition of delta opioid receptor (unknown origin) expressed in human UO5S cells assessed as increase in beta arrestin recruitmentInhibition of delta opioid receptor (unknown origin) expressed in human UO5S cells assessed as increase in beta arrestin recruitment
ChEMBL 408 8 1 4 4.4 CCOC(=O)C1(CCc2ccccc2)CCN(Cc2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2019.111701
10183838 72672 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 472 7 1 4 4.7 O=S(=O)(Nc1ccccc1)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1 10.1016/j.bmcl.2005.09.025
CHEMBL199518 72672 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 472 7 1 4 4.7 O=S(=O)(Nc1ccccc1)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1 10.1016/j.bmcl.2005.09.025
68090936 160848 None 0 Human Functional pEC50 = 6.1 6.1 -4 3
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 480 6 0 7 4.0 COc1ccc2c3c1O[C@@H]1[C@]34CCN(C)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1c(C)noc1C)C2 nan
CHEMBL4114002 160848 None 0 Human Functional pEC50 = 6.1 6.1 -4 3
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 480 6 0 7 4.0 COc1ccc2c3c1O[C@@H]1[C@]34CCN(C)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1c(C)noc1C)C2 nan
162651726 180395 None 0 Human Functional pEC50 = 6.1 6.1 -2 3
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 1350 33 15 16 1.1 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](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2Cc3ccc(O)cc3C[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4750783 180395 None 0 Human Functional pEC50 = 6.1 6.1 -2 3
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 1350 33 15 16 1.1 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](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2Cc3ccc(O)cc3C[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
164620054 185772 None 0 Rat Functional pEC50 = 6.1 6.1 -14 2
Agonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 526 8 1 5 5.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1cccc(NCC3CC3)c1)C2 10.1021/acs.jmedchem.1c01082
CHEMBL4864911 185772 None 0 Rat Functional pEC50 = 6.1 6.1 -14 2
Agonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
ChEMBL 526 8 1 5 5.9 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](c1cccc(NCC3CC3)c1)C2 10.1021/acs.jmedchem.1c01082
44573403 187398 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 269 3 1 4 2.5 COc1cccc(C2(C)CN(c3cc(N)ccn3)C2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL492909 187398 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 269 3 1 4 2.5 COc1cccc(C2(C)CN(c3cc(N)ccn3)C2)c1 10.1016/j.bmcl.2009.01.106
CHEMBL261608 212978 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 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)OCc1ccccc1 10.1021/jm070332f
11750461 169250 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 418 6 3 4 3.6 CCCc1[nH]c([C@@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1C 10.1021/jm030548r
CHEMBL440380 169250 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
ChEMBL 418 6 3 4 3.6 CCCc1[nH]c([C@@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1C 10.1021/jm030548r
9909743 35264 None 1 Mouse Functional pEC50 = 7.1 7.1 -19 4
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 414 5 1 3 5.6 CC(C)(C)c1ccc(C(c2cccc(O)c2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm980374r
CHEMBL143592 35264 None 1 Mouse Functional pEC50 = 7.1 7.1 -19 4
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 414 5 1 3 5.6 CC(C)(C)c1ccc(C(c2cccc(O)c2)N2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm980374r
4885516 36494 None 3 Human Functional pEC50 = 4.1 4.1 - 1
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 405 8 1 5 2.0 COc1ccc(C(CNC(=O)c2ccc(S(=O)(=O)N(C)C)cc2)N(C)C)cc1 nan
CHEMBL1447552 36494 None 3 Human Functional pEC50 = 4.1 4.1 - 1
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 405 8 1 5 2.0 COc1ccc(C(CNC(=O)c2ccc(S(=O)(=O)N(C)C)cc2)N(C)C)cc1 nan
86711645 160901 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
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 474 6 1 5 3.4 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C(N)=O)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
CHEMBL4114477 160901 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
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 474 6 1 5 3.4 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C(N)=O)c5c4[C@@]3(CCN1C)[C@H]2O5 nan
45485982 199896 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 0 5 5.6 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3ccoc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
CHEMBL569704 199896 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 0 5 5.6 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3ccoc3)CC2)cc1 10.1016/j.bmcl.2009.09.072
44339409 109018 None 0 Human Functional pEC50 = 7.1 7.1 -8 2
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 443 7 0 4 4.5 O=C1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4cccc5c4C2(CCN3CC2CC2)C1O5 10.1021/jm031126k
CHEMBL321170 109018 None 0 Human Functional pEC50 = 7.1 7.1 -8 2
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 443 7 0 4 4.5 O=C1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4cccc5c4C2(CCN3CC2CC2)C1O5 10.1021/jm031126k
2860484 31097 None 7 Human Functional pEC50 = 4.1 4.1 - 1
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 386 3 1 2 4.8 CN1C(CC(=O)Nc2ccc(Br)cc2)c2ccccc2CC1(C)C nan
CHEMBL1399743 31097 None 7 Human Functional pEC50 = 4.1 4.1 - 1
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 386 3 1 2 4.8 CN1C(CC(=O)Nc2ccc(Br)cc2)c2ccccc2CC1(C)C nan
25137868 14523 None 0 Human Functional pEC50 = 4.1 4.1 - 1
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 339 8 0 3 4.3 CCC(=O)OC(Cc1ccccc1)(c1ccccc1)[C@H](C)CN(C)C nan
CHEMBL1201790 14523 None 0 Human Functional pEC50 = 4.1 4.1 - 1
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 339 8 0 3 4.3 CCC(=O)OC(Cc1ccccc1)(c1ccccc1)[C@H](C)CN(C)C nan
CHEMBL1864323 14523 None 0 Human Functional pEC50 = 4.1 4.1 - 1
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 339 8 0 3 4.3 CCC(=O)OC(Cc1ccccc1)(c1ccccc1)[C@H](C)CN(C)C nan
89978589 160377 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 721 23 0 10 5.2 COCCOCCOCCOCCOCCOc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
CHEMBL4110312 160377 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
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 721 23 0 10 5.2 COCCOCCOCCOCCOCCOc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2 nan
44433400 155067 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assay
ChEMBL 387 2 3 6 1.2 CO[C@]12C(O)C[C@@]3(C[C@@H]1[C@@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1016/j.bmcl.2007.06.050
CHEMBL401245 155067 None 0 Human Functional pEC50 = 7.1 7.1 -2 3
Agonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor expressed in CHO membrane by [35S]GTPgammaS binding assay
ChEMBL 387 2 3 6 1.2 CO[C@]12C(O)C[C@@]3(C[C@@H]1[C@@H](C)O)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1016/j.bmcl.2007.06.050
168274223 190575 None 0 Rat Functional pEC50 = 6.1 6.1 -58884 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 501 6 1 5 5.0 COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)[C@H](O)c4ccccc4)[C@@H](C2)N(CC2CC2)CC[C@]315 10.1021/acs.jmedchem.2c00014
CHEMBL5178795 190575 None 0 Rat Functional pEC50 = 6.1 6.1 -58884 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 501 6 1 5 5.0 COc1ccc2c3c1O[C@H]1[C@@]4(OC)CC[C@@]5(C[C@@]4(C)[C@H](O)c4ccccc4)[C@@H](C2)N(CC2CC2)CC[C@]315 10.1021/acs.jmedchem.2c00014
11452117 187612 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 390 4 0 3 4.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCN(C)CC3)Oc3ccccc32)cc1 10.1021/jm8008986
CHEMBL494275 187612 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 390 4 0 3 4.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCN(C)CC3)Oc3ccccc32)cc1 10.1021/jm8008986
71605589 87561 None 0 Human Functional pEC50 = 7.1 7.1 -162 2
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 640 12 6 7 2.4 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCN(C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1)c1ccco1 10.1021/jm400195y
CHEMBL2335120 87561 None 0 Human Functional pEC50 = 7.1 7.1 -162 2
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 640 12 6 7 2.4 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCN(C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1)c1ccco1 10.1021/jm400195y
CHEMBL205965 211628 None 0 Human Functional pEC50 = 6.1 6.1 -42 5
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]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
CHEMBL205965 211628 None 0 Human Functional pEC50 = 6.1 6.1 -42 5
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]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
162670764 183057 None 0 Human Functional pEC50 = 6.1 6.1 -31 5
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 1041 29 14 13 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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
CHEMBL4792870 183057 None 0 Human Functional pEC50 = 6.1 6.1 -31 5
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 1041 29 14 13 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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
172464002 196592 None 0 Human Functional pEC50 = 5.1 5.1 -1 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)C/C=C/CCCC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5427400 196592 None 0 Human Functional pEC50 = 5.1 5.1 -1 4
Agonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at DOR (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1136 24 13 13 -0.8 CN1C(=O)CNC(=O)[C@@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)C/C=C/CCCC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
162657942 181093 None 0 Human Functional pEC50 = 6.1 6.1 -229 4
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 1366 36 16 16 1.5 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](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL4758754 181093 None 0 Human Functional pEC50 = 6.1 6.1 -229 4
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 1366 36 16 16 1.5 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](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)O)C(C)(C)C)C1=O 10.1021/acs.jmedchem.0c01376
162670764 183057 None 0 Human Functional pEC50 = 6.1 6.1 -31 5
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 1041 29 14 13 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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
CHEMBL4792870 183057 None 0 Human Functional pEC50 = 6.1 6.1 -31 5
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 1041 29 14 13 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=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
25256781 187491 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 417 5 1 6 3.7 COc1ccc(C(=O)N(c2cc(C)ccn2)C2CCN(c3cc(N)ccn3)CC2)cc1 10.1016/j.bmcl.2009.01.106
CHEMBL493515 187491 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 417 5 1 6 3.7 COc1ccc(C(=O)N(c2cc(C)ccn2)C2CCN(c3cc(N)ccn3)CC2)cc1 10.1016/j.bmcl.2009.01.106
44306988 102131 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 404 5 1 3 4.9 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3C)c2ccc(O)cc2)cc1 10.1016/j.bmcl.2004.02.051
CHEMBL302121 102131 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 404 5 1 3 4.9 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3C)c2ccc(O)cc2)cc1 10.1016/j.bmcl.2004.02.051
73330543 92862 None 0 Mouse Functional pEC50 = 8.0 8.0 -6 3
Agonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 414 3 2 4 3.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@H](NC(=O)/C=C/c2ccccc2)C=C[C@H]3[C@H]1C5 10.1016/j.ejmech.2013.09.031
CHEMBL2437063 92862 None 0 Mouse Functional pEC50 = 8.0 8.0 -6 3
Agonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at mouse cloned delta opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 414 3 2 4 3.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@H](NC(=O)/C=C/c2ccccc2)C=C[C@H]3[C@H]1C5 10.1016/j.ejmech.2013.09.031
1607 1306 None 30 Human Functional pEC50 = 8.0 8.0 -22 6
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2022.114728
6917707 1306 None 30 Human Functional pEC50 = 8.0 8.0 -22 6
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2022.114728
CHEMBL340032 1306 None 30 Human Functional pEC50 = 8.0 8.0 -22 6
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2022.114728
DB08856 1306 None 30 Human Functional pEC50 = 8.0 8.0 -22 6
Agonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assayAgonist activity at human DOR receptor expressed in CHO-K1 cells assessed as decrease in intracellular cAMP level measured after 1 hr by LANCE ultra cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2022.114728
90655827 111270 None 0 Human Functional pEC50 = 8.0 8.0 2 3
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 550 5 1 6 4.2 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CCc3ccccc3)[C@@H]4C7)[C@H]25)N1Cc1ccccc1 10.1021/ml400491k
CHEMBL3264746 111270 None 0 Human Functional pEC50 = 8.0 8.0 2 3
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 550 5 1 6 4.2 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CCc3ccccc3)[C@@H]4C7)[C@H]25)N1Cc1ccccc1 10.1021/ml400491k
CHEMBL294616 213353 None 0 Human Functional pEC50 = 8.0 8.0 -2 7
Agonist activity at human DOR expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human DOR expressed in CHO 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 10.1016/j.bmcl.2014.08.012
CHEMBL3580747 214234 None 0 Human Functional pEC50 = 8.0 8.0 -1 2
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 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(C(F)(F)F)cc2)NC1=O 10.1021/acsmedchemlett.5b00056
44408484 137595 None 0 Human Functional pEC50 = 8.0 8.0 -1 5
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 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL375412 137595 None 0 Human Functional pEC50 = 8.0 8.0 -1 5
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 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
44418924 156974 None 0 Human Functional pEC50 = 8.0 8.0 1 5
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 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=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
CHEMBL407198 156974 None 0 Human Functional pEC50 = 8.0 8.0 1 5
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 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=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
44408484 137595 None 0 Human Functional pEC50 = 8.0 8.0 -1 5
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 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL375412 137595 None 0 Human Functional pEC50 = 8.0 8.0 -1 5
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 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[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](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL389651 214889 None 0 Human Functional pEC50 = 8.0 8.0 -3 4
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(C)C)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
46877633 204709 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 426 2 2 5 3.6 Oc1ccc2c3c1O[C@H]1c4nc5ccccc5cc4C[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1016/j.bmcl.2015.05.038
CHEMBL610012 204709 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 426 2 2 5 3.6 Oc1ccc2c3c1O[C@H]1c4nc5ccccc5cc4C[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1016/j.bmcl.2015.05.038
172439679 195348 None 0 Human Functional pEC50 = 8.0 8.0 3 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1150 24 13 13 -0.4 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
CHEMBL5401796 195348 None 0 Human Functional pEC50 = 8.0 8.0 3 4
Agonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assayAgonist activity at NPFF1R (unknown origin) transfected in CHO cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
ChEMBL 1150 24 13 13 -0.4 CN1C(=O)CNC(=O)[C@H](N[C@@H](Cc2ccc(O)cc2)C(=O)O)CCCC/C=C\CC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.3c02093
44421409 84329 None 0 Human Functional pEC50 = 8.0 8.0 75 3
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 468 2 2 5 4.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2Cc2ccccc2)CCCC4)C[C@@]3(O)C1C5 10.1021/jm040817t
CHEMBL221421 84329 None 0 Human Functional pEC50 = 8.0 8.0 75 3
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 468 2 2 5 4.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2Cc2ccccc2)CCCC4)C[C@@]3(O)C1C5 10.1021/jm040817t
11382472 197754 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 348 3 2 3 3.4 CCNC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL551412 197754 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 348 3 2 3 3.4 CCNC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1 10.1021/jm900773n
CHEMBL2387212 212860 None 0 Human Functional pEC50 = 7.1 7.1 1 3
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](CCC(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)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 10.1016/j.bmcl.2013.03.065
44337642 109766 None 0 Human Functional pEC50 = 7.0 7.0 10 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 440 2 2 3 5.6 CC(C)=CC[C@@]12Cc3c([nH]c4ccccc34)[C@]3(C)Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm030801n
CHEMBL322875 109766 None 0 Human Functional pEC50 = 7.0 7.0 10 3
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
ChEMBL 440 2 2 3 5.6 CC(C)=CC[C@@]12Cc3c([nH]c4ccccc34)[C@]3(C)Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5 10.1021/jm030801n
5487663 72864 None 12 Mouse Functional pEC50 = 7.0 7.0 -15 4
Agonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at mouse delta opioid receptor expressed in CHO 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/ml500241n
CHEMBL200199 72864 None 12 Mouse Functional pEC50 = 7.0 7.0 -15 4
Agonist activity at mouse delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at mouse delta opioid receptor expressed in CHO 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/ml500241n
118200491 165810 None 0 Rat Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 425 5 1 5 3.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(CO)C2 10.1016/j.bmc.2018.07.020
CHEMBL4245818 165810 None 0 Rat Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 425 5 1 5 3.3 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(CO)C2 10.1016/j.bmc.2018.07.020
137630443 161161 None 0 Rat Functional pEC50 = 6.0 6.0 -47 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 405 4 2 3 4.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccc(C(F)(F)F)cc2)CC3)c1 10.1016/j.bmc.2017.02.064
CHEMBL4102551 161161 None 0 Rat Functional pEC50 = 6.0 6.0 -47 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 405 4 2 3 4.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccc(C(F)(F)F)cc2)CC3)c1 10.1016/j.bmc.2017.02.064
CHEMBL4116648 161161 None 0 Rat Functional pEC50 = 6.0 6.0 -47 3
Agonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting methodAgonist activity at rat delta opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 405 4 2 3 4.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccc(C(F)(F)F)cc2)CC3)c1 10.1016/j.bmc.2017.02.064
CHEMBL3609619 214293 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 None None None C[C@@H](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
16394140 59364 None 4 Human Functional pEC50 = 4.0 4.0 - 1
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 326 5 1 3 3.3 CN(C)C(CNC(=O)c1ccc(C(F)(F)F)cc1)c1ccco1 nan
CHEMBL1707116 59364 None 4 Human Functional pEC50 = 4.0 4.0 - 1
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 326 5 1 3 3.3 CN(C)C(CNC(=O)c1ccc(C(F)(F)F)cc1)c1ccco1 nan
CHEMBL5085013 217432 None 0 Human Functional pEC50 = 6.0 6.0 -11 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
44255043 198772 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 378 4 1 5 2.9 CCN(CC)C(=O)c1ncc(C2=CC3(CCNCC3)Oc3ccccc32)cn1 10.1021/jm900773n
CHEMBL562280 198772 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 378 4 1 5 2.9 CCN(CC)C(=O)c1ncc(C2=CC3(CCNCC3)Oc3ccccc32)cn1 10.1021/jm900773n
CHEMBL5085013 217432 None 0 Human Functional pEC50 = 6.0 6.0 -11 4
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
1847781 37739 None 2 Human Functional pEC50 = 5.0 5.0 - 1
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 373 3 2 4 3.3 Cc1cc(/C=C2/C(=O)NN(c3ccccc3)C2=O)c(C)n1-c1ccc(O)cc1 nan
CHEMBL1457803 37739 None 2 Human Functional pEC50 = 5.0 5.0 - 1
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 373 3 2 4 3.3 Cc1cc(/C=C2/C(=O)NN(c3ccccc3)C2=O)c(C)n1-c1ccc(O)cc1 nan
162665777 182457 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 521 11 1 4 5.1 CCC(=O)N(Cc1cccs1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
CHEMBL4784650 182457 None 0 Human Functional pEC50 = 7.0 7.0 1 2
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 521 11 1 4 5.1 CCC(=O)N(Cc1cccs1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
1623 1560 None 36 Human Functional pEC50 = 6.0 6.0 -109 6
Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None None 10.1021/jm060998u
5311080 1560 None 36 Human Functional pEC50 = 6.0 6.0 -109 6
Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None None 10.1021/jm060998u
CHEMBL316446 1560 None 36 Human Functional pEC50 = 6.0 6.0 -109 6
Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None None 10.1021/jm060998u
134578291 196080 None 0 Human Functional pEC50 = 6.0 6.0 -128 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CN4CCCC4)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
CHEMBL5416582 196080 None 0 Human Functional pEC50 = 6.0 6.0 -128 3
Agonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 minsAgonist activity at human DOP expressed in CHO cells membrane assessed as increase in [35S]GTPgammaS binding incubated for 60 mins
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3c(CN4CCCC4)cc4ccccc43)CC2)CC1 10.1016/j.bmc.2023.117421
11200189 285 None 27 Human Functional pEC50 = 7.0 7.0 - 1
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 392 4 2 4 3.8 CCN(C(=O)c1ccc(c(c1)O)C1=CC2(CCNCC2)Oc2c1cccc2)CC 10.1021/jm900773n
9003 285 None 27 Human Functional pEC50 = 7.0 7.0 - 1
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 392 4 2 4 3.8 CCN(C(=O)c1ccc(c(c1)O)C1=CC2(CCNCC2)Oc2c1cccc2)CC 10.1021/jm900773n
CHEMBL561339 285 None 27 Human Functional pEC50 = 7.0 7.0 - 1
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 392 4 2 4 3.8 CCN(C(=O)c1ccc(c(c1)O)C1=CC2(CCNCC2)Oc2c1cccc2)CC 10.1021/jm900773n
CHEMBL5091560 217804 None 0 Human Functional pEC50 = 7.0 7.0 -2 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
CHEMBL5091560 217804 None 0 Human Functional pEC50 = 7.0 7.0 -2 5
Agonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at DOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
10315939 167974 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 351 0 2 6 1.4 Cc1ncc2c(n1)C1Oc3c(O)ccc4c3C13CCN(C)C(C4)C3(O)C2 10.1016/s0960-894x(99)00608-3
CHEMBL431074 167974 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Agonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligandAgonistic activity against human opioid Delta receptor transfected into Chinese hamster ovary (CHO) cells using [3H]Cl-DPDPE as radioligand
ChEMBL 351 0 2 6 1.4 Cc1ncc2c(n1)C1Oc3c(O)ccc4c3C13CCN(C)C(C4)C3(O)C2 10.1016/s0960-894x(99)00608-3
168296046 192410 None 0 Rat Functional pEC50 = 6.0 6.0 -18 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 529 7 0 6 5.2 COc1cccc(C(=O)[C@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)c1 10.1021/acs.jmedchem.2c00014
CHEMBL5206165 192410 None 0 Rat Functional pEC50 = 6.0 6.0 -18 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 529 7 0 6 5.2 COc1cccc(C(=O)[C@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(OC)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)c1 10.1021/acs.jmedchem.2c00014
168285744 191470 None 0 Human Functional pEC50 = 6.0 6.0 -20 4
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 555 15 6 6 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1039/D1MD00025J
CHEMBL5192115 191470 None 0 Human Functional pEC50 = 6.0 6.0 -20 4
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 555 15 6 6 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1039/D1MD00025J
168285744 191470 None 0 Human Functional pEC50 = 6.0 6.0 -20 4
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 555 15 6 6 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1039/D1MD00025J
CHEMBL5192115 191470 None 0 Human Functional pEC50 = 6.0 6.0 -20 4
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 555 15 6 6 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)C/C=C(\F)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1039/D1MD00025J
CHEMBL260120 212976 None 0 Human Functional pEC50 = 6.0 6.0 -288 5
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 C[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)CC(N)=O)N(C)C(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm200894e
CHEMBL246479 212960 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc2nc(N)sc2c1)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1016/j.bmcl.2007.01.092
46227361 205040 None 0 Human Functional pEC50 = 7.0 7.0 -38 5
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 18 10 12 4.6 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
CHEMBL611925 205040 None 0 Human Functional pEC50 = 7.0 7.0 -38 5
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 18 10 12 4.6 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
3319690 59828 None 4 Human Functional pEC50 = 5.0 5.0 - 1
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 481 10 2 5 4.4 COc1ccc(NC(=O)COc2ccccc2C(=O)NCC(c2ccccc2)N(C)C)cc1Cl nan
CHEMBL1727246 59828 None 4 Human Functional pEC50 = 5.0 5.0 - 1
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 481 10 2 5 4.4 COc1ccc(NC(=O)COc2ccccc2C(=O)NCC(c2ccccc2)N(C)C)cc1Cl nan
46227361 205040 None 0 Human Functional pEC50 = 7.0 7.0 -38 5
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 18 10 12 4.6 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
CHEMBL611925 205040 None 0 Human Functional pEC50 = 7.0 7.0 -38 5
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 18 10 12 4.6 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2009.08.035
11188794 168758 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 400 5 0 5 5.0 c1ccc(Cn2ccnc2C2(c3ccccc3)CCN(c3nccs3)CC2)cc1 10.1016/j.bmcl.2005.09.025
CHEMBL436323 168758 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 400 5 0 5 5.0 c1ccc(Cn2ccnc2C2(c3ccccc3)CCN(c3nccs3)CC2)cc1 10.1016/j.bmcl.2005.09.025
10499145 18153 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 366 5 1 2 4.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(F)cc2)cc1 10.1021/jm000229p
CHEMBL126946 18153 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 366 5 1 2 4.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(F)cc2)cc1 10.1021/jm000229p
25232541 192996 None 0 Mouse Functional pEC50 = 7.0 7.0 -29 4
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 497 4 3 6 3.3 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2cn1 10.1016/j.bmc.2015.02.055
CHEMBL522201 192996 None 0 Mouse Functional pEC50 = 7.0 7.0 -29 4
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 497 4 3 6 3.3 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2cn1 10.1016/j.bmc.2015.02.055
44254059 197660 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 366 4 1 4 3.7 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)o1 10.1021/jm900773n
CHEMBL550669 197660 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 366 4 1 4 3.7 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)o1 10.1021/jm900773n
44255045 198388 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 394 4 1 3 4.3 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)c(F)c1 10.1021/jm900773n
CHEMBL559414 198388 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 394 4 1 3 4.3 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)c(F)c1 10.1021/jm900773n
145984702 165591 None 0 Rat Functional pEC50 = 5 5.0 -6 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 499 6 0 5 5.2 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccccc1)C2 10.1016/j.bmc.2018.07.020
CHEMBL4240426 165591 None 0 Rat Functional pEC50 = 5 5.0 -6 3
Agonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysisAgonist activity at rat DOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding based liquid scintillation counting analysis
ChEMBL 499 6 0 5 5.2 COc1ccc2c3c1O[C@@H]1[C@]34CCN(CC3CC3)[C@H](C2)[C@]42CC[C@@]1(OC)[C@@](C)(C(=O)c1ccccc1)C2 10.1016/j.bmc.2018.07.020
71455949 83885 None 0 Human Functional pED50 = 10.0 10.0 - 1
Partial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayPartial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 745 18 5 6 4.4 CCCCCCNC(=O)c1ccc(C[C@H](N)C(=O)N2Cc3ccccc3CC2C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)O)cc1 10.1016/j.bmcl.2012.01.063
CHEMBL2206325 83885 None 0 Human Functional pED50 = 10.0 10.0 - 1
Partial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayPartial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 745 18 5 6 4.4 CCCCCCNC(=O)c1ccc(C[C@H](N)C(=O)N2Cc3ccccc3CC2C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)O)cc1 10.1016/j.bmcl.2012.01.063
71459668 83886 None 0 Human Functional pED50 = 9.6 9.6 - 1
Partial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayPartial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 801 22 5 6 5.9 CCCCCCCCCCNC(=O)c1ccc(C[C@H](N)C(=O)N2Cc3ccccc3CC2C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)O)cc1 10.1016/j.bmcl.2012.01.063
CHEMBL2206326 83886 None 0 Human Functional pED50 = 9.6 9.6 - 1
Partial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayPartial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 801 22 5 6 5.9 CCCCCCCCCCNC(=O)c1ccc(C[C@H](N)C(=O)N2Cc3ccccc3CC2C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)O)cc1 10.1016/j.bmcl.2012.01.063
44541641 83887 None 0 Human Functional pED50 = 9.4 9.4 - 0
Partial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayPartial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 841 17 5 6 5.7 N[C@@H](Cc1ccc(C(=O)NCCc2ccc(-c3ccccc3)cc2)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
CHEMBL2206327 83887 None 0 Human Functional pED50 = 9.4 9.4 - 0
Partial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayPartial agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 841 17 5 6 5.7 N[C@@H](Cc1ccc(C(=O)NCCc2ccc(-c3ccccc3)cc2)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
72735562 106387 None 0 Human Functional pED50 = 9.3 9.3 - 1
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 430 4 2 5 3.4 COCCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2017.04.059
CHEMBL3139154 106387 None 0 Human Functional pED50 = 9.3 9.3 - 1
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 430 4 2 5 3.4 COCCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2017.04.059
CHEMBL4296734 106387 None 0 Human Functional pED50 = 9.3 9.3 - 1
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 430 4 2 5 3.4 COCCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13 10.1016/j.bmcl.2017.04.059
71452441 83890 None 0 Human Functional pED50 = 9.3 9.3 - 1
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayAgonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 815 16 5 6 5.2 N[C@@H](Cc1ccc(C(=O)NCCc2ccc3ccccc3c2)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
CHEMBL2206330 83890 None 0 Human Functional pED50 = 9.3 9.3 - 1
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayAgonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 815 16 5 6 5.2 N[C@@H](Cc1ccc(C(=O)NCCc2ccc3ccccc3c2)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
71455950 83889 None 0 Human Functional pED50 = 9.0 9.0 - 1
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayAgonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 815 16 5 6 5.2 N[C@@H](Cc1ccc(C(=O)NCCc2cccc3ccccc23)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
CHEMBL2206329 83889 None 0 Human Functional pED50 = 9.0 9.0 - 1
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayAgonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 815 16 5 6 5.2 N[C@@H](Cc1ccc(C(=O)NCCc2cccc3ccccc23)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
71461393 83888 None 0 Human Functional pED50 = 8.8 8.8 - 1
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayAgonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 847 17 5 6 6.1 N[C@@H](Cc1ccc(C(=O)NCCc2ccc(C3CCCCC3)cc2)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
CHEMBL2206328 83888 None 0 Human Functional pED50 = 8.8 8.8 - 1
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayAgonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 847 17 5 6 6.1 N[C@@H](Cc1ccc(C(=O)NCCc2ccc(C3CCCCC3)cc2)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
71660127 90469 None 0 Human Functional pED50 = 5.9 5.9 - 0
Partial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysisPartial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
ChEMBL 467 6 1 3 6.0 Oc1ccc2c(c1)[C@]1(CCc3ccccc3)CCN(CCc3ccc(C(F)(F)F)cc3)C[C@@H]1O2 10.1016/j.bmc.2013.02.060
CHEMBL2386900 90469 None 0 Human Functional pED50 = 5.9 5.9 - 0
Partial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysisPartial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
ChEMBL 467 6 1 3 6.0 Oc1ccc2c(c1)[C@]1(CCc3ccccc3)CCN(CCc3ccc(C(F)(F)F)cc3)C[C@@H]1O2 10.1016/j.bmc.2013.02.060
45487174 201468 None 0 Human Functional pED50 = 6.8 6.8 - 0
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 349 3 1 3 4.1 Oc1cccc2c1O[C@H]1CCC[C@H]3CN(CCc4ccccc4)CC[C@]213 10.1021/jm901503e
CHEMBL585721 201468 None 0 Human Functional pED50 = 6.8 6.8 - 0
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 349 3 1 3 4.1 Oc1cccc2c1O[C@H]1CCC[C@H]3CN(CCc4ccccc4)CC[C@]213 10.1021/jm901503e
123924 3633 None 34 Human Functional pED50 = 7.6 7.6 1 9
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay
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/jm061325e
1611 3633 None 34 Human Functional pED50 = 7.6 7.6 1 9
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay
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/jm061325e
CHEMBL13470 3633 None 34 Human Functional pED50 = 7.6 7.6 1 9
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay
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/jm061325e
1627 2594 None 9 Human Functional pED50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm901503e
1845 2594 None 9 Human Functional pED50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm901503e
5288826 2594 None 9 Human Functional pED50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm901503e
5288826.0 2594 None 9 Human Functional pED50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm901503e
CHEMBL70 2594 None 9 Human Functional pED50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm901503e
DB00295 2594 None 9 Human Functional pED50 = 6.5 6.5 -13 9
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 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1021/jm901503e
16756840 142447 None 0 Human Functional pED50 = 6.5 6.5 -15 3
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay
ChEMBL 337 4 2 3 3.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1 10.1021/jm061325e
CHEMBL388873 142447 None 0 Human Functional pED50 = 6.5 6.5 -15 3
Agonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assayAgonist activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S assay
ChEMBL 337 4 2 3 3.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1 10.1021/jm061325e
71660125 90467 None 0 Human Functional pED50 = 6.5 6.5 - 0
Partial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysisPartial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
ChEMBL 417 6 1 3 5.1 Oc1ccc2c(c1)[C@]1(CCc3ccccc3)CCN(CCc3ccc(F)cc3)C[C@@H]1O2 10.1016/j.bmc.2013.02.060
CHEMBL2386898 90467 None 0 Human Functional pED50 = 6.5 6.5 - 0
Partial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysisPartial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
ChEMBL 417 6 1 3 5.1 Oc1ccc2c(c1)[C@]1(CCc3ccccc3)CCN(CCc3ccc(F)cc3)C[C@@H]1O2 10.1016/j.bmc.2013.02.060
71660087 90465 None 0 Human Functional pED50 = 6.4 6.4 - 0
Partial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysisPartial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
ChEMBL 399 6 1 3 5.0 Oc1ccc2c(c1)[C@]1(CCc3ccccc3)CCN(CCc3ccccc3)C[C@@H]1O2 10.1016/j.bmc.2013.02.060
CHEMBL2386896 90465 None 0 Human Functional pED50 = 6.4 6.4 - 0
Partial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysisPartial agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
ChEMBL 399 6 1 3 5.0 Oc1ccc2c(c1)[C@]1(CCc3ccccc3)CCN(CCc3ccccc3)C[C@@H]1O2 10.1016/j.bmc.2013.02.060
10788323 167943 None 0 Human Functional pED50 = 7.3 7.3 3 4
Agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysisAgonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
ChEMBL 421 8 1 4 4.1 C=CCN1C[C@H](C)N([C@H](c2ccc(C(=O)NCC)cc2)c2cccc(OC)c2)C[C@H]1C 10.1016/j.bmc.2013.02.060
CHEMBL430851 167943 None 0 Human Functional pED50 = 7.3 7.3 3 4
Agonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysisAgonist activity at human recombinant delta opioid receptor expressed in mouse/rat NG108-15 cell membranes assessed as stimulation of [35S]GTPgammaS binding after 3 hrs by liquid scintillation counting analysis
ChEMBL 421 8 1 4 4.1 C=CCN1C[C@H](C)N([C@H](c2ccc(C(=O)NCC)cc2)c2cccc(OC)c2)C[C@H]1C 10.1016/j.bmc.2013.02.060
CHEMBL294616 213353 None 0 Human Functional pED50 = 8.2 8.2 -2 7
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayAgonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1016/j.bmcl.2012.01.063
71452440 83884 None 0 Human Functional pED50 = 8.2 8.2 - 1
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayAgonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 804 16 6 6 4.5 N[C@@H](Cc1ccc(C(=O)NCCc2c[nH]c3ccccc23)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
CHEMBL2206323 83884 None 0 Human Functional pED50 = 8.2 8.2 - 1
Agonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assayAgonist activity at human delta opioid receptor expressed in HEK293 cells by [35S]GTP binding assay
ChEMBL 804 16 6 6 4.5 N[C@@H](Cc1ccc(C(=O)NCCc2c[nH]c3ccccc23)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
3029906 110246 None 0 Human Functional pED50 = 5.1 5.1 - 0
Agonist activity at human delta opioid receptor expressed CHO cells assessed as inhibition of [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed CHO cells assessed as inhibition of [35S]-GTP[gammaS] binding
ChEMBL 205 1 1 2 2.4 CN1CCC(C)(c2cccc(O)c2)CC1 10.1021/jm500184j
CHEMBL3237121 110246 None 0 Human Functional pED50 = 5.1 5.1 - 0
Agonist activity at human delta opioid receptor expressed CHO cells assessed as inhibition of [35S]-GTP[gammaS] bindingAgonist activity at human delta opioid receptor expressed CHO cells assessed as inhibition of [35S]-GTP[gammaS] binding
ChEMBL 205 1 1 2 2.4 CN1CCC(C)(c2cccc(O)c2)CC1 10.1021/jm500184j
CHEMBL2114469 211715 None 0 Rat Functional pIC50 = 11 11.0 125 2
Inhibitory activity against forskolin-stimulated cAMP production in chinese hamster ovary cells expressing Opioid receptor delta 1Inhibitory activity against forskolin-stimulated cAMP production in chinese hamster ovary cells expressing Opioid receptor delta 1
ChEMBL None None None CC(C)C[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@]1(NC(=O)[C@H](N)Cc2ccc(O)cc2)CCC[C@@H]1O)C(=O)O 10.1016/s0960-894x(98)00349-7
CHEMBL607401 218319 None 0 Mouse Functional pIC50 = 10.8 10.8 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](Cc1nc2ccccc2[nH]1)C(=O)O 10.1021/jm020336e
CHEMBL339320 214079 None 0 Mouse Functional pIC50 = 10.8 10.8 89 4
Inhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferensInhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferens
ChEMBL None None None CC1(C)SSC[C@@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm00027a018
44407872 75453 None 0 Mouse Functional pIC50 = 10.7 10.7 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 506 7 2 4 6.4 C[C@@H]1CN([C@H](c2ccc(-c3ccccc3C(=O)O)cc2)c2cccc(O)c2)[C@@H](C)CN1Cc1ccccc1 10.1016/j.bmcl.2005.10.102
CHEMBL204136 75453 None 0 Mouse Functional pIC50 = 10.7 10.7 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 506 7 2 4 6.4 C[C@@H]1CN([C@H](c2ccc(-c3ccccc3C(=O)O)cc2)c2cccc(O)c2)[C@@H](C)CN1Cc1ccccc1 10.1016/j.bmcl.2005.10.102
16087283 169607 None 0 Human Functional pIC50 = 10.7 10.7 -1 2
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 492 7 2 5 4.4 O=C1CC[C@@]2(NCCCc3ccc(Cl)cc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm060595u
CHEMBL443311 169607 None 0 Human Functional pIC50 = 10.7 10.7 -1 2
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 492 7 2 5 4.4 O=C1CC[C@@]2(NCCCc3ccc(Cl)cc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm060595u
CHEMBL169860 211298 None 0 Mouse Functional pIC50 = 10.7 10.7 - 1
In vitro biological activity by electrically induced smooth muscle contractions in mouse vas deferens (Opioid receptor delta 1); inhibitory concentration was evaluatedIn vitro biological activity by electrically induced smooth muscle contractions in mouse vas deferens (Opioid receptor delta 1); inhibitory concentration was evaluated
ChEMBL None None None Cc1cccc(C)c1C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C)C(C)C 10.1016/s0960-894x(02)00035-5
10481479 204195 None 0 Mouse Functional pIC50 = 10.6 10.6 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)
ChEMBL 511 6 4 5 3.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](C)c1nc2ccccc2[nH]1 10.1021/jm020336e
CHEMBL606603 204195 None 0 Mouse Functional pIC50 = 10.6 10.6 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)
ChEMBL 511 6 4 5 3.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](C)c1nc2ccccc2[nH]1 10.1021/jm020336e
11005741 204364 None 0 Mouse Functional pIC50 = 10.6 10.6 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)
ChEMBL 511 6 4 5 3.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](C)c1nc2ccccc2[nH]1 10.1021/jm020336e
CHEMBL607479 204364 None 0 Mouse Functional pIC50 = 10.6 10.6 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)
ChEMBL 511 6 4 5 3.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](C)c1nc2ccccc2[nH]1 10.1021/jm020336e
CHEMBL2372314 212674 None 0 Mouse Functional pIC50 = 10.6 10.6 35 3
Inhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferensInhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferens
ChEMBL None None None CC1(C)SSC[C@@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)O)NC(=O)[C@H](Cc2ccc(Br)cc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm00027a018
CHEMBL2372327 212678 None 0 Mouse Functional pIC50 = 10.6 10.6 25 3
Inhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferensInhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferens
ChEMBL None None None CC1(C)SSC[C@@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)O)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm00027a018
50994531 57238 None 0 Mouse Functional pIC50 = 10.5 10.5 6 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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 57238 None 0 Mouse Functional pIC50 = 10.5 10.5 6 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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
16087270 97104 None 0 Human Functional pIC50 = 10.5 10.5 -1 2
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 506 6 2 5 3.9 O=C(CCc1ccc(Cl)cc1)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5 10.1021/jm060595u
CHEMBL267027 97104 None 0 Human Functional pIC50 = 10.5 10.5 -1 2
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 506 6 2 5 3.9 O=C(CCc1ccc(Cl)cc1)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5 10.1021/jm060595u
10345770 8480 None 0 Mouse Functional pIC50 = 10.5 10.5 - 1
Functional bioactivity against delta opioid receptor in mouse vas deferensFunctional bioactivity against delta opioid receptor in mouse vas deferens
ChEMBL 497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCc1nc2ccccc2[nH]1 10.1021/jm058259l
CHEMBL109390 8480 None 0 Mouse Functional pIC50 = 10.5 10.5 - 1
Functional bioactivity against delta opioid receptor in mouse vas deferensFunctional bioactivity against delta opioid receptor in mouse vas deferens
ChEMBL 497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCc1nc2ccccc2[nH]1 10.1021/jm058259l
10345770 8480 None 0 Mouse Functional pIC50 = 10.5 10.5 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in 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/jm020336e
CHEMBL109390 8480 None 0 Mouse Functional pIC50 = 10.5 10.5 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in 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/jm020336e
44407697 74436 None 0 Mouse Functional pIC50 = 10.4 10.4 25118 2
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 499 7 2 5 4.5 C[C@H]1CN(Cc2ccccc2)[C@H](C)CN1[C@@H](c1cccc(O)c1)c1ccc2c(c1)CN(CC(=O)O)CC2 10.1016/j.bmcl.2005.10.102
CHEMBL202578 74436 None 0 Mouse Functional pIC50 = 10.4 10.4 25118 2
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 499 7 2 5 4.5 C[C@H]1CN(Cc2ccccc2)[C@H](C)CN1[C@@H](c1cccc(O)c1)c1ccc2c(c1)CN(CC(=O)O)CC2 10.1016/j.bmcl.2005.10.102
CHEMBL60936 218328 None 0 Rat Functional pIC50 = 10.2 10.2 38 2
Inhibitory activity against forskolin-stimulated cAMP production in chinese hamster ovary cells expressing Opioid receptor delta 1Inhibitory activity against forskolin-stimulated cAMP production in chinese hamster ovary cells expressing Opioid receptor delta 1
ChEMBL None None None CC(C)C[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@](C)(CO)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)O 10.1016/s0960-894x(98)00349-7
CHEMBL2372328 212679 None 0 Mouse Functional pIC50 = 10.1 10.1 6 3
Inhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferensInhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferens
ChEMBL None None None CC1(C)SSC[C@@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)O)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm00027a018
44138064 178991 None 0 Human Functional pIC50 = 10.1 10.1 354 2
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
ChEMBL 443 3 4 4 2.8 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)Cc1c([nH]c2ccccc12)C3 10.1016/j.bmcl.2009.02.078
CHEMBL469815 178991 None 0 Human Functional pIC50 = 10.1 10.1 354 2
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
ChEMBL 443 3 4 4 2.8 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)Cc1c([nH]c2ccccc12)C3 10.1016/j.bmcl.2009.02.078
CHEMBL124435 211119 None 0 Mouse Functional pIC50 = 10.1 10.1 5 3
Inhibition of electrically evoked contractions in mouse vas deferensInhibition of electrically evoked contractions in mouse vas deferens
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)C1(NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)Cc2ccccc2C1)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1021/jm00099a025
CHEMBL317956 213665 None 31 Mouse Functional pIC50 = 10.0 10.0 -1 7
Inhibitory activity against Mouse vas deferens smooth muscleInhibitory activity against Mouse vas deferens smooth muscle
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 10.1016/S0960-894X(01)81195-1
44348645 16878 None 0 Mouse Functional pIC50 = 9.9 9.9 3 3
Inhibition of electrically evoked contractions in mouse vas deferensInhibition of electrically evoked contractions in mouse vas deferens
ChEMBL 794 19 10 10 -1.3 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)C1(NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCc2ccccc2C1)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1021/jm00099a025
CHEMBL124941 16878 None 0 Mouse Functional pIC50 = 9.9 9.9 3 3
Inhibition of electrically evoked contractions in mouse vas deferensInhibition of electrically evoked contractions in mouse vas deferens
ChEMBL 794 19 10 10 -1.3 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)C1(NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCc2ccccc2C1)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1021/jm00099a025
10918703 3932 None 11 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
ChEMBL 555 8 5 6 3.0 Oc1cc(C)c(c(c1)C)C[C@@H](C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](c1[nH]c2c(n1)cccc2)CC(=O)O)N 10.1016/j.bmc.2010.06.073
9006 3932 None 11 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
ChEMBL 555 8 5 6 3.0 Oc1cc(C)c(c(c1)C)C[C@@H](C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](c1[nH]c2c(n1)cccc2)CC(=O)O)N 10.1016/j.bmc.2010.06.073
CHEMBL442577 3932 None 11 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
ChEMBL 555 8 5 6 3.0 Oc1cc(C)c(c(c1)C)C[C@@H](C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](c1[nH]c2c(n1)cccc2)CC(=O)O)N 10.1016/j.bmc.2010.06.073
CHEMBL540972 218206 None 0 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked contraction
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)c1nc2ccccc2[nH]1 10.1021/jm900686q
10918703 3932 None 11 Mouse Functional pIC50 = 9.9 9.9 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)
ChEMBL 555 8 5 6 3.0 Oc1cc(C)c(c(c1)C)C[C@@H](C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](c1[nH]c2c(n1)cccc2)CC(=O)O)N 10.1021/jm020336e
9006 3932 None 11 Mouse Functional pIC50 = 9.9 9.9 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)
ChEMBL 555 8 5 6 3.0 Oc1cc(C)c(c(c1)C)C[C@@H](C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](c1[nH]c2c(n1)cccc2)CC(=O)O)N 10.1021/jm020336e
CHEMBL442577 3932 None 11 Mouse Functional pIC50 = 9.9 9.9 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)
ChEMBL 555 8 5 6 3.0 Oc1cc(C)c(c(c1)C)C[C@@H](C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](c1[nH]c2c(n1)cccc2)CC(=O)O)N 10.1021/jm020336e
16082892 141922 None 0 Human Functional pIC50 = 9.9 9.9 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 522 7 2 3 6.6 Cc1ccccc1/C=C/CN1C[C@H](C)[C@@]2(c3cccc(O)c3)C[C@H](NC(=O)C(C)(C)c3ccccc3)C[C@@H]1C2 10.1021/jm060459p
CHEMBL386434 141922 None 0 Human Functional pIC50 = 9.9 9.9 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 522 7 2 3 6.6 Cc1ccccc1/C=C/CN1C[C@H](C)[C@@]2(c3cccc(O)c3)C[C@H](NC(=O)C(C)(C)c3ccccc3)C[C@@H]1C2 10.1021/jm060459p
44407863 140970 None 0 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 458 8 2 4 5.1 C[C@@H]1CN([C@H](c2ccc(CCC(=O)O)cc2)c2cccc(O)c2)[C@@H](C)CN1Cc1ccccc1 10.1016/j.bmcl.2005.10.102
CHEMBL382024 140970 None 0 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 458 8 2 4 5.1 C[C@@H]1CN([C@H](c2ccc(CCC(=O)O)cc2)c2cccc(O)c2)[C@@H](C)CN1Cc1ccccc1 10.1016/j.bmcl.2005.10.102
73347271 89638 None 0 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor by mouse vas deferens assayAgonist activity at delta opioid receptor by mouse vas deferens assay
ChEMBL 539 9 4 5 3.9 Cc1cc(O)cc(C)c1C[C@@H](C)CN1Cc2ccccc2C[C@H]1C(=O)NCC(=O)NCc1nc2ccccc2[nH]1 10.1021/jm0603264
CHEMBL2375157 89638 None 0 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor by mouse vas deferens assayAgonist activity at delta opioid receptor by mouse vas deferens assay
ChEMBL 539 9 4 5 3.9 Cc1cc(O)cc(C)c1C[C@@H](C)CN1Cc2ccccc2C[C@H]1C(=O)NCC(=O)NCc1nc2ccccc2[nH]1 10.1021/jm0603264
10345770 8480 None 0 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
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.bmc.2010.06.073
CHEMBL109390 8480 None 0 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
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.bmc.2010.06.073
CHEMBL556230 218224 None 0 Mouse Functional pIC50 = 9.9 9.9 - 1
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked contraction
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCC(=O)c1nc2ccccc2[nH]1 10.1021/jm900686q
CHEMBL294616 213353 None 0 Human Functional pIC50 = 9.9 9.9 -2 7
Agonist activity at delta opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at delta opioid expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H]1C(=O)O 10.1016/j.bmc.2010.06.005
CHEMBL26575 213121 None 0 Mouse Functional pIC50 = 9.8 9.8 -5 4
Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractionsAgonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)NCC(=O)O)C(C)C 10.1016/j.bmcl.2018.05.015
CHEMBL317956 213665 None 31 Mouse Functional pIC50 = 9.8 9.8 -1 7
Inhibition of electrically evoked contractions in mouse vas deferensInhibition of electrically evoked contractions in mouse vas deferens
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/jm00099a025
16082879 80021 None 0 Human Functional pIC50 = 9.8 9.8 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 496 8 2 3 6.1 C[C@@H](C(=O)N[C@@H]1C[C@@H]2C[C@](c3cccc(O)c3)(C1)[C@@H](C)CN2CCCc1ccccc1)c1ccccc1 10.1021/jm060459p
CHEMBL212752 80021 None 0 Human Functional pIC50 = 9.8 9.8 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 496 8 2 3 6.1 C[C@@H](C(=O)N[C@@H]1C[C@@H]2C[C@](c3cccc(O)c3)(C1)[C@@H](C)CN2CCCc1ccccc1)c1ccccc1 10.1021/jm060459p
44407861 140434 None 0 Mouse Functional pIC50 = 9.8 9.8 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 444 7 2 4 4.7 C[C@@H]1CN([C@H](c2ccc(CC(=O)O)cc2)c2cccc(O)c2)[C@@H](C)CN1Cc1ccccc1 10.1016/j.bmcl.2005.10.102
CHEMBL380737 140434 None 0 Mouse Functional pIC50 = 9.8 9.8 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 444 7 2 4 4.7 C[C@@H]1CN([C@H](c2ccc(CC(=O)O)cc2)c2cccc(O)c2)[C@@H](C)CN1Cc1ccccc1 10.1016/j.bmcl.2005.10.102
CHEMBL317956 213665 None 31 Mouse Functional pIC50 = 9.8 9.8 -1 7
Inhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferensInhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferens
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/jm00027a018
44348645 16878 None 0 Mouse Functional pIC50 = 9.8 9.8 3 3
Inhibition of electrically evoked contractions in mouse vas deferensInhibition of electrically evoked contractions in mouse vas deferens
ChEMBL 794 19 10 10 -1.3 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)C1(NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCc2ccccc2C1)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1021/jm00099a025
CHEMBL124941 16878 None 0 Mouse Functional pIC50 = 9.8 9.8 3 3
Inhibition of electrically evoked contractions in mouse vas deferensInhibition of electrically evoked contractions in mouse vas deferens
ChEMBL 794 19 10 10 -1.3 CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)C1(NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCc2ccccc2C1)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1021/jm00099a025
CHEMBL317956 213665 None 31 Mouse Functional pIC50 = 9.8 9.8 -1 7
Functional bioactivity against delta opioid receptor in mouse vas deferensFunctional bioactivity against delta opioid receptor in mouse vas deferens
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/jm058259l
6540640 141933 None 2 Human Functional pIC50 = 9.7 9.7 -1 3
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 504 5 2 5 4.0 O=C(/C=C/c1ccc(Cl)cc1)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5 10.1021/jm060595u
CHEMBL386492 141933 None 2 Human Functional pIC50 = 9.7 9.7 -1 3
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 504 5 2 5 4.0 O=C(/C=C/c1ccc(Cl)cc1)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5 10.1021/jm060595u
2494 102435 None 3 Mouse Functional pIC50 = 9.7 9.7 109 2
Tested for agonist activity against delta opioid receptor mouse vas deferensTested for agonist activity against delta opioid receptor mouse vas deferens
ChEMBL 435 8 1 4 4.5 C=CCN1CC(C)N(C(c2ccc(C(=O)N(CC)CC)cc2)c2cccc(O)c2)CC1C 10.1021/jm00040a002
CHEMBL303855 102435 None 3 Mouse Functional pIC50 = 9.7 9.7 109 2
Tested for agonist activity against delta opioid receptor mouse vas deferensTested for agonist activity against delta opioid receptor mouse vas deferens
ChEMBL 435 8 1 4 4.5 C=CCN1CC(C)N(C(c2ccc(C(=O)N(CC)CC)cc2)c2cccc(O)c2)CC1C 10.1021/jm00040a002
50994602 57239 None 0 Mouse Functional pIC50 = 9.7 9.7 -2 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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 57239 None 0 Mouse Functional pIC50 = 9.7 9.7 -2 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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
CHEMBL289006 213328 None 0 Mouse Functional pIC50 = 9.6 9.6 3 3
In vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferensIn vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferens
ChEMBL None None None CC(C)[C@@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CC(=O)O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm00027a017
CHEMBL153466 211257 None 0 Mouse Functional pIC50 = 9.6 9.6 3 3
Inhibitory activity against Mouse vas deferens smooth muscleInhibitory activity against Mouse vas deferens smooth muscle
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CC(=O)O)C(=O)N1)C(=O)NCC(N)=O 10.1016/S0960-894X(01)81195-1
CHEMBL396356 214955 None 0 Mouse Functional pIC50 = 9.6 9.6 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL None None None NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1 10.1016/j.bmcl.2007.01.092
CHEMBL286629 213323 None 0 Mouse Functional pIC50 = 9.6 9.6 8 3
In vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferensIn vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferens
ChEMBL None None None CC(C)[C@@H](NC(=O)[C@@H]1NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC1(C)C)C(=O)NCC(N)=O 10.1021/jm00027a017
10031234 112968 None 0 Mouse Functional pIC50 = 9.6 9.6 - 1
Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deference (MVD, delta receptor)Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deference (MVD, delta receptor)
ChEMBL 585 7 7 8 -0.3 CC1(C)SC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm020108k
CHEMBL331043 112968 None 0 Mouse Functional pIC50 = 9.6 9.6 - 1
Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deference (MVD, delta receptor)Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deference (MVD, delta receptor)
ChEMBL 585 7 7 8 -0.3 CC1(C)SC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm020108k
CHEMBL551937 218210 None 0 Mouse Functional pIC50 = 9.6 9.6 - 1
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked contraction
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](C)C(=O)c1nc2ccccc2[nH]1 10.1021/jm900686q
1607 1306 None 30 Mouse Functional pIC50 = 9.6 9.6 -1 6
Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1021/jm061369n
6917707 1306 None 30 Mouse Functional pIC50 = 9.6 9.6 -1 6
Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1021/jm061369n
CHEMBL340032 1306 None 30 Mouse Functional pIC50 = 9.6 9.6 -1 6
Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1021/jm061369n
DB08856 1306 None 30 Mouse Functional pIC50 = 9.6 9.6 -1 6
Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1021/jm061369n
16116089 84822 None 0 Mouse Functional pIC50 = 9.6 9.6 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 550 7 7 7 -1.1 NC(=O)[C@@H]1C/C=C/C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm061294n
CHEMBL223244 84822 None 0 Mouse Functional pIC50 = 9.6 9.6 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 550 7 7 7 -1.1 NC(=O)[C@@H]1C/C=C/C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm061294n
CHEMBL32202 213692 None 0 Mouse Functional pIC50 = 9.6 9.6 4 3
In vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferensIn vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferens
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00027a017
104787 1473 None 17 Human Functional pIC50 = 9.5 9.5 -2 4
Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assayAgonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2016.09.003
1608 1473 None 17 Human Functional pIC50 = 9.5 9.5 -2 4
Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assayAgonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2016.09.003
CHEMBL31421 1473 None 17 Human Functional pIC50 = 9.5 9.5 -2 4
Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assayAgonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2016.09.003
DB08861 1473 None 17 Human Functional pIC50 = 9.5 9.5 -2 4
Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assayAgonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2016.09.003
CHEMBL26861 213220 None 0 Mouse Functional pIC50 = 9.5 9.5 - 1
In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD)
ChEMBL None None None None 10.1021/jm020336e
CHEMBL2372310 212672 None 0 Mouse Functional pIC50 = 9.5 9.5 3 3
Inhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferensInhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferens
ChEMBL None None None CC1(C)SSC[C@@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)O)NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm00027a018
145961376 161704 None 0 Mouse Functional pIC50 = 9.5 9.5 -20 3
Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractionsAgonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions
ChEMBL 569 15 9 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
CHEMBL4129679 161704 None 0 Mouse Functional pIC50 = 9.5 9.5 -20 3
Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractionsAgonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions
ChEMBL 569 15 9 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
44407732 75410 None 0 Mouse Functional pIC50 = 9.5 9.5 12589 2
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 575 7 2 5 5.9 C[C@H]1CN(Cc2ccccc2)[C@H](C)CN1[C@@H](c1cccc(O)c1)c1ccc2c(c1)CN(C(=O)c1ccccc1C(=O)O)C2 10.1016/j.bmcl.2005.10.102
CHEMBL203903 75410 None 0 Mouse Functional pIC50 = 9.5 9.5 12589 2
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 575 7 2 5 5.9 C[C@H]1CN(Cc2ccccc2)[C@H](C)CN1[C@@H](c1cccc(O)c1)c1ccc2c(c1)CN(C(=O)c1ccccc1C(=O)O)C2 10.1016/j.bmcl.2005.10.102
CHEMBL1213989 211070 None 0 Mouse Functional pIC50 = 9.5 9.5 - 1
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C)C(C)C 10.1016/j.bmc.2010.06.073
CHEMBL2372329 212680 None 0 Mouse Functional pIC50 = 9.5 9.5 37 3
Inhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferensInhibitory concentration against delta opioid receptor of electrically induced smooth muscle contraction of mouse vas deferens
ChEMBL None None None CC1(C)SSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]1NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm00027a018
11071778 164149 None 0 Mouse Functional pIC50 = 9.5 9.5 - 1
Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deferens (MVD, delta receptor)Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deferens (MVD, delta receptor)
ChEMBL 557 7 7 8 -1.1 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1021/jm020108k
CHEMBL420903 164149 None 0 Mouse Functional pIC50 = 9.5 9.5 - 1
Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deferens (MVD, delta receptor)Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deferens (MVD, delta receptor)
ChEMBL 557 7 7 8 -1.1 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1021/jm020108k
155536594 176472 None 0 Human Functional pIC50 = 9.4 9.4 48 3
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hr
ChEMBL 932 12 12 12 -1.3 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1021/acsmedchemlett.8b00495
CHEMBL4473857 176472 None 0 Human Functional pIC50 = 9.4 9.4 48 3
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hr
ChEMBL 932 12 12 12 -1.3 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1021/acsmedchemlett.8b00495
CHEMBL4595743 176472 None 0 Human Functional pIC50 = 9.4 9.4 48 3
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding incubated for 1 hr
ChEMBL 932 12 12 12 -1.3 N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1C/C=C/C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)NNC(=O)[C@H](Cc2ccccc2)NC(=O)CNC1=O 10.1021/acsmedchemlett.8b00495
CHEMBL420606 215712 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Functional biological activity for Opioid receptor delta 1 was determined in vitro, on mouse vas deferens (MVD).Functional biological activity for Opioid receptor delta 1 was determined in vitro, on mouse vas deferens (MVD).
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)NCC(N)=O 10.1021/jm9700530
CHEMBL317956 213665 None 31 Mouse Functional pIC50 = 9.4 9.4 -1 7
In vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferensIn vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferens
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/jm00027a017
50994460 57233 None 0 Mouse Functional pIC50 = 9.4 9.4 -2 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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 57233 None 0 Mouse Functional pIC50 = 9.4 9.4 -2 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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
CHEMBL317956 213665 None 31 Mouse Functional pIC50 = 9.4 9.4 -1 7
Agonist activity at delta opioid receptor assessed as inhibition of electrically-evoked contraction of mouse vas deferensAgonist activity at delta opioid receptor assessed as inhibition of electrically-evoked contraction of mouse vas deferens
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/jm060741w
1641 2728 None 8 Human Functional pIC50 = 9.4 9.4 2 7
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmcl.2009.02.078
3829 2728 None 8 Human Functional pIC50 = 9.4 9.4 2 7
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmcl.2009.02.078
5497186 2728 None 8 Human Functional pIC50 = 9.4 9.4 2 7
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmcl.2009.02.078
CHEMBL567175 2728 None 8 Human Functional pIC50 = 9.4 9.4 2 7
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS bindingAntagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmcl.2009.02.078
156019450 178039 None 0 Human Functional pIC50 = 9.4 9.4 4 2
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 585 8 1 6 6.5 Cc1cc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)ccn1 10.1021/acs.jmedchem.0c00503
CHEMBL4645508 178039 None 0 Human Functional pIC50 = 9.4 9.4 4 2
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 585 8 1 6 6.5 Cc1cc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)ccn1 10.1021/acs.jmedchem.0c00503
16082876 138656 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 564 8 2 3 7.5 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccccc4)CCCCCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
CHEMBL377540 138656 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 564 8 2 3 7.5 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccccc4)CCCCCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
4060 1308 None 0 Mouse Functional pIC50 = 9.4 9.4 4 3
inhibitory concentration for inhibition of electrically induced smooth muscle contractions of MVD (mouse vas deferens) myenteric-plexus-longitudinal muscle strips.inhibitory concentration for inhibition of electrically induced smooth muscle contractions of MVD (mouse vas deferens) myenteric-plexus-longitudinal muscle strips.
ChEMBL None None None None 10.1021/jm9911534
CHEMBL296603 1308 None 0 Mouse Functional pIC50 = 9.4 9.4 4 3
inhibitory concentration for inhibition of electrically induced smooth muscle contractions of MVD (mouse vas deferens) myenteric-plexus-longitudinal muscle strips.inhibitory concentration for inhibition of electrically induced smooth muscle contractions of MVD (mouse vas deferens) myenteric-plexus-longitudinal muscle strips.
ChEMBL None None None None 10.1021/jm9911534
71455949 83885 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 745 18 5 6 4.4 CCCCCCNC(=O)c1ccc(C[C@H](N)C(=O)N2Cc3ccccc3CC2C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)O)cc1 10.1016/j.bmcl.2012.01.063
CHEMBL2206325 83885 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 745 18 5 6 4.4 CCCCCCNC(=O)c1ccc(C[C@H](N)C(=O)N2Cc3ccccc3CC2C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)O)cc1 10.1016/j.bmcl.2012.01.063
CHEMBL1213990 211071 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
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](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1c(F)cc(O)cc1F)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1016/j.bmc.2010.06.073
16082877 142042 None 1 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 510 8 2 3 6.2 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C(C)(C)c3ccccc3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
CHEMBL387245 142042 None 1 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 510 8 2 3 6.2 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C(C)(C)c3ccccc3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
145961883 161459 None 0 Mouse Functional pIC50 = 9.4 9.4 -223 4
Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractionsAgonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions
ChEMBL 594 16 9 7 -0.4 C=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4126102 161459 None 0 Mouse Functional pIC50 = 9.4 9.4 -223 4
Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractionsAgonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions
ChEMBL 594 16 9 7 -0.4 C=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
52937468 62542 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
ChEMBL 580 12 8 7 -0.8 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/jm1016285
CHEMBL1782140 62542 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
ChEMBL 580 12 8 7 -0.8 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/jm1016285
52937468 62542 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Agonist activity at delta-type opioid receptor in mouse vas deferens assessed as inhibition of electrically stimulated contractionsAgonist activity at delta-type opioid receptor in mouse vas deferens assessed as inhibition of electrically stimulated contractions
ChEMBL 580 12 8 7 -0.8 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/acsmedchemlett.7b00347
CHEMBL1782140 62542 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Agonist activity at delta-type opioid receptor in mouse vas deferens assessed as inhibition of electrically stimulated contractionsAgonist activity at delta-type opioid receptor in mouse vas deferens assessed as inhibition of electrically stimulated contractions
ChEMBL 580 12 8 7 -0.8 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/acsmedchemlett.7b00347
16082874 81166 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 522 8 2 3 6.4 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccccc4)CCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
CHEMBL215693 81166 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 522 8 2 3 6.4 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccccc4)CCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
44308087 103096 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Concentration required for 50% inhibition of electrically induced contraction of the mouse vas deferens mediated through delta opioid receptorConcentration required for 50% inhibition of electrically induced contraction of the mouse vas deferens mediated through delta opioid receptor
ChEMBL 537 10 5 7 1.0 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)N(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1=O 10.1016/s0960-894x(01)00706-5
CHEMBL307133 103096 None 0 Mouse Functional pIC50 = 9.4 9.4 - 1
Concentration required for 50% inhibition of electrically induced contraction of the mouse vas deferens mediated through delta opioid receptorConcentration required for 50% inhibition of electrically induced contraction of the mouse vas deferens mediated through delta opioid receptor
ChEMBL 537 10 5 7 1.0 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)N(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1=O 10.1016/s0960-894x(01)00706-5
16082884 80189 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 542 8 2 4 6.8 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccsc4)CCCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
CHEMBL213421 80189 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 542 8 2 4 6.8 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccsc4)CCCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
16082881 139514 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 554 8 2 3 6.9 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccc(F)cc4)CCCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
CHEMBL379389 139514 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 554 8 2 3 6.9 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccc(F)cc4)CCCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
16735664 79148 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 639 6 4 7 5.6 O=Cc1cc2ccc(C(=O)Nc3cccc4c5c([nH]c34)[C@@H]3Oc4c(O)ccc6c4[C@@]34CCN(CC3CC3)[C@H](C6)[C@]4(O)C5)cc2cc1C=O 10.1021/jm061194h
CHEMBL2113281 79148 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 639 6 4 7 5.6 O=Cc1cc2ccc(C(=O)Nc3cccc4c5c([nH]c34)[C@@H]3Oc4c(O)ccc6c4[C@@]34CCN(CC3CC3)[C@H](C6)[C@]4(O)C5)cc2cc1C=O 10.1021/jm061194h
CHEMBL317956 213665 None 31 Mouse Functional pIC50 = 9.3 9.3 -1 7
Functional biological activity for Opioid receptor delta 1 was determined in vitro, on mouse vas deferens (MVD).Functional biological activity for Opioid receptor delta 1 was determined in vitro, on 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/jm9700530
CHEMBL132164 211158 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Inhibition of electrically evoked contractions in mouse vas deferensInhibition of electrically evoked contractions in mouse vas deferens
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CCC(=O)NCCCC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C 10.1021/jm00099a025
16082880 138342 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 566 9 2 4 6.8 COc1ccc(C2(C(=O)N[C@@H]3C[C@@H]4C[C@](c5cccc(O)c5)(C3)[C@@H](C)CN4CCCc3ccccc3)CCCC2)cc1 10.1021/jm060459p
CHEMBL377044 138342 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 566 9 2 4 6.8 COc1ccc(C2(C(=O)N[C@@H]3C[C@@H]4C[C@](c5cccc(O)c5)(C3)[C@@H](C)CN4CCCc3ccccc3)CCCC2)cc1 10.1021/jm060459p
16116088 83538 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 550 7 7 7 -1.1 NC(=O)[C@@H]1C/C=C\C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm061294n
CHEMBL220333 83538 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 550 7 7 7 -1.1 NC(=O)[C@@H]1C/C=C\C[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm061294n
16082913 161999 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 548 7 2 3 7.2 Cc1ccccc1/C=C/CN1C[C@H](C)[C@@]2(c3cccc(O)c3)C[C@H](NC(=O)C3(c4ccccc4)CCCC3)C[C@@H]1C2 10.1021/jm060459p
CHEMBL415223 161999 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 548 7 2 3 7.2 Cc1ccccc1/C=C/CN1C[C@H](C)[C@@]2(c3cccc(O)c3)C[C@H](NC(=O)C3(c4ccccc4)CCCC3)C[C@@H]1C2 10.1021/jm060459p
44407550 73529 None 0 Mouse Functional pIC50 = 9.3 9.3 2511 2
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 485 7 2 5 4.5 C[C@H]1CN(Cc2ccccc2)[C@H](C)CN1[C@@H](c1cccc(O)c1)c1ccc2c(c1)CN(CC(=O)O)C2 10.1016/j.bmcl.2005.10.102
CHEMBL201678 73529 None 0 Mouse Functional pIC50 = 9.3 9.3 2511 2
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 485 7 2 5 4.5 C[C@H]1CN(Cc2ccccc2)[C@H](C)CN1[C@@H](c1cccc(O)c1)c1ccc2c(c1)CN(CC(=O)O)C2 10.1016/j.bmcl.2005.10.102
CHEMBL374818 214667 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None CCc1cccc(C)c1C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061238m
156021519 178244 None 0 Human Functional pIC50 = 9.3 9.3 1023 2
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 571 8 1 6 6.2 Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccn5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/acs.jmedchem.0c00503
CHEMBL4648628 178244 None 0 Human Functional pIC50 = 9.3 9.3 1023 2
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 571 8 1 6 6.2 Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccn5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/acs.jmedchem.0c00503
4060 1308 None 0 Mouse Functional pIC50 = 9.3 9.3 4 3
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
ChEMBL None None None None 10.1016/j.bmc.2010.06.073
CHEMBL296603 1308 None 0 Mouse Functional pIC50 = 9.3 9.3 4 3
Agonist activity at delta opioid receptor in mouse vas deferenceAgonist activity at delta opioid receptor in mouse vas deference
ChEMBL None None None None 10.1016/j.bmc.2010.06.073
71455950 83889 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 815 16 5 6 5.2 N[C@@H](Cc1ccc(C(=O)NCCc2cccc3ccccc23)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
CHEMBL2206329 83889 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL 815 16 5 6 5.2 N[C@@H](Cc1ccc(C(=O)NCCc2cccc3ccccc23)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2012.01.063
CHEMBL317956 213665 None 31 Rat Functional pIC50 = 9.3 9.3 -1 7
Agonist activity for Opioid receptor delta 1Agonist activity for Opioid receptor delta 1
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/jm9607663
44308607 205928 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Concentration required for 50% inhibition of electrically induced contraction of the mouse vas deferens mediated through delta opioid receptorConcentration required for 50% inhibition of electrically induced contraction of the mouse vas deferens mediated through delta opioid receptor
ChEMBL 509 9 5 7 0.4 C[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)N(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1=O 10.1016/s0960-894x(01)00706-5
CHEMBL66009 205928 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Concentration required for 50% inhibition of electrically induced contraction of the mouse vas deferens mediated through delta opioid receptorConcentration required for 50% inhibition of electrically induced contraction of the mouse vas deferens mediated through delta opioid receptor
ChEMBL 509 9 5 7 0.4 C[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)N(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1=O 10.1016/s0960-894x(01)00706-5
CHEMBL2370485 212318 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
In vitro delta opioid activity was determined by its ability to inhibit the electrically induced contractions of smooth muscle preparations in mouse vas deferens (MVD)In vitro delta opioid activity was determined by its ability to inhibit the electrically induced contractions of smooth muscle preparations in mouse vas deferens (MVD)
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC1=O 10.1016/s0960-894x(99)00625-3
CHEMBL220327 211878 None 0 Mouse Functional pIC50 = 9.3 9.3 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL None None None NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm061294n
CHEMBL317956 213665 None 31 Mouse Functional pIC50 = 9.2 9.2 -1 7
In vitro biological activity by electrically induced smooth muscle contractions in mouse vas deferens (Opioid receptor delta 1); inhibitory concentration was evaluatedIn vitro biological activity by electrically induced smooth muscle contractions in mouse vas deferens (Opioid receptor delta 1); inhibitory concentration was evaluated
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 10.1016/s0960-894x(02)00035-5
16733485 137300 None 0 Mouse Functional pIC50 = 9.2 9.2 1 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-evoked muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-evoked muscle contraction
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 137300 None 0 Mouse Functional pIC50 = 9.2 9.2 1 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-evoked muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-evoked muscle contraction
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
CHEMBL331325 213821 None 2 Mouse Functional pIC50 = 9.2 9.2 -1 2
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm061238m
16720646 137674 None 0 Human Functional pIC50 = 9.2 9.2 158 3
Antagonist activity at human delta opioid receptor expressed in CHO membrane assessed as inhibition of SNC80-induced [35S]GTPgammaS bindingAntagonist activity at human delta opioid receptor expressed in CHO membrane assessed as inhibition of SNC80-induced [35S]GTPgammaS 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 137674 None 0 Human Functional pIC50 = 9.2 9.2 158 3
Antagonist activity at human delta opioid receptor expressed in CHO membrane assessed as inhibition of SNC80-induced [35S]GTPgammaS bindingAntagonist activity at human delta opioid receptor expressed in CHO membrane assessed as inhibition of SNC80-induced [35S]GTPgammaS 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
CHEMBL373572 214640 None 0 Mouse Functional pIC50 = 9.2 9.2 - 1
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
ChEMBL None None None NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm061294n
156011033 177252 None 0 Human Functional pIC50 = 9.2 9.2 5 2
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 560 8 2 6 5.5 Oc1ccc2c3c1O[C@H]1c4ncc(-c5cn[nH]c5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/acs.jmedchem.0c00503
CHEMBL4634007 177252 None 0 Human Functional pIC50 = 9.2 9.2 5 2
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 560 8 2 6 5.5 Oc1ccc2c3c1O[C@H]1c4ncc(-c5cn[nH]c5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/acs.jmedchem.0c00503
145961895 161477 None 0 Mouse Functional pIC50 = 9.2 9.2 -194 4
Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractionsAgonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions
ChEMBL 622 16 9 7 0.4 CC(C)=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4126322 161477 None 0 Mouse Functional pIC50 = 9.2 9.2 -194 4
Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractionsAgonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions
ChEMBL 622 16 9 7 0.4 CC(C)=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
119029 753 None 27 Mouse Functional pIC50 = 9.2 9.2 -1 6
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
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 10.1016/j.bmcl.2005.10.102
9002 753 None 27 Mouse Functional pIC50 = 9.2 9.2 -1 6
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
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 10.1016/j.bmcl.2005.10.102
CHEMBL25230 753 None 27 Mouse Functional pIC50 = 9.2 9.2 -1 6
Agonist activity at delta opioid receptor in mouse vas deferensAgonist activity at delta opioid receptor in mouse vas deferens
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 10.1016/j.bmcl.2005.10.102
16087285 82270 None 0 Human Functional pIC50 = 9.2 9.2 -2 3
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 506 8 2 5 4.8 O=C1CC[C@@]2(NCCCCc3ccc(Cl)cc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm060595u
CHEMBL217102 82270 None 0 Human Functional pIC50 = 9.2 9.2 -2 3
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 506 8 2 5 4.8 O=C1CC[C@@]2(NCCCCc3ccc(Cl)cc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm060595u
156015005 177644 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 571 8 1 6 6.2 Oc1ccc2c3c1O[C@H]1c4ncc(-c5cccnc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/acs.jmedchem.0c00503
CHEMBL4640141 177644 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 571 8 1 6 6.2 Oc1ccc2c3c1O[C@H]1c4ncc(-c5cccnc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/acs.jmedchem.0c00503
CHEMBL317956 213665 None 31 Mouse Functional pIC50 = 9.2 9.2 -1 7
In vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferensIn vitro inhibition of electrically induced smooth muscle contractions of mouse vas deferens
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/jm00027a017
156017544 177891 None 0 Human Functional pIC50 = 9.2 9.2 5 2
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 575 8 1 7 6.1 Cc1nocc1-c1cnc2c(c1)C[C@@]1(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]1(CCN3CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.0c00503
CHEMBL4643256 177891 None 0 Human Functional pIC50 = 9.2 9.2 5 2
Antagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hrAntagonist activity at human delta opioid receptor expressed in CHO cell membranes assessed as reduction in SNC80-induced [35S]GTPgammaS binding preincubated for 5 mins followed by SNC80 addition and measured after 1 hr
ChEMBL 575 8 1 7 6.1 Cc1nocc1-c1cnc2c(c1)C[C@@]1(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]1(CCN3CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.0c00503
16082875 141573 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 550 8 2 3 7.2 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccccc4)CCCCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
CHEMBL384406 141573 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDPInverse agonist activity at human cloned delta opioid receptor expressed in CHO cells assessed as inhibition of DPDPE-stimulated [35S]GTP-gamma-S binding in presence of 1 uM GDP
ChEMBL 550 8 2 3 7.2 C[C@H]1CN(CCCc2ccccc2)[C@@H]2C[C@@H](NC(=O)C3(c4ccccc4)CCCCC3)C[C@@]1(c1cccc(O)c1)C2 10.1021/jm060459p
145963053 161628 None 0 Mouse Functional pIC50 = 9.2 9.2 -17 3
Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractionsAgonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions
ChEMBL 523 12 5 6 0.7 C=Cc1ccccc1C[C@@H](C(=O)NCC(N)=O)N(C)C(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1016/j.bmcl.2018.05.015
CHEMBL4128530 161628 None 0 Mouse Functional pIC50 = 9.2 9.2 -17 3
Agonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractionsAgonist activity at delta-opioid receptor in mouse vasa deferens assessed as inhibition of electrically induced contractions
ChEMBL 523 12 5 6 0.7 C=Cc1ccccc1C[C@@H](C(=O)NCC(N)=O)N(C)C(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C 10.1016/j.bmcl.2018.05.015
50994380 57229 None 0 Mouse Functional pIC50 = 9.2 9.2 -3 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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 57229 None 0 Mouse Functional pIC50 = 9.2 9.2 -3 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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
CHEMBL20775 211647 None 30 Mouse Functional pIC50 = 9.2 9.2 - 1
Inhibition of electrically evoked contractions in mouse vas deferensInhibition of electrically evoked contractions in mouse vas deferens
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCSC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00099a025
50925450 57234 None 0 Mouse Functional pIC50 = 9.2 9.2 -3 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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 57234 None 0 Mouse Functional pIC50 = 9.2 9.2 -3 3
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
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
156011239 177405 None 0 Human Functional pIC50 = 9.2 9.2 3 2