Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL100940 oprd_human Human Yes - None Funct
UnclassifiedUnclassified
415 2 2 5 3.8 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1oc1c2cccc1)CC1CC1
CHEMBL2151735 oprd_human Human No 10.8 EC50 = 0.0 nM Funct
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
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
CHEMBL611926 oprd_human Human No 10.8 EC50 = 0.0 nM Funct
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
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
CHEMBL559518 oprd_human Human No 10.7 EC50 = 0.0 nM Funct
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
396 2 1 3 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1cc2ccccc2nc1C3
CHEMBL559518 oprd_human Human No 10.7 EC50 = 0.0 nM Funct
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
396 2 1 3 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1cc2ccccc2nc1C3
CHEMBL3758292 oprd_mouse Mouse No 10.7 EC50 = 0.0 nM Bind
Agonist activity at delta-opioid receptor in mouse vas deferensAgonist activity at delta-opioid receptor in mouse vas deferens
497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)NCc1nc2ccccc2[nH]1
CHEMBL340032 oprd_human Human Yes 10.7 EC50 = 0.0 nM Funct
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
None None None None
CHEMBL611926 oprd_human Human No 10.7 EC50 = 0.0 nM Funct
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
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
CHEMBL552308 oprd_human Human No 10.3 EC50 = 0.0 nM Funct
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
356 0 1 3 3.9 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13
CHEMBL552308 oprd_human Human No 10.3 EC50 = 0.0 nM Funct
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
356 0 1 3 3.9 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13
CHEMBL564538 oprd_human Human No 10.2 EC50 = 0.1 nM Funct
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
398 2 1 3 4.9 CC(C)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13
CHEMBL564538 oprd_human Human No 10.2 EC50 = 0.1 nM Funct
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
398 2 1 3 4.9 CC(C)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1ccc(O)cc13
CHEMBL1649941 oprd_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL1649941 oprd_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL1649942 oprd_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL1649942 oprd_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL15038 oprd_human Human Yes 10.1 EC50 = 0.1 nM Bind
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cellsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cells
None None None None
CHEMBL8234 oprd_human Human Yes 10.1 EC50 = 0.1 nM Bind
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cellsAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cells
None None None None
CHEMBL15038 oprd_human Human Yes 10.1 EC50 = 0.1 nM Funct
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
None None None None
CHEMBL8234 oprd_human Human Yes 10.1 EC50 = 0.1 nM Funct
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
None None None None
CHEMBL3758292 oprd_human Human No 10.1 EC50 = 0.1 nM Funct
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
497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)NCc1nc2ccccc2[nH]1
CHEMBL1649947 oprd_human Human No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL1649947 oprd_human Human No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL1649938 oprd_human Human No 10.0 EC50 = 0.1 nM Funct
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
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
CHEMBL1766204 oprd_human Human No 10.0 EC50 = 0.1 nM Funct
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
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
CHEMBL26575 oprd_rat Rat No 10.0 EC50 = 0.1 nM Funct
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
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
CHEMBL2113666 oprd_human Human No 10.0 EC50 = 0.1 nM Funct
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
448 3 1 4 3.5 CN1CC[C@]23c4c5cccc4O[C@H]2C(=O)CC[C@@]3(NC(=O)/C=C/c2ccccc2Cl)[C@H]1C5
CHEMBL567175 oprd_human Human Yes 10.0 EC50 = 0.1 nM Funct
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1
CHEMBL31421 oprd_human Human Yes 9.9 EC50 = 0.1 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
None None None None
CHEMBL1649946 oprd_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL25230 oprd_human Human Yes 9.9 EC50 = 0.1 nM Bind
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
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
CHEMBL1649946 oprd_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL1766204 oprd_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL109390 oprd_mouse Mouse No 9.9 EC50 = 0.1 nM Funct
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)
497 6 4 5 3.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C(=O)NCc1nc2ccccc2[nH]1
CHEMBL1198015 oprd_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL593214 oprd_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL294616 oprd_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL2208349 oprd_human Human No 9.8 EC50 = 0.2 nM Funct
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
494 7 2 3 6.0 CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccccc5O)cc4)cc3C1(C)CCN2CC1CC1
CHEMBL1649943 oprd_human Human No 9.8 EC50 = 0.2 nM Funct
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
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
CHEMBL226166 oprd_human Human No 9.8 EC50 = 0.2 nM Funct
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
384 2 2 2 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3
CHEMBL1649943 oprd_human Human No 9.8 EC50 = 0.2 nM Funct
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
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
CHEMBL1834247 oprd_human Human No 9.8 EC50 = 0.2 nM Funct
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
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
CHEMBL226217 oprd_human Human No 9.8 EC50 = 0.2 nM Funct
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
367 2 2 5 3.1 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2
CHEMBL3086304 oprd_human Human No 9.8 EC50 = 0.2 nM Funct
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
367 2 2 5 3.1 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2
CHEMBL1929365 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
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
396 2 1 3 4.6 Oc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1cc2ccccc2nc1C3
CHEMBL1198702 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
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
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
CHEMBL611930 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
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
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
CHEMBL1649948 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
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
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
CHEMBL1766206 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
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
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
CHEMBL67192 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
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
508 7 0 4 6.5 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2ccccc2)cc1
CHEMBL1649948 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
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
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
CHEMBL568818 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
461 9 1 5 5.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccoc3)CC2)cc1
CHEMBL584941 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
477 9 1 5 5.8 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccsc3)CC2)cc1
CHEMBL2387214 oprd_human Human No 9.7 EC50 = 0.2 nM Funct
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
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
CHEMBL4103044 oprd_human Human No 9.6 EC50 = 0.2 nM Funct
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
444 3 1 4 4.2 O=C(c1ccoc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21
CHEMBL569316 oprd_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
472 9 1 5 5.1 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccn3)CC2)cc1
CHEMBL2419538 oprd_human Human No 9.6 EC50 = 0.3 nM Funct
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
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
CHEMBL2179656 oprd_human Human No 9.6 EC50 = 0.3 nM Funct
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
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
CHEMBL577615 oprd_human Human No 9.5 EC50 = 0.3 nM Bind
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
484 9 1 4 5.1 CCN(CC)C(=O)c1ccc(N(c2cccc(C(N)=O)c2)C2CCN(Cc3ccccc3)CC2)cc1
CHEMBL281986 oprd_human Human No 9.5 EC50 = 0.3 nM Funct
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
435 3 2 5 3.3 CO[C@]12C=CC3(CC14CCC[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1CC1CC1)[C@@H]2O5
CHEMBL1198704 oprd_human Human No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL611932 oprd_human Human No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL2208347 oprd_human Human No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL4083940 oprd_human Human No 9.5 EC50 = 0.3 nM Funct
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
454 3 1 3 4.6 O=C(c1ccccc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21
CHEMBL421520 oprd_human Human No 9.5 EC50 = 0.3 nM Bind
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
468 5 4 4 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C/N=C(/S)NC(C)(C)C
CHEMBL2113383 oprd_human Human No 9.5 EC50 = 0.3 nM Funct
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.
401 2 3 4 3.4 CCN[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5
CHEMBL296603 oprd_mouse Mouse No 9.5 EC50 = 0.3 nM Funct
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
None None None None
CHEMBL2387215 oprd_human Human No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL4797394 oprd_human Human No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL4068691 oprd_human Human No 9.5 EC50 = 0.4 nM Funct
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
455 3 1 4 4.0 O=C(c1ccccn1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21
CHEMBL49581 oprd_mouse Mouse No 9.4 EC50 = 0.4 nM Bind
Effective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitroEffective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitro
None None None CC(C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)N)C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C
CHEMBL3608938 oprd_human Human No 9.4 EC50 = 0.4 nM Funct
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
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
CHEMBL4754944 oprd_human Human No 9.4 EC50 = 0.4 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
464 6 3 6 2.5 CO[C@@]12CC[C@H](N[C@@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL3264747 oprd_human Human No 9.4 EC50 = 0.4 nM Bind
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
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
CHEMBL25230 oprd_human Human Yes 9.4 EC50 = 0.4 nM Funct
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
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
CHEMBL607125 oprd_human Human No 9.4 EC50 = 0.4 nM Funct
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
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
CHEMBL3264748 oprd_human Human No 9.4 EC50 = 0.4 nM Funct
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
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
CHEMBL4061334 oprd_human Human No 9.4 EC50 = 0.4 nM Funct
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
440 4 1 3 5.0 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1Cc1ccccc1)C2
CHEMBL4075409 oprd_human Human No 9.4 EC50 = 0.4 nM Funct
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
442 3 1 4 3.5 C=CCN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1
CHEMBL4076303 oprd_human Human No 9.4 EC50 = 0.4 nM Funct
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
416 1 1 4 3.0 CN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1
CHEMBL4094845 oprd_human Human No 9.4 EC50 = 0.4 nM Funct
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
428 3 1 5 3.8 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1c1cnccn1)C2
CHEMBL1766206 oprd_human Human No 9.4 EC50 = 0.4 nM Funct
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
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
CHEMBL226114 oprd_human Human No 9.3 EC50 = 0.5 nM Funct
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
344 0 2 2 3.8 CN1CC[C@]23Cc4[nH]c5ccccc5c4C[C@H]2[C@H]1Cc1ccc(O)cc13
CHEMBL4795312 oprd_human Human No 9.3 EC50 = 0.5 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
464 6 3 6 2.5 CO[C@@]12CC[C@@H](N[C@@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL2408013 oprd_human Human No 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL63732 oprd_human Human No 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL408889 oprd_human Human No 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL1270282 oprd_human Human No 9.3 EC50 = 0.5 nM Funct
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
372 0 2 4 3.0 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL4296720 oprd_human Human No 9.3 EC50 = 0.5 nM Funct
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
372 0 2 4 3.0 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL408889 oprd_human Human No 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL4066752 oprd_human Human No 9.3 EC50 = 0.5 nM Funct
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
456 3 1 4 3.7 O=C(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21
CHEMBL294616 oprd_human Human No 9.3 EC50 = 0.6 nM Funct
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
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
CHEMBL567604 oprd_human Human No 9.3 EC50 = 0.6 nM Bind
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
457 8 1 4 5.7 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(Cc3ccccc3)CC2)cc1
CHEMBL569755 oprd_human Human No 9.3 EC50 = 0.6 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
471 9 1 4 5.7 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccc3)CC2)cc1
CHEMBL1766207 oprd_human Human No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL2179655 oprd_human Human No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL1766207 oprd_human Human No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL4096314 oprd_human Human No 9.2 EC50 = 0.6 nM Funct
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
506 4 1 4 4.6 O=C(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CCc2ccccc2)C4Cc2ccc(O)cc21
CHEMBL3264748 oprd_human Human No 9.2 EC50 = 0.6 nM Bind
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
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
CHEMBL3262092 oprd_human Human No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL310842 oprd_human Human No 9.2 EC50 = 0.7 nM Bind
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
452 5 4 4 2.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNC(=O)NC(C)(C)C
CHEMBL49507 oprd_mouse Mouse No 9.2 EC50 = 0.7 nM Bind
Effective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitroEffective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitro
None None None Cc1cc(O)cc(C)c1[C@H](C)[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(N)=O)C(C)C)C(C)C
CHEMBL4100943 oprd_human Human No 9.2 EC50 = 0.7 nM Funct
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
442 4 1 4 4.1 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1Cc1ccccc1)O2
CHEMBL249985 oprd_human Human No 9.2 EC50 = 0.7 nM Funct
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
508 8 1 3 6.3 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)[C@@]3(C)CCN(CC5CC5)C(C4)[C@@H]3C)cc2)cc1
CHEMBL1739441 oprd_human Human No 9.2 EC50 = 0.7 nM Funct
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
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
CHEMBL3216476 oprd_human Human No 9.2 EC50 = 0.7 nM Funct
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
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
CHEMBL327745 oprd_human Human Yes 9.2 EC50 = 0.7 nM Funct
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
344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O
CHEMBL327745 oprd_human Human Yes 9.2 EC50 = 0.7 nM Funct
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
344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O
CHEMBL4476818 oprd_rat Rat No 9.2 EC50 = 0.7 nM Funct
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
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
CHEMBL4597054 oprd_rat Rat No 9.2 EC50 = 0.7 nM Funct
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
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
CHEMBL80463 oprd_human Human No 9.1 EC50 = 0.8 nM Bind
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
472 6 4 4 3.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNC(=O)Nc1ccccc1
CHEMBL392185 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL235109 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL392185 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL235109 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL3139076 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
444 5 2 5 3.8 CCOCCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL4296728 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
444 5 2 5 3.8 CCOCCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL4790994 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL294616 oprd_human Human No 9.1 EC50 = 0.8 nM Bind
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology measured over 30 mins by label free binding assayAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology measured over 30 mins by label free binding assay
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
CHEMBL2208351 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
522 7 1 4 6.0 CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc6c(c5)OCO6)cc4)cc3C1(C)CCN2CC1CC1
CHEMBL375504 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
398 2 2 2 5.0 Oc1ccc2c(c1)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3
CHEMBL3787263 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
412 2 2 4 3.7 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL4115222 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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.
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
CHEMBL375025 oprd_human Human No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL4458337 oprd_mouse Mouse No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL3759489 oprd_human Human No 9.1 EC50 = 0.9 nM Funct
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
490 4 2 3 6.2 CN1CC[C@]23c4c5ccc(O)c4O[C@@]2(C)c2[nH]c4ccccc4c2C[C@@]3(CCCc2ccccc2)[C@H]1C5
CHEMBL2113378 oprd_human Human No 9.1 EC50 = 0.9 nM Funct
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.
491 5 3 4 5.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NCCCc2ccccc2)C1C5
CHEMBL229440 oprd_human Human No 9.1 EC50 = 0.9 nM Funct
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
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
CHEMBL382051 oprd_human Human No 9.1 EC50 = 0.9 nM Funct
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
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
CHEMBL382051 oprd_human Human No 9.1 EC50 = 0.9 nM Funct
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
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
CHEMBL208454 oprd_mouse Mouse No 9.1 EC50 = 0.9 nM Funct
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
466 5 3 4 4.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1
CHEMBL208454 oprd_human Human No 9.1 EC50 = 0.9 nM Funct
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
466 5 3 4 4.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1
CHEMBL129034 oprd_human Human No 9.1 EC50 = 0.9 nM Funct
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.
398 5 1 2 5.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc3ccccc23)cc1
CHEMBL77001 oprd_human Human No 9.0 EC50 = 0.9 nM Bind
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
443 7 3 4 3.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNCc1ccccc1
CHEMBL2113382 oprd_human Human No 9.0 EC50 = 1.0 nM Funct
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.
477 4 3 4 4.6 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NCCc2ccccc2)C1C5
CHEMBL76089 oprd_human Human No 9.0 EC50 = 1.0 nM Bind
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
444 7 2 4 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1COCc1ccccc1
CHEMBL1766208 oprd_human Human No 9.0 EC50 = 1.0 nM Funct
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
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
CHEMBL3264747 oprd_human Human No 9.0 EC50 = 1.0 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1 nM Funct
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
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
CHEMBL1766208 oprd_human Human No 9.0 EC50 = 1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1 nM Bind
Binding affinity to DOR (unknown origin)Binding affinity to DOR (unknown origin)
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
CHEMBL13786 oprd_human Human Yes 9.0 EC50 = 1.0 nM Funct
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
None None None None
CHEMBL13786 oprd_human Human Yes 9.0 EC50 = 1.0 nM Funct
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
None None None None
CHEMBL1270475 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
412 2 2 4 3.7 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL4296721 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
412 2 2 4 3.7 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL3787016 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
414 2 3 3 4.1 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)CCc1c([nH]c2ccccc12)C3
CHEMBL1739442 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL3216936 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL574640 oprd_human Human No 9.0 EC50 = 1.1 nM Bind
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
514 9 1 5 6.2 CCN(CC)C(=O)c1ccc(N(c2cccc(NC(=O)OC)c2)C2CCN(Cc3ccccc3)CC2)cc1
CHEMBL3139097 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
386 1 2 4 3.4 CCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL4296733 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
386 1 2 4 3.4 CCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL2419542 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL3264742 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL2387328 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL2113671 oprd_human Human No 9.0 EC50 = 1.1 nM Bind
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
459 5 1 5 4.2 CO[C@]12C=C[C@@]3(C[C@H]1[C@@H](C)OCc1ccccc1)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5
CHEMBL31030 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
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
463 3 2 5 3.9 CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1CC1CC1)[C@@H]2O5
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL4741203 oprd_human Human No 9.0 EC50 = 1.1 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
416 5 3 6 1.9 CO[C@@]12CC[C@H](N[C@@H](C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL576267 oprd_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
489 9 1 4 5.9 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccccc3F)CC2)cc1
CHEMBL4129679 oprd_rat Rat No 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL569728 oprd_human Human No 8.9 EC50 = 1.1 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
485 9 1 4 6.0 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccc(C)cc3)CC2)cc1
CHEMBL4789014 oprd_human Human No 8.9 EC50 = 1.2 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
579 9 5 8 2.3 CO[C@@]12CC[C@H](N[C@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL569956 oprd_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
461 9 2 5 4.4 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ncc[nH]3)CC2)cc1
CHEMBL2208358 oprd_human Human No 8.9 EC50 = 1.2 nM Funct
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
508 8 1 3 6.3 COc1cccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)c1
CHEMBL4081856 oprd_human Human No 8.9 EC50 = 1.2 nM Funct
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
492 4 1 5 3.3 O=S(=O)(c1ccccc1)N1C[C@H]2OC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21
CHEMBL2113379 oprd_human Human No 8.9 EC50 = 1.2 nM Funct
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.
491 3 3 4 4.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NC(=O)Cc2ccccc2)C1C5
CHEMBL3139191 oprd_human Human No 8.9 EC50 = 1.2 nM Funct
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
400 2 2 4 3.7 CCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL4296730 oprd_human Human No 8.9 EC50 = 1.2 nM Funct
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
400 2 2 4 3.7 CCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL3408737 oprd_human Human No 8.9 EC50 = 1.3 nM Funct
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
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
CHEMBL570000 oprd_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
461 9 1 5 5.3 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3ccco3)CC2)cc1
CHEMBL4795517 oprd_human Human No 8.9 EC50 = 1.3 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
416 5 3 6 1.9 CO[C@@]12CC[C@@H](N[C@@H](C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL4076681 oprd_human Human No 8.9 EC50 = 1.3 nM Funct
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
470 3 1 4 5.0 O=C(Oc1ccccc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21
CHEMBL412331 oprd_human Human No 8.9 EC50 = 1.3 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.9 EC50 = 1.3 nM Funct
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.
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
CHEMBL412331 oprd_human Human No 8.9 EC50 = 1.3 nM Funct
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
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
CHEMBL3139163 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
442 2 2 5 3.5 Oc1ccc2c(c1)[C@]13CCN(C[C@@H]4CCCO4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL4296737 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
442 2 2 5 3.5 Oc1ccc2c(c1)[C@]13CCN(C[C@@H]4CCCO4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL272215 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL593215 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL3785854 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
400 2 3 3 3.7 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@@H](C2)[C@]1(O)Cc1c([nH]c2ccccc12)C3
CHEMBL4076673 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
474 5 1 5 3.4 COCCCN1CCC23c4cc(O)ccc4CC1C21CCC2C3[C@@H](CN2C(=O)c2ccccc2)O1
CHEMBL494479 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
392 4 2 4 3.8 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccc(O)cc32)cc1
CHEMBL327745 oprd_human Human Yes 8.9 EC50 = 1.4 nM Funct
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
344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O
CHEMBL4458337 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL4458337 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL361033 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
452 5 3 4 4.3 Cc1[nH]c([C@@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1-c1ccccc1
CHEMBL2113373 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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.
505 4 3 4 4.5 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccccc4c2C[C@@]3(NC(=O)CCc2ccccc2)C1C5
CHEMBL3139248 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
404 2 2 4 3.3 Oc1ccc2c(c1)[C@]13CCN(CCF)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL4296731 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
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
404 2 2 4 3.3 Oc1ccc2c(c1)[C@]13CCN(CCF)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL568803 oprd_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
477 9 1 5 5.8 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3cccs3)CC2)cc1
CHEMBL31421 oprd_rat Rat Yes 8.9 EC50 = 1.4 nM Funct
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
None None None None
CHEMBL4130303 oprd_human Human No 8.8 EC50 = 1.4 nM Funct
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
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
CHEMBL4130303 oprd_human Human No 8.8 EC50 = 1.5 nM Funct
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
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
CHEMBL226113 oprd_human Human No 8.8 EC50 = 1.5 nM Funct
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
398 3 1 2 4.9 COc1ccc2c(c1)[C@]13CCN(CC4CC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3
CHEMBL4076632 oprd_human Human No 8.8 EC50 = 1.5 nM Funct
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
469 3 2 3 5.0 O=C(Nc1ccccc1)N1C[C@H]2CC34CCC1C2C31CCN(CC2CC2)C4Cc2ccc(O)cc21
CHEMBL80823 oprd_human Human No 8.8 EC50 = 1.5 nM Bind
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
395 5 3 4 2.0 CC(=O)NC[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C
CHEMBL1169585 oprd_human Human No 8.8 EC50 = 1.5 nM Bind
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
411 4 2 5 3.2 CCC[C@@](C)(O)[C@@H]1CC23C=C[C@]1(OC)[C@H]1Oc4c(O)ccc5c4C12CCN(C)C3C5
CHEMBL3264742 oprd_human Human No 8.8 EC50 = 1.5 nM Bind
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
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
CHEMBL4792012 oprd_human Human No 8.8 EC50 = 1.6 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
579 9 5 8 2.3 CO[C@@]12CC[C@@H](N[C@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL4453526 oprd_rat Rat No 8.8 EC50 = 1.6 nM Funct
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
511 6 3 5 4.8 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21
CHEMBL4594713 oprd_rat Rat No 8.8 EC50 = 1.6 nM Funct
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
511 6 3 5 4.8 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cc4ccccc4o3)ccc21
CHEMBL294616 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL3139175 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
416 2 3 5 2.7 C[C@H](O)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL4296732 oprd_human Human No 8.8 EC50 = 1.6 nM Funct
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
416 2 3 5 2.7 C[C@H](O)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL2387211 oprd_human Human No 8.8 EC50 = 1.7 nM Funct
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
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
CHEMBL3339378 oprd_human Human No 8.8 EC50 = 1.7 nM Funct
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
485 5 3 6 2.5 O=C(NCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5
CHEMBL13470 oprd_human Human Yes 8.8 EC50 = 1.7 nM Bind
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
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
CHEMBL4098662 oprd_human Human No 8.8 EC50 = 1.7 nM Funct
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
446 4 1 3 5.4 Oc1ccc2c(c1)C13CCN(CC4CC4)C(C2)C12CCC1C3[C@@H](CN1CC1CCCCC1)C2
CHEMBL75802 oprd_human Human No 8.8 EC50 = 1.7 nM Bind
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
488 6 4 4 4.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1C/N=C(/S)Nc1ccccc1
CHEMBL58362 oprd_human Human No 8.8 EC50 = 1.7 nM Funct
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
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
CHEMBL58362 oprd_human Human No 8.8 EC50 = 1.7 nM Funct
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
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
CHEMBL4783612 oprd_human Human No 8.8 EC50 = 1.7 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
464 6 3 6 2.5 CO[C@@]12CC[C@@H](N[C@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL4753934 oprd_human Human No 8.8 EC50 = 1.8 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
480 6 4 7 2.2 CO[C@@]12CC[C@H](N[C@@H](Cc3ccc(O)cc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL3262093 oprd_human Human No 8.8 EC50 = 1.8 nM Funct
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
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
CHEMBL1929364 oprd_human Human No 8.8 EC50 = 1.8 nM Funct
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
356 0 1 3 3.9 CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1cccc(O)c13
CHEMBL426084 oprd_human Human Yes 8.7 EC50 = 1.8 nM Funct
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
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
CHEMBL229280 oprd_human Human No 8.7 EC50 = 1.8 nM Funct
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
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
CHEMBL67846 oprd_human Human No 8.7 EC50 = 1.8 nM Funct
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
374 5 1 2 4.9 CCN(CC)C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3)c2ccccc2)cc1
CHEMBL334369 oprd_mouse Mouse No 8.7 EC50 = 1.8 nM Funct
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
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
CHEMBL150625 oprd_mouse Mouse No 8.7 EC50 = 1.8 nM Funct
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
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
CHEMBL3786083 oprd_human Human No 8.7 EC50 = 1.8 nM Funct
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
429 3 2 4 4.2 O=C1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]3(O)CC/C1=C/c1ccccc1
CHEMBL229280 oprd_human Human No 8.7 EC50 = 1.9 nM Funct
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
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
CHEMBL13470 oprd_human Human Yes 8.7 EC50 = 1.9 nM Funct
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
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
CHEMBL4446945 oprd_rat Rat No 8.7 EC50 = 1.9 nM Funct
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
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
CHEMBL4595985 oprd_rat Rat No 8.7 EC50 = 1.9 nM Funct
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
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
CHEMBL408680 oprd_human Human No 8.7 EC50 = 1.9 nM Funct
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
516 5 3 4 4.7 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(Br)c(-c2ccccc2)[nH]1
CHEMBL3139108 oprd_human Human No 8.7 EC50 = 1.9 nM Funct
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
438 2 2 5 4.1 Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL4296726 oprd_human Human No 8.7 EC50 = 1.9 nM Funct
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
438 2 2 5 4.1 Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL1627325 oprd_human Human No 8.7 EC50 = 2.0 nM Funct
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
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
CHEMBL3139134 oprd_human Human No 8.7 EC50 = 2.0 nM Funct
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
422 2 2 4 3.6 Oc1ccc2c(c1)[C@]13CCN(CC(F)F)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL4296727 oprd_human Human No 8.7 EC50 = 2.0 nM Funct
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
422 2 2 4 3.6 Oc1ccc2c(c1)[C@]13CCN(CC(F)F)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3
CHEMBL246956 oprd_human Human No 8.0 EC50 = 10 nM Funct
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
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
CHEMBL562340 oprd_human Human No 8.0 EC50 = 10 nM Funct
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
384 2 2 2 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)C[C@@]1(C2)Cc1c([nH]c2ccccc12)C3
CHEMBL13470 oprd_human Human Yes 8.0 EC50 = 10 nM Funct
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
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
CHEMBL31421 oprd_mouse Mouse Yes 8.0 EC50 = 10 nM Funct
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
None None None None
CHEMBL3823231 oprd_rat Rat No 8.0 EC50 = 10 nM Funct
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
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
CHEMBL271619 oprd_human Human No 8.0 EC50 = 10 nM Bind
Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cellsDisplacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cells
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
CHEMBL4740360 oprd_human Human No 8.0 EC50 = 10.1 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
432 6 4 7 0.7 CO[C@@]12CC[C@H](N[C@@H](CC(=O)O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL3262361 oprd_human Human No 8.0 EC50 = 10.2 nM Funct
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
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
CHEMBL222704 oprd_human Human No 8.0 EC50 = 10.3 nM Funct
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
406 1 2 5 3.0 CCn1c2c(c3c1[C@@H]1Oc4c(O)ccc5c4[C@@]14CCN(C)C(C5)[C@]4(O)C3)CCCC2
CHEMBL3139482 oprd_human Human No 8.0 EC50 = 10.3 nM Funct
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
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
CHEMBL3217271 oprd_human Human No 8.0 EC50 = 10.3 nM Funct
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
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
CHEMBL4649733 oprd_human Human No 8.0 EC50 = 10.4 nM Funct
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
490 3 2 4 4.5 O=C(CCc1ccccc1)N1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL127434 oprd_human Human No 8.0 EC50 = 10.4 nM Bind
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
423 7 1 4 4.3 CCN(CC)C(=O)c1ccc(C(c2cccc(OC)c2)N2CC(C)(C)NCC2C)cc1
CHEMBL3309510 oprd_human Human No 8.0 EC50 = 10.6 nM Funct
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
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
CHEMBL129300 oprd_human Human No 8.0 EC50 = 10.6 nM Funct
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.
390 6 1 3 4.6 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(C(C)=O)c2)cc1
CHEMBL1730890 oprd_human Human Yes 8.0 EC50 = 10.7 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
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
CHEMBL4761211 oprd_human Human No 8.0 EC50 = 10.8 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
446 7 4 7 1.1 CO[C@@]12CC[C@H](N[C@@H](CCC(=O)O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL550261 oprd_human Human No 7.0 EC50 = 100 nM Funct
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
388 2 1 3 4.3 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1CCCCC1
CHEMBL551536 oprd_human Human No 7.0 EC50 = 100 nM Funct
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
424 4 1 3 4.9 CN(Cc1ccccc1)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL3426792 oprd_human Human Yes 7.0 EC50 = 100 nM Bind
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
474 4 0 4 6.8 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccccc2F)cc1
CHEMBL3426794 oprd_human Human Yes 7.0 EC50 = 100 nM Bind
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
474 4 0 4 6.8 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccc(F)cc2)cc1
CHEMBL3426796 oprd_human Human No 7.0 EC50 = 100 nM Bind
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
524 4 0 4 8.0 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2cccc(Cl)c2Cl)cc1
CHEMBL3809323 oprd_human Human No 6.0 EC50 = 1000 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
457 5 2 4 5.3 CN(C)C[C@H]1CCc2cc(-c3ccccc3OC(F)(F)F)ccc2[C@]1(O)c1cccc(O)c1
CHEMBL3426793 oprd_human Human No 6.0 EC50 = 1000 nM Bind
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
474 4 0 4 6.8 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2cccc(F)c2)cc1
CHEMBL3426801 oprd_human Human No 6.0 EC50 = 1000 nM Bind
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
486 5 1 5 6.2 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccccc2CO)cc1
CHEMBL2112214 oprd_human Human No 5.0 EC50 = 10000 nM Funct
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
518 6 0 2 7.8 CC1CCCC(C)N1C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3CCc2ccccc2)c2ccccc2)cc1
CHEMBL2418741 oprd_human Human No 4.0 EC50 = 100000 nM Funct
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
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
CHEMBL3393993 oprd_human Human No 4.0 EC50 = 100000 nM Funct
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
349 5 1 5 3.1 Cc1ccc(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)nc1
CHEMBL3393999 oprd_human Human No 4.0 EC50 = 100000 nM Funct
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
391 5 1 6 4.0 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1nc2ccccc2s1
CHEMBL4755700 oprd_human Human No 6.0 EC50 = 1018 nM Funct
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
549 11 1 3 5.7 CCC(=O)N(Cc1cccc(Cl)c1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1
CHEMBL2159117 oprd_human Human No 7.0 EC50 = 103 nM Funct
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
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
CHEMBL608246 oprd_rat Rat No 7.0 EC50 = 104 nM Funct
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
416 2 2 4 4.0 CCO[C@@]12Cc3c([nH]c4ccccc34)[C@]3(C)Oc4c(O)ccc5c4[C@]13CCN(C)[C@@H]2C5
CHEMBL407057 oprd_human Human No 7.0 EC50 = 104.7 nM Funct
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
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
CHEMBL1388222 oprd_human Human Yes 6.0 EC50 = 1072 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
337 5 1 3 3.4 CN(C)C(CNC(=O)c1cnc(Cl)c(Cl)c1)c1ccccc1
CHEMBL493781 oprd_human Human No 7.0 EC50 = 108 nM Funct
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
337 4 1 5 2.5 Nc1ccnc(N2CCC(N(C(=O)C3CC3)c3ccccn3)CC2)c1
CHEMBL3401554 oprd_mouse Mouse No 7.0 EC50 = 108.1 nM Funct
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
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
CHEMBL2112215 oprd_human Human No 6.0 EC50 = 1081 nM Funct
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
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
CHEMBL388873 oprd_rat Rat No 6.0 EC50 = 1084 nM Funct
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
337 4 2 3 3.5 Oc1cccc([C@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1
CHEMBL20226 oprd_human Human Yes 8.0 EC50 = 11 nM Funct
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
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
CHEMBL2179654 oprd_human Human No 8.0 EC50 = 11 nM Funct
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
536 4 1 5 6.3 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2ncc(-c4ccc(Cl)cc4)cc2C[C@@]3(OCc2ccccc2)[C@H]1C5
CHEMBL3264743 oprd_human Human No 8.0 EC50 = 11 nM Funct
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
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
CHEMBL4126803 oprd_human Human No 7.9 EC50 = 11.8 nM Funct
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
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
CHEMBL4747179 oprd_human Human No 7.9 EC50 = 11.8 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
432 6 4 7 0.7 CO[C@@]12CC[C@@H](N[C@@H](CC(=O)O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL3309508 oprd_human Human No 7.9 EC50 = 11.8 nM Funct
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
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
CHEMBL407057 oprd_human Human No 7.0 EC50 = 110 nM Funct
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
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
CHEMBL222762 oprd_human Human No 7.0 EC50 = 110 nM Funct
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
522 5 2 5 5.0 Oc1ccc2c3c1O[C@H]1c4c(c5c(n4CCc4ccccc4)CCCC5)C[C@@]4(O)C(C2)N(CC2CC2)CC[C@]314
CHEMBL550063 oprd_human Human No 7.0 EC50 = 110 nM Funct
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
320 2 2 3 2.7 NC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL551413 oprd_human Human No 7.0 EC50 = 110 nM Funct
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
334 2 2 3 3.0 CNC(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL392206 oprd_human Human No 7.0 EC50 = 110 nM Funct
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
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
CHEMBL2322568 oprd_rat Rat No 7.0 EC50 = 110 nM Funct
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
429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21
CHEMBL4444479 oprd_rat Rat No 7.0 EC50 = 110 nM Funct
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
429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21
CHEMBL2322568 oprd_rat Rat No 7.0 EC50 = 110 nM Funct
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
429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21
CHEMBL4444479 oprd_rat Rat No 7.0 EC50 = 110 nM Funct
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
429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21
CHEMBL2322568 oprd_rat Rat No 7.0 EC50 = 110 nM Funct
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
429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21
CHEMBL4444479 oprd_rat Rat No 7.0 EC50 = 110 nM Funct
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
429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccccc3)cc21
CHEMBL1628270 oprd_human Human Yes 6.0 EC50 = 1105 nM Funct
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
355 4 0 4 3.1 COc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3
CHEMBL322796 oprd_human Human Yes 6.0 EC50 = 1105 nM Funct
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
355 4 0 4 3.1 COc1cccc2c1[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3
CHEMBL1577639 oprd_human Human No 5.0 EC50 = 11159 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
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
CHEMBL63750 oprd_human Human No 7.0 EC50 = 112 nM Funct
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
492 9 0 2 7.2 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCCc2ccccc2)c2ccccc2)cc1
CHEMBL392206 oprd_human Human No 7.0 EC50 = 112.2 nM Funct
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
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
CHEMBL4786173 oprd_rat Rat No 7.0 EC50 = 112.2 nM Funct
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
369 4 3 4 2.7 CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1
CHEMBL4803577 oprd_rat Rat No 7.0 EC50 = 112.2 nM Funct
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
369 4 3 4 2.7 CN(C)CC1CN(C(=O)Nc2ccccc2)CCC1(O)c1cccc(O)c1
CHEMBL128006 oprd_human Human No 7.0 EC50 = 113 nM Bind
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
385 6 1 3 3.8 CCN(CC)C(=O)c1ccc(C(c2ccc(Cl)cc2)N2CCNCC2)cc1
CHEMBL4759079 oprd_human Human No 6.9 EC50 = 113.8 nM Funct
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
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
CHEMBL382349 oprd_human Human No 6.9 EC50 = 114.8 nM Funct
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
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
CHEMBL4759079 oprd_human Human No 6.9 EC50 = 114.8 nM Funct
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
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
CHEMBL1214025 oprd_human Human No 6.9 EC50 = 114.8 nM Funct
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
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
CHEMBL1416425 oprd_human Human Yes 4.9 EC50 = 11473 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
333 5 2 2 4.3 CN(C)C(CN=C(S)Nc1cccc(Cl)c1)c1ccccc1
CHEMBL3394008 oprd_human Human No 5.9 EC50 = 1150 nM Funct
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
402 6 2 7 1.5 CS(=O)(=O)c1c[nH]c(C(=O)Nc2nc3cccnc3n2CCN2CCCC2)c1
CHEMBL47545 oprd_human Human Yes 6.9 EC50 = 116 nM Funct
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
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
CHEMBL1509052 oprd_human Human Yes 4.9 EC50 = 11628 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
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
CHEMBL4126803 oprd_human Human No 6.9 EC50 = 117 nM Funct
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
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
CHEMBL198238 oprd_human Human No 6.9 EC50 = 117 nM Funct
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
388 5 1 3 4.0 CCNC(=O)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1
CHEMBL199378 oprd_human Human No 6.9 EC50 = 117 nM Funct
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
466 6 1 4 5.6 COc1ccccc1NC(=O)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1
CHEMBL4785222 oprd_human Human No 6.9 EC50 = 117.5 nM Funct
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
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
CHEMBL4785222 oprd_human Human No 6.9 EC50 = 117.7 nM Funct
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
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
CHEMBL1893806 oprd_human Human Yes 4.9 EC50 = 11706 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
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
CHEMBL4749564 oprd_human Human No 6.9 EC50 = 119.9 nM Funct
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
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
CHEMBL1731939 oprd_human Human Yes 4.9 EC50 = 11928 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
471 3 1 3 3.1 O=S(=O)(c1c(Cl)cc(Br)cc1Cl)N1CCN(C(=S)NC2CC2)CC1
CHEMBL222814 oprd_human Human No 7.9 EC50 = 12 nM Funct
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
482 3 2 5 4.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CCc2ccccc2)CCCC4)C[C@@]3(O)C1C5
CHEMBL492552 oprd_human Human No 7.9 EC50 = 12 nM Funct
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
380 4 1 5 3.1 CCN(CC)C(=O)[C@H]1OC2(CCN(c3cc(N)ccn3)CC2)c2ccccc21
CHEMBL3394003 oprd_human Human No 7.9 EC50 = 12 nM Funct
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
369 6 2 5 3.4 CSc1c[nH]c(C(=O)Nc2nc3ccccc3n2CCN2CCCC2)c1
CHEMBL3609620 oprd_human Human No 7.9 EC50 = 12 nM Funct
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
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
CHEMBL4521319 oprd_rat Rat No 7.9 EC50 = 12 nM Funct
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
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
CHEMBL4595172 oprd_rat Rat No 7.9 EC50 = 12 nM Funct
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
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
CHEMBL304196 oprd_human Human No 7.9 EC50 = 12 nM Funct
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
377 6 1 3 4.6 CCN(CC)C(=O)c1ccc(N(c2ccccc2)C2C[C@@H]3CC[C@H](C2)N3)cc1
CHEMBL67545 oprd_human Human No 7.9 EC50 = 12 nM Funct
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
417 8 0 3 5.5 C=CCN1[C@H]2CC[C@@H]1CC(N(c1ccccc1)c1ccc(C(=O)N(CC)CC)cc1)C2
CHEMBL339922 oprd_human Human No 7.9 EC50 = 12.1 nM Funct
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.
378 6 1 3 4.4 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(OC)cc2)cc1
CHEMBL3786970 oprd_human Human No 7.9 EC50 = 12.5 nM Funct
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
415 3 2 4 3.8 O=C1C[C@]23CCN(CC4CC4)[C@H](Cc4ccc(O)cc42)[C@]3(O)C/C1=C\c1ccccc1
CHEMBL317956 oprd_mouse Mouse Yes 7.9 EC50 = 12.6 nM Funct
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)
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
CHEMBL1169580 oprd_human Human No 7.9 EC50 = 12.7 nM Bind
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
411 4 2 5 3.2 CCC[C@](C)(O)[C@@H]1CC23C=C[C@]1(OC)[C@H]1Oc4c(O)ccc5c4C12CCN(C)C3C5
CHEMBL382349 oprd_human Human No 6.9 EC50 = 120 nM Funct
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
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
CHEMBL4790712 oprd_human Human No 6.9 EC50 = 120 nM Funct
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
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
CHEMBL406030 oprd_human Human No 6.9 EC50 = 120 nM Funct
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
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
CHEMBL1214025 oprd_human Human No 6.9 EC50 = 120 nM Funct
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
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
CHEMBL1214027 oprd_human Human No 6.9 EC50 = 120 nM Funct
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
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
CHEMBL15038 oprd_human Human Yes 6.9 EC50 = 120.2 nM Bind
Agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
None None None None
CHEMBL8234 oprd_human Human Yes 6.9 EC50 = 120.2 nM Bind
Agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
None None None None
CHEMBL4749564 oprd_human Human No 6.9 EC50 = 120.2 nM Funct
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
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
CHEMBL2112189 oprd_rat Rat No 5.9 EC50 = 1200 nM Bind
Compound was evaluated for its binding affinity to Opioid receptor delta 1 in rat brainCompound was evaluated for its binding affinity to Opioid receptor delta 1 in rat brain
473 4 2 9 3.1 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](O)C[C@H](SSc2ccc([N+](=O)[O-])cn2)C3[C@H]1C5
CHEMBL126382 oprd_human Human No 6.9 EC50 = 121 nM Bind
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
350 6 1 2 4.3 CCN(CC)C(=O)c1ccc(C(c2ccccc2)C2CCNCC2)cc1
CHEMBL126382 oprd_human Human No 6.9 EC50 = 121 nM Funct
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.
350 6 1 2 4.3 CCN(CC)C(=O)c1ccc(C(c2ccccc2)C2CCNCC2)cc1
CHEMBL1214027 oprd_human Human No 6.9 EC50 = 123.0 nM Funct
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
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
CHEMBL570181 oprd_human Human No 6.9 EC50 = 125 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
475 10 1 5 4.7 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3ncc[nH]3)CC2)cc1
CHEMBL31421 oprd_mouse Mouse Yes 6.9 EC50 = 125.9 nM Bind
Agonist activity at DOR in CD1 mouse vas deferens assessed as inhibition of EFS-induced contractions incubated for 60 minsAgonist activity at DOR in CD1 mouse vas deferens assessed as inhibition of EFS-induced contractions incubated for 60 mins
None None None None
CHEMBL3580743 oprd_human Human No 6.9 EC50 = 125.9 nM Funct
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
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
CHEMBL4636799 oprd_human Human No 6.9 EC50 = 126.8 nM Funct
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
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
CHEMBL361033 oprd_human Human No 6.9 EC50 = 127 nM Funct
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
452 5 3 4 4.3 Cc1[nH]c([C@@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2ccc(O)cc2)nc1-c1ccccc1
CHEMBL4112771 oprd_human Human No 6.9 EC50 = 128.1 nM Funct
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.
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
CHEMBL379405 oprd_human Human No 6.9 EC50 = 128.8 nM Funct
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
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
CHEMBL383458 oprd_human Human No 6.9 EC50 = 128.8 nM Funct
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
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
CHEMBL4107821 oprd_human Human No 6.9 EC50 = 129.0 nM Funct
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.
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
CHEMBL4482942 oprd_human Human No 6.9 EC50 = 129 nM Funct
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
439 9 3 5 3.6 CCOc1ccc(CN2CCCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C
CHEMBL4596318 oprd_human Human No 6.9 EC50 = 129 nM Funct
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
439 9 3 5 3.6 CCOc1ccc(CN2CCCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C
CHEMBL4788377 oprd_human Human No 5.9 EC50 = 1296 nM Bind
Agonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation beta-arrestin recruitment after 60 mins by Pathhunter chemiluminescence assayAgonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation beta-arrestin recruitment after 60 mins by Pathhunter chemiluminescence assay
499 10 1 4 5.2 CCC(=O)N(Cc1ccccc1)C1(C(=O)Nc2ccc(OC)cc2)CCN(CCc2ccccc2)CC1
CHEMBL218600 oprd_human Human No 7.9 EC50 = 13 nM Funct
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
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
CHEMBL222579 oprd_human Human No 7.9 EC50 = 13 nM Funct
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
474 2 2 5 4.6 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2c(c4c(n2CC2CCCCC2)CCCC4)C[C@@]3(O)C1C5
CHEMBL493744 oprd_human Human No 7.9 EC50 = 13 nM Funct
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
412 3 1 4 3.8 Nc1ccnc(N2CCC(C(=O)N3CCc4ccccc4C3)(c3ccccc3)CC2)c1
CHEMBL592969 oprd_human Human No 7.9 EC50 = 13 nM Funct
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
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
CHEMBL592969 oprd_human Human No 7.9 EC50 = 13.2 nM Funct
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
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
CHEMBL31421 oprd_human Human Yes 7.9 EC50 = 13.2 nM Funct
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
None None None None
CHEMBL423694 oprd_human Human No 7.9 EC50 = 13.7 nM Funct
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.
378 6 1 3 4.4 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(OC)c2)cc1
CHEMBL542267 oprd_human Human No 7.9 EC50 = 13.7 nM Funct
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.
378 6 1 3 4.4 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(OC)c2)cc1
CHEMBL4741308 oprd_human Human No 7.9 EC50 = 13.9 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
404 5 4 7 0.2 CO[C@@]12CC[C@H](N[C@@H](CO)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL379405 oprd_human Human No 6.9 EC50 = 130 nM Funct
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
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
CHEMBL383458 oprd_human Human No 6.9 EC50 = 130 nM Funct
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
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
CHEMBL2418740 oprd_human Human No 4.9 EC50 = 13000 nM Funct
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
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
CHEMBL4638693 oprd_human Human No 6.9 EC50 = 131.5 nM Funct
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
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
CHEMBL4747671 oprd_human Human No 6.9 EC50 = 131.8 nM Bind
Agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
1050 38 9 12 3.6 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccc(O)cc2)C(N)=O)C1=O
CHEMBL4522335 oprd_rat Rat No 6.9 EC50 = 132.4 nM Funct
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
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
CHEMBL4744531 oprd_human Human No 5.9 EC50 = 1320 nM Funct
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
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
CHEMBL577394 oprd_human Human No 6.9 EC50 = 133 nM Bind
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
471 9 1 4 5.5 CCN(CC)C(=O)c1ccc(N(c2cccc(CO)c2)C2CCN(Cc3ccccc3)CC2)cc1
CHEMBL66668 oprd_human Human No 5.9 EC50 = 1348 nM Funct
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
484 8 0 3 6.9 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2cccs2)c2ccccc2)cc1
CHEMBL205049 oprd_mouse Mouse No 6.9 EC50 = 135 nM Funct
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
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
CHEMBL205049 oprd_human Human No 6.9 EC50 = 135 nM Funct
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
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
CHEMBL4109652 oprd_human Human No 6.9 EC50 = 135.5 nM Funct
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.
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
CHEMBL4564309 oprd_human Human No 5.9 EC50 = 1360 nM Funct
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
425 9 3 5 3.2 CCOc1ccc(CN2CCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C
CHEMBL4596196 oprd_human Human No 5.9 EC50 = 1360 nM Funct
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
425 9 3 5 3.2 CCOc1ccc(CN2CCCC2)cc1CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C
CHEMBL340032 oprd_human Human Yes 5.9 EC50 = 1380.4 nM Bind
Agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in DOR/G beta1 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assayAgonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in DOR/G beta1 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assay
None None None None
CHEMBL68113 oprd_human Human No 5.9 EC50 = 1387 nM Funct
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
478 8 0 2 6.8 CCN(CC)C(=O)c1ccc(/C(=C2\C[C@@H]3CC[C@H](C2)N3CCc2ccccc2)c2ccccc2)cc1
CHEMBL495346 oprd_human Human No 7.9 EC50 = 14 nM Funct
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
432 6 2 6 3.6 COc1ccc(C(=O)NC2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)c(OC)c1
CHEMBL250993 oprd_human Human No 7.9 EC50 = 14 nM Funct
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
480 6 1 2 5.4 C[C@H]1C2Cc3ccc(C(=O)NCCc4cccc(Br)c4)cc3[C@@]1(C)CCN2CC1CC1
CHEMBL495402 oprd_human Human No 7.9 EC50 = 14 nM Funct
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
382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl
CHEMBL3823830 oprd_rat Rat No 7.9 EC50 = 14 nM Funct
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
487 6 3 5 4.3 COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21
CHEMBL3634250 oprd_rat Rat No 7.9 EC50 = 14 nM Funct
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
477 6 3 4 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3CCCCC3)ccc21
CHEMBL202238 oprd_human Human No 7.9 EC50 = 14 nM Funct
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
395 5 0 5 4.3 c1ccc(Cn2ccnc2C2(c3ccccc3)CCN(c3ncccn3)CC2)cc1
CHEMBL584727 oprd_human Human No 7.9 EC50 = 14.1 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
461 9 2 5 4.4 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3c[nH]cn3)CC2)cc1
CHEMBL126141 oprd_human Human No 7.9 EC50 = 14.1 nM Funct
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.
416 7 0 2 6.0 CCN(CC)C(=O)c1ccc(C(=C2CCN(CC=C(C)C)CC2)c2ccccc2)cc1
CHEMBL2397016 oprd_human Human No 7.9 EC50 = 14.2 nM Funct
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
495 4 2 6 3.5 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1cc2ccccc2cn1
CHEMBL3086750 oprd_human Human No 7.9 EC50 = 14.2 nM Funct
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
495 4 2 6 3.5 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1cc2ccccc2cn1
CHEMBL13470 oprd_human Human Yes 7.8 EC50 = 14.4 nM Funct
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
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
CHEMBL4632584 oprd_human Human No 7.8 EC50 = 14.4 nM Funct
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
476 2 2 4 4.1 O=C(Cc1ccccc1)N1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL4079574 oprd_human Human No 7.8 EC50 = 14.5 nM Bind
Agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in DOR/G beta1 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assayAgonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as increase in DOR/G beta1 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assay
337 3 2 3 3.7 C[C@H]1[C@H]2Cc3ccc(O)cc3[C@]1(C)CCN2C[C@@H](O)c1ccccc1
CHEMBL2408016 oprd_human Human No 7.8 EC50 = 14.5 nM Funct
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
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
CHEMBL570448 oprd_human Human No 7.8 EC50 = 14.5 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
475 9 1 6 4.5 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3nccn3C)CC2)cc1
CHEMBL3916122 oprd_human Human No 7.8 EC50 = 14.7 nM Funct
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.
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
CHEMBL273820 oprd_human Human No 7.8 EC50 = 14.8 nM Bind
Agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
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(=O)O
CHEMBL3139588 oprd_human Human No 7.8 EC50 = 14.8 nM Funct
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
378 6 2 3 4.4 CN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1
CHEMBL3217272 oprd_human Human No 7.8 EC50 = 14.8 nM Funct
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
378 6 2 3 4.4 CN[C@H]1C[C@H]2C[C@@](c3cccc(O)c3)(C1)[C@H](C)CN2CCCc1ccccc1
CHEMBL4754992 oprd_mouse Mouse No 6.9 EC50 = 140 nM Bind
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electric-field induced measured after 5 minsAgonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electric-field induced measured after 5 mins
556 15 6 8 0.3 CC(C)C[C@H](OC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)O
CHEMBL4782368 oprd_human Human No 6.9 EC50 = 140 nM Funct
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
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
CHEMBL3264744 oprd_human Human No 6.9 EC50 = 140 nM Bind
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
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
CHEMBL495094 oprd_human Human No 6.9 EC50 = 140 nM Funct
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
392 4 2 4 3.8 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3cc(O)ccc32)cc1
CHEMBL1515502 oprd_human Human Yes 4.9 EC50 = 14052 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
467 10 2 5 3.9 CCOc1ccc(S(=O)(=O)Nc2cccc(C(=O)NCC(c3ccccc3)N(C)C)c2)cc1
CHEMBL569084 oprd_human Human No 6.9 EC50 = 141 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
485 10 0 4 6.0 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3ccccc3)CC2)cc1
CHEMBL3264743 oprd_human Human No 6.9 EC50 = 141 nM Bind
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
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
CHEMBL1315948 oprd_human Human No 4.9 EC50 = 14159 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
426 5 1 3 6.7 CCc1ccc(Nc2n[n+](-c3ccccc3)c(-c3c(Cl)cccc3Cl)s2)cc1
CHEMBL1617450 oprd_human Human No 4.9 EC50 = 14159 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
426 5 1 3 6.7 CCc1ccc(Nc2n[n+](-c3ccccc3)c(-c3c(Cl)cccc3Cl)s2)cc1
CHEMBL4586954 oprd_human Human No 6.9 EC50 = 142 nM Funct
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
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
CHEMBL4594798 oprd_human Human No 6.9 EC50 = 142 nM Funct
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
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
CHEMBL4748689 oprd_human Human No 6.8 EC50 = 143 nM Funct
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
405 6 1 4 4.5 COC(=O)/C=C/[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1
CHEMBL4248801 oprd_rat Rat No 6.8 EC50 = 143.9 nM Funct
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
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
CHEMBL68416 oprd_human Human No 5.8 EC50 = 1463 nM Funct
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
476 6 0 2 6.6 O=C(c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2ccccc2)cc1)N1CCCC1
CHEMBL382326 oprd_human Human No 5.8 EC50 = 1479 nM Funct
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
436 5 1 3 5.5 O=C(Nc1ccccc1)N1CCC(c2ccccc2)(c2nccn2Cc2ccccc2)CC1
CHEMBL3145240 oprd_human Human Yes 4.8 EC50 = 14800 nM Funct
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]
376 3 1 4 4.7 Cc1ccc(-n2[nH]c(C)c(C=Nc3ccc(Cl)c4cccnc34)c2=O)cc1
CHEMBL1734003 oprd_human Human Yes 5.8 EC50 = 1487 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
509 10 2 6 7.0 CCN(CC)Cc1cc(Nc2c3ccccc3nc3c4ccccc4n(C)c23)cc(CN(CC)CC)c1O
CHEMBL1740933 oprd_human Human Yes 5.8 EC50 = 1487 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
509 10 2 6 7.0 CCN(CC)Cc1cc(Nc2c3ccccc3nc3c4ccccc4n(C)c23)cc(CN(CC)CC)c1O
CHEMBL307775 oprd_human Human No 6.8 EC50 = 149 nM Funct
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
388 5 0 2 5.2 CCN(CC)C(=O)c1ccc(/C(=C2\C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1
CHEMBL408330 oprd_human Human No 7.8 EC50 = 15 nM Funct
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
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
CHEMBL294616 oprd_human Human No 7.8 EC50 = 15 nM Funct
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
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
CHEMBL218651 oprd_human Human No 7.8 EC50 = 15 nM Funct
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
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
CHEMBL2408016 oprd_human Human No 7.8 EC50 = 15 nM Funct
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
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
CHEMBL3823815 oprd_rat Rat No 7.8 EC50 = 15 nM Funct
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
515 9 3 6 4.1 CCOC(=O)CN1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21
CHEMBL408330 oprd_human Human No 7.8 EC50 = 15.1 nM Funct
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
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
CHEMBL522143 oprd_human Human No 7.8 EC50 = 15.2 nM Funct
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
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
CHEMBL254919 oprd_human Human No 7.8 EC50 = 15.5 nM Funct
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
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
CHEMBL254919 oprd_human Human No 7.8 EC50 = 15.5 nM Funct
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
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
CHEMBL3264744 oprd_human Human No 7.8 EC50 = 15.6 nM Funct
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
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
CHEMBL70 oprd_human Human Yes 7.8 EC50 = 15.6 nM Funct
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
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
CHEMBL13470 oprd_human Human Yes 7.8 EC50 = 15.7 nM Funct
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
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
CHEMBL13470 oprd_human Human Yes 7.8 EC50 = 15.7 nM Funct
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
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
CHEMBL294616 oprd_human Human No 7.8 EC50 = 15.9 nM Funct
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
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
CHEMBL126370 oprd_human Human No 7.8 EC50 = 15.9 nM Funct
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.
366 5 1 2 4.5 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccccc2F)cc1
CHEMBL247064 oprd_human Human No 6.8 EC50 = 150 nM Funct
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
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
CHEMBL272665 oprd_human Human No 6.8 EC50 = 150 nM Funct
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
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
CHEMBL557054 oprd_human Human No 6.8 EC50 = 150 nM Funct
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
377 4 1 4 3.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cn1
CHEMBL3609616 oprd_human Human No 6.8 EC50 = 150 nM Funct
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
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
CHEMBL439026 oprd_human Human No 6.8 EC50 = 150 nM Funct
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
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
CHEMBL290440 oprd_rat Rat No 5.8 EC50 = 1500 nM Bind
The binding affinity was evaluated against [3H]dalamid binding to rat brain membranes (Opioid receptor delta 1)The binding affinity was evaluated against [3H]dalamid binding to rat brain membranes (Opioid receptor delta 1)
486 11 1 5 4.7 CCOc1ccc(Cc2nc3cc(NC(=O)CBr)ccc3n2CCN(CC)CC)cc1
CHEMBL1507251 oprd_human Human Yes 4.8 EC50 = 15054 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
344 2 1 5 3.6 Cc1cc(/C=C2\SC(=S)N(C)C2=O)c(C)n1-c1ccc(O)cc1
CHEMBL573739 oprd_human Human No 6.8 EC50 = 151 nM Bind
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
498 9 1 4 5.3 CCN(CC)C(=O)c1ccc(N(c2cccc(C(=O)NC)c2)C2CCN(Cc3ccccc3)CC2)cc1
CHEMBL4112051 oprd_human Human No 6.8 EC50 = 151.2 nM Funct
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.
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
CHEMBL439026 oprd_human Human No 6.8 EC50 = 151.4 nM Funct
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
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
CHEMBL4793888 oprd_human Human No 6.8 EC50 = 152 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
445 8 4 7 1.4 CO[C@@]12CC[C@H](N[C@@H](CCCCN)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL63597 oprd_human Human No 6.8 EC50 = 153 nM Funct
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
388 5 0 2 5.2 CCN(CC)C(=O)c1ccc(/C(=C2/C[C@@H]3CC[C@H](C2)N3C)c2ccccc2)cc1
CHEMBL4777999 oprd_human Human No 6.8 EC50 = 154.9 nM Funct
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
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
CHEMBL1892729 oprd_human Human Yes 4.8 EC50 = 15492 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
533 10 2 9 2.7 COC(=O)C1=C(C)N(CCCC(=O)O)C(=O)NC1c1ccccc1OS(=O)(=O)c1ccccc1[N+](=O)[O-]
CHEMBL841 oprd_human Human Yes 6.8 EC50 = 156 nM Funct
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1
CHEMBL4777999 oprd_human Human No 6.8 EC50 = 156.7 nM Funct
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
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
CHEMBL248839 oprd_human Human No 7.8 EC50 = 16 nM Funct
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
392 0 3 4 2.9 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2c2[nH]c4ccc(F)cc4c2C[C@@]3(O)[C@H]1C5
CHEMBL522854 oprd_human Human No 7.8 EC50 = 16 nM Funct
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
386 3 1 7 3.0 Nc1ccnc(N2CCC(n3c(=O)n(-c4ccccc4)c4cccnc43)CC2)c1
CHEMBL556648 oprd_human Human No 7.8 EC50 = 16 nM Funct
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
378 4 1 3 4.2 CCN(CC)C(=O)c1ccc([C@H]2CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL294616 oprd_human Human No 7.8 EC50 = 16 nM Funct
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
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
CHEMBL63213 oprd_human Human No 7.8 EC50 = 16 nM Funct
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
517 8 1 2 7.3 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2c[nH]c3ccccc23)c2ccccc2)cc1
CHEMBL2371978 oprd_human Human No 7.8 EC50 = 16.6 nM Funct
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
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
CHEMBL31421 oprd_human Human Yes 7.8 EC50 = 17.0 nM Funct
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
None None None None
CHEMBL3608937 oprd_human Human No 6.8 EC50 = 160 nM Funct
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
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
CHEMBL1169582 oprd_human Human No 6.8 EC50 = 160 nM Bind
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
383 3 1 5 2.6 CO[C@@H](C)[C@@H]1CC23C=C[C@]1(OC)[C@H]1Oc4c(O)ccc5c4C12CCN(C)C3C5
CHEMBL3809684 oprd_human Human No 5.8 EC50 = 1600 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
391 4 2 3 4.6 CN(C)C[C@H]1CCc2cc(-c3ccccc3F)ccc2[C@]1(O)c1cccc(O)c1
CHEMBL1511139 oprd_human Human Yes 5.8 EC50 = 1600 nM Funct
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]
479 10 2 5 3.4 CC(=O)c1ccc(S(=O)(=O)NCc2ccc(C(=O)NCC(c3ccccc3)N(C)C)cc2)cc1
CHEMBL2418744 oprd_human Human No 4.8 EC50 = 16000 nM Funct
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
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
CHEMBL126842 oprd_human Human No 6.8 EC50 = 161 nM Funct
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.
362 5 0 2 4.7 CCN(CC)C(=O)c1ccc(C(=C2CCN(C)CC2)c2ccccc2)cc1
CHEMBL326860 oprd_human Human No 5.8 EC50 = 1613 nM Funct
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
397 7 0 4 4.3 CCCCOc1cccc2c1C13CCN(CC4CC4)[C@H](C2)[C@]1(OC)CCC(=O)C3
CHEMBL4744365 oprd_human Human No 6.8 EC50 = 162 nM Funct
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
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
CHEMBL4744365 oprd_human Human No 6.8 EC50 = 162.2 nM Funct
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
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
CHEMBL3580744 oprd_human Human No 6.8 EC50 = 162.2 nM Funct
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
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
CHEMBL3589705 oprd_human Human No 5.8 EC50 = 1639 nM Funct
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
534 9 1 5 5.8 CC(C)C[C@H]1CN2C(=CC3=NC[C@H](Cc4ccccc4)N3C[C@@H]2Cc2ccc(O)cc2)N1CCc1ccccc1
CHEMBL4109220 oprd_human Human No 6.8 EC50 = 164.7 nM Funct
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.
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
CHEMBL392185 oprd_human Human No 6.8 EC50 = 166.0 nM Funct
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
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
CHEMBL13470 oprd_rat Rat Yes 6.8 EC50 = 166 nM Funct
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
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
CHEMBL50284 oprd_mouse Mouse No 6.8 EC50 = 168 nM Bind
Effective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitroEffective concentration was measured towards delta opioid receptor using mouse vas deferens(MVD, delta) bioassay in vitro
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
CHEMBL567818 oprd_human Human No 7.8 EC50 = 17 nM Bind
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
469 9 0 4 5.8 CCN(CC)C(=O)c1ccc(N(c2cccc(C=O)c2)C2CCN(Cc3ccccc3)CC2)cc1
CHEMBL271619 oprd_human Human No 7.8 EC50 = 17 nM Funct
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
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
CHEMBL2371978 oprd_human Human No 7.8 EC50 = 17 nM Funct
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
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
CHEMBL3596366 oprd_human Human No 7.8 EC50 = 17.2 nM Funct
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
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
CHEMBL3598302 oprd_human Human No 7.8 EC50 = 17.2 nM Funct
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
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
CHEMBL1332208 oprd_human Human Yes 7.8 EC50 = 17.3 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
497 8 2 6 5.6 COc1ccc(C2Nc3ccccc3C(=O)N2Cc2ccco2)cc1COc1ccc(NC(C)=O)cc1
CHEMBL4111231 oprd_human Human No 7.8 EC50 = 17.3 nM Funct
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.
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
CHEMBL570645 oprd_human Human No 7.8 EC50 = 17.4 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
491 10 0 5 6.1 CCN(CC)C(=O)c1ccc(N(c2cccc(OC)c2)C2CCN(CCc3cccs3)CC2)cc1
CHEMBL611139 oprd_human Human No 7.8 EC50 = 17.5 nM Funct
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
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
CHEMBL2387327 oprd_human Human No 6.8 EC50 = 170 nM Funct
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
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
CHEMBL392185 oprd_human Human No 6.8 EC50 = 170 nM Funct
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
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
CHEMBL133719 oprd_mouse Mouse No 6.8 EC50 = 170 nM Funct
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
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
CHEMBL246682 oprd_human Human No 5.8 EC50 = 1700 nM Funct
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
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
CHEMBL3393991 oprd_human Human No 5.8 EC50 = 1700 nM Funct
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
402 5 1 4 4.7 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(Cl)c(Cl)c1
CHEMBL493752 oprd_human Human No 6.8 EC50 = 171 nM Funct
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
366 4 2 5 2.5 Nc1ccnc(N2CCC(NC(=O)[C@@H]3CCCO3)(c3ccccc3)CC2)c1
CHEMBL23472 oprd_human Human Yes 4.8 EC50 = 17179 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
464 9 1 4 4.3 OC(=O)COc1cccc(c1)C(N(C(=O)Cc1ccc(c(c1)Cl)Cl)C)CN1CCCC1
CHEMBL4795492 oprd_human Human No 6.8 EC50 = 172 nM Funct
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
515 11 1 3 5.0 CCC(=O)N(Cc1ccccc1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1
CHEMBL66387 oprd_human Human No 6.8 EC50 = 173 nM Funct
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
492 8 0 3 6.5 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CC(=O)c2ccccc2)c2ccccc2)cc1
CHEMBL4800237 oprd_human Human No 6.8 EC50 = 173.8 nM Funct
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
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
CHEMBL4800237 oprd_human Human No 6.8 EC50 = 174 nM Funct
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
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
CHEMBL356587 oprd_mouse Mouse No 6.8 EC50 = 174 nM Funct
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
358 5 1 3 4.3 Oc1cccc(C(c2ccccc2)N2CCN(Cc3ccccc3)CC2)c1
CHEMBL4107918 oprd_human Human No 6.8 EC50 = 175.8 nM Funct
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.
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
CHEMBL4112656 oprd_human Human No 6.8 EC50 = 175.8 nM Funct
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.
447 6 1 5 4.0 COc1ccc2c3c1O[C@@H]1[C@]34CCN[C@H](C2)[C@]42CC[C@@]1(OC)[C@@H](COCc1ccccc1)C2
CHEMBL4241369 oprd_rat Rat No 5.8 EC50 = 1759 nM Funct
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
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
CHEMBL4745899 oprd_human Human No 6.8 EC50 = 177 nM Funct
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
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
CHEMBL304989 oprd_human Human No 6.8 EC50 = 177 nM Funct
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
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
CHEMBL1307063 oprd_human Human Yes 4.8 EC50 = 17815 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
328 5 2 3 3.7 Cc1cccc(NC(S)=NCC(c2cccnc2)N(C)C)c1C
CHEMBL401278 oprd_human Human No 7.8 EC50 = 18 nM Funct
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
478 7 1 2 6.3 C[C@H]1C2Cc3ccc(C(=O)NCCc4cccc(-c5ccccc5)c4)cc3[C@@]1(C)CCN2CC1CC1
CHEMBL2208361 oprd_human Human No 7.8 EC50 = 18 nM Funct
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
536 9 1 3 7.0 CC(C)Oc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1
CHEMBL125734 oprd_human Human No 7.8 EC50 = 18 nM Bind
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
401 6 1 3 4.3 CCN(CC)C(=O)c1ccc(C(c2cccc3ccccc23)N2CCNCC2)cc1
CHEMBL31605 oprd_human Human No 7.7 EC50 = 18.6 nM Funct
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
423 1 2 5 3.2 CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5
CHEMBL265813 oprd_human Human Yes 7.7 EC50 = 18.6 nM Funct
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
None None None None
CHEMBL405618 oprd_human Human Yes 7.7 EC50 = 18.6 nM Funct
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
None None None None
CHEMBL265813 oprd_human Human Yes 7.7 EC50 = 18.6 nM Funct
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
None None None None
CHEMBL405618 oprd_human Human Yes 7.7 EC50 = 18.6 nM Funct
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
None None None None
CHEMBL411557 oprd_human Human Yes 7.7 EC50 = 18.6 nM Funct
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
None None None None
CHEMBL570233 oprd_human Human No 7.7 EC50 = 18.9 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
477 9 1 4 6.4 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCC3CCCCC3)CC2)cc1
CHEMBL4763725 oprd_human Human No 6.8 EC50 = 180 nM Funct
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
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
CHEMBL3393881 oprd_human Human No 5.8 EC50 = 1800 nM Funct
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
352 5 1 4 3.5 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(F)cc1
CHEMBL3394006 oprd_human Human No 5.7 EC50 = 1850 nM Funct
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
384 5 2 5 3.0 O=C(Nc1nc2ccccc2n1CCN1CC[C@H](O)C1)c1ccc(Cl)cc1
CHEMBL4577032 oprd_human Human No 5.7 EC50 = 1862.1 nM Bind
Agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to beta-arrestin-2 assessed as increase in DOR/beta-arrestin-2 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assayAgonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to beta-arrestin-2 assessed as increase in DOR/beta-arrestin-2 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assay
351 4 1 3 4.3 CO[C@H](CN1CC[C@@]2(C)c3cc(O)ccc3C[C@@H]1[C@@H]2C)c1ccccc1
CHEMBL127638 oprd_human Human No 6.7 EC50 = 187 nM Bind
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
381 7 1 4 3.2 CCN(CC)C(=O)c1ccc(C(c2ccc(OC)cc2)N2CCNCC2)cc1
CHEMBL4115338 oprd_human Human No 6.7 EC50 = 188.7 nM Funct
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.
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
CHEMBL361274 oprd_mouse Mouse No 7.7 EC50 = 19 nM Funct
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
438 5 3 4 4.0 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1
CHEMBL386212 oprd_human Human No 7.7 EC50 = 19 nM Funct
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
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
CHEMBL1824517 oprd_human Human No 7.7 EC50 = 19 nM Funct
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
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
CHEMBL1852458 oprd_human Human No 7.7 EC50 = 19 nM Funct
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
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
CHEMBL361274 oprd_human Human No 7.7 EC50 = 19 nM Funct
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
438 5 3 4 4.0 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1
CHEMBL2179661 oprd_human Human No 7.7 EC50 = 19 nM Funct
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
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
CHEMBL494462 oprd_human Human No 7.7 EC50 = 19 nM Funct
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
376 4 1 3 4.1 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL494462 oprd_human Human No 7.7 EC50 = 19 nM Funct
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
376 4 1 3 4.1 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL2113372 oprd_human Human No 7.7 EC50 = 19 nM Funct
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.
485 6 3 4 4.9 CCCCCCC(=O)N[C@@]12Cc3c([nH]c4ccccc34)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)C2C5
CHEMBL573757 oprd_human Human No 7.7 EC50 = 19.2 nM Bind
Agonist activity at human delta opioid receptor by GTP[gamma]35S binding assayAgonist activity at human delta opioid receptor by GTP[gamma]35S binding assay
456 8 1 4 5.6 CCN(CC)C(=O)c1ccc(N(c2cccc(N)c2)C2CCN(Cc3ccccc3)CC2)cc1
CHEMBL4126322 oprd_rat Rat No 7.7 EC50 = 19.4 nM Funct
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
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
CHEMBL2113672 oprd_human Human No 7.7 EC50 = 19.4 nM Bind
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
459 5 1 5 4.2 CO[C@]12C=C[C@@]3(C[C@H]1[C@H](C)OCc1ccccc1)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5
CHEMBL2397020 oprd_human Human No 7.7 EC50 = 19.7 nM Funct
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
445 4 2 6 2.4 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1ccccn1
CHEMBL3086746 oprd_human Human No 7.7 EC50 = 19.7 nM Funct
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
445 4 2 6 2.4 O=C(N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5)c1ccccn1
CHEMBL4636807 oprd_human Human No 6.7 EC50 = 190 nM Funct
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
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
CHEMBL4650976 oprd_human Human No 6.7 EC50 = 190 nM Funct
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
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
CHEMBL2419540 oprd_human Human No 6.7 EC50 = 190 nM Funct
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
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
CHEMBL551615 oprd_human Human No 6.7 EC50 = 190 nM Funct
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
374 2 1 3 3.7 CCN1CCc2cc(C3=CC4(CCNCC4)Oc4ccccc43)ccc2C1=O
CHEMBL235743 oprd_human Human Yes 6.7 EC50 = 190 nM Funct
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
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
CHEMBL495073 oprd_human Human No 6.7 EC50 = 190 nM Funct
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
307 2 1 3 3.6 COc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL235743 oprd_human Human Yes 6.7 EC50 = 190 nM Funct
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
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
CHEMBL235743 oprd_human Human Yes 6.7 EC50 = 190.6 nM Funct
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
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
CHEMBL235743 oprd_human Human Yes 6.7 EC50 = 190.6 nM Funct
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
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
CHEMBL4740521 oprd_human Human No 6.7 EC50 = 199 nM Funct
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
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
CHEMBL4740521 oprd_human Human No 6.7 EC50 = 199.5 nM Funct
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
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
CHEMBL4750006 oprd_human Human No 6.7 EC50 = 199.5 nM Funct
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
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
CHEMBL4449491 oprd_human Human No 5.7 EC50 = 1995.3 nM Funct
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
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
CHEMBL438871 oprd_human Human No 8.7 EC50 = 2 nM Funct
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
512 7 1 2 6.9 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(Cl)cc5)cc4)cc3[C@@]1(C)CCN2CC1CC1
CHEMBL3264745 oprd_human Human No 8.7 EC50 = 2 nM Bind
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
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
CHEMBL4749747 oprd_human Human No 8.7 EC50 = 2.0 nM Bind
Agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
1450 52 13 18 4.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCSC)NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(N)=O)C1=O
CHEMBL294616 oprd_mouse Mouse No 8.7 EC50 = 2.1 nM Funct
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
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
CHEMBL4788003 oprd_human Human No 8.7 EC50 = 2.2 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
503 6 4 6 3.0 CO[C@@]12CC[C@@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL2387213 oprd_human Human No 8.7 EC50 = 2.2 nM Funct
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
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
CHEMBL607016 oprd_human Human No 8.7 EC50 = 2.2 nM Funct
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
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
CHEMBL4781006 oprd_human Human No 8.7 EC50 = 2.2 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
402 5 3 6 1.7 CC[C@H](N[C@@H]1CC[C@@]2(OC)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3C)[C@H]1O5)C(=O)O
CHEMBL1766205 oprd_human Human No 8.6 EC50 = 2.3 nM Funct
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
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
CHEMBL3139110 oprd_human Human No 8.6 EC50 = 2.3 nM Funct
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
402 2 3 5 2.3 OCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL4296735 oprd_human Human No 8.6 EC50 = 2.3 nM Funct
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
402 2 3 5 2.3 OCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL1929362 oprd_human Human No 8.6 EC50 = 2.3 nM Funct
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
398 2 1 3 4.9 CC(C)CN1CC[C@]23Cc4nc5ccccc5cc4C[C@H]2[C@H]1Cc1cccc(O)c13
CHEMBL3309264 oprd_human Human No 8.6 EC50 = 2.4 nM Funct
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
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
CHEMBL4126050 oprd_rat Rat No 8.6 EC50 = 2.4 nM Funct
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
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
CHEMBL218763 oprd_human Human No 8.6 EC50 = 2.5 nM Funct
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
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
CHEMBL3287467 oprd_human Human No 8.6 EC50 = 2.5 nM Funct
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
396 2 1 3 4.6 Oc1ccc2c(c1)[C@]13CCN(CC4CC4)C[C@@]1(C2)Cc1cc2ccccc2nc1C3
CHEMBL2419537 oprd_human Human No 8.6 EC50 = 2.5 nM Funct
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
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
CHEMBL247758 oprd_human Human No 8.6 EC50 = 2.5 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 8.6 EC50 = 2.5 nM Funct
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
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
CHEMBL376355 oprd_human Human No 8.6 EC50 = 2.5 nM Funct
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
381 2 2 5 3.5 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CCC1)C2
CHEMBL218763 oprd_human Human No 8.6 EC50 = 2.5 nM Funct
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
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
CHEMBL448998 oprd_human Human No 8.6 EC50 = 2.5 nM Funct
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
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
CHEMBL4755067 oprd_human Human No 8.6 EC50 = 2.5 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
503 6 4 6 3.0 CO[C@@]12CC[C@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL3139135 oprd_human Human No 8.6 EC50 = 2.5 nM Funct
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
430 4 2 5 3.4 CCOCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL4296736 oprd_human Human No 8.6 EC50 = 2.5 nM Funct
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
430 4 2 5 3.4 CCOCCN1CC[C@]23Cc4nc5ccccc5cc4C[C@@]2(O)[C@H]1Cc1ccc(O)cc13
CHEMBL3759292 oprd_mouse Mouse No 8.6 EC50 = 2.6 nM Bind
Agonist activity at delta-opioid receptor in mouse vas deferensAgonist activity at delta-opioid receptor in mouse vas deferens
514 8 4 5 2.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)NCC(=O)NCc1ccccc1
CHEMBL3808766 oprd_human Human No 8.6 EC50 = 2.6 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assayAgonist activity at human DOR expressed in CHO cell membranes after 60 mins by [35S]GTP-gamma-S binding assay
403 5 2 4 4.4 COc1ccccc1-c1ccc2c(c1)CCC(CN(C)C)C2(O)c1cccc(O)c1
CHEMBL4798954 oprd_human Human No 8.6 EC50 = 2.6 nM Funct
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
337 4 2 3 3.5 Oc1cccc([C@@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1
CHEMBL448998 oprd_human Human No 8.6 EC50 = 2.6 nM Funct
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
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
CHEMBL200199 oprd_human Human Yes 8.6 EC50 = 2.6 nM Bind
Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cellsDisplacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cells
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
CHEMBL569006 oprd_human Human No 8.6 EC50 = 2.6 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
489 9 1 4 5.9 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(CCc3cccc(F)c3)CC2)cc1
CHEMBL3262089 oprd_human Human No 8.6 EC50 = 2.7 nM Funct
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
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
CHEMBL2208352 oprd_human Human No 8.6 EC50 = 2.8 nM Funct
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
522 8 1 3 6.6 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1C
CHEMBL373984 oprd_human Human No 8.6 EC50 = 2.8 nM Funct
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
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
CHEMBL1649939 oprd_human Human No 8.6 EC50 = 2.8 nM Funct
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
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
CHEMBL2387329 oprd_human Human No 8.6 EC50 = 2.8 nM Funct
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
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
CHEMBL76573 oprd_human Human No 8.6 EC50 = 2.8 nM Bind
Agonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptorAgonist potency using GTP-gamma [35S]- binding assay for delta-opioid receptor
423 6 3 4 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1Cc2ccccc2C[C@H]1CNCC(C)(C)C
CHEMBL1649939 oprd_human Human No 8.6 EC50 = 2.8 nM Funct
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
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
CHEMBL4754111 oprd_human Human No 8.6 EC50 = 2.8 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
431 6 4 7 -0.0 CO[C@@]12CC[C@@H](NCC(=O)NCC(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL389652 oprd_human Human No 8.5 EC50 = 2.9 nM Funct
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
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
CHEMBL389652 oprd_human Human No 8.5 EC50 = 2.9 nM Funct
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
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
CHEMBL389652 oprd_human Human No 8.5 EC50 = 2.9 nM Funct
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
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
CHEMBL294616 oprd_human Human No 8.5 EC50 = 3.0 nM Funct
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
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
CHEMBL13470 oprd_human Human Yes 8.5 EC50 = 3.0 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
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
CHEMBL2159118 oprd_human Human No 7.7 EC50 = 20 nM Funct
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
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
CHEMBL249567 oprd_human Human No 7.7 EC50 = 20 nM Funct
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
480 6 1 2 5.4 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(Br)cc4)cc3[C@@]1(C)CCN2CC1CC1
CHEMBL563893 oprd_human Human No 7.7 EC50 = 20 nM Funct
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
390 4 1 3 4.5 CCN(CC)C(=O)c1ccc(C2=CC3(CCCNCC3)Oc3ccccc32)cc1
CHEMBL494480 oprd_human Human Yes 7.7 EC50 = 20 nM Funct
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
392 4 2 4 3.8 CCN(C(=O)c1ccc(cc1)C1=CC2(CCNCC2)Oc2c1c(O)ccc2)CC
CHEMBL606642 oprd_rat Rat No 7.7 EC50 = 20 nM Bind
The binding affinity was evaluated against [3H]dalamid binding to neuroblastoma X glioma hybrid cell NG108-15 (Opioid receptor delta 1)membranesThe binding affinity was evaluated against [3H]dalamid binding to neuroblastoma X glioma hybrid cell NG108-15 (Opioid receptor delta 1)membranes
382 2 1 6 2.5 CO[C@]12C=C[C@@]3(C[C@@H]1N=C=S)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@H]2O5
CHEMBL4757463 oprd_human Human No 7.7 EC50 = 20.1 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
388 5 3 6 1.3 CO[C@@]12CC[C@@H](NCCC(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL4748047 oprd_human Human No 7.7 EC50 = 20.5 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
456 5 3 6 2.8 CO[C@@]12CC[C@H](N[C@H](C(=O)O)C3CCCCC3)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL3264746 oprd_human Human No 7.7 EC50 = 20.5 nM Bind
Agonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human delta opioid receptor expressed in HEK293 cells by CellKey method
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
CHEMBL127495 oprd_human Human No 7.7 EC50 = 20.5 nM Funct
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.
363 5 2 3 3.9 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2cccc(N)c2)cc1
CHEMBL110640 oprd_human Human No 7.7 EC50 = 20.6 nM Funct
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
459 8 0 4 5.1 COc1cccc2c1C13CCN(CC4CC4)[C@H](C2)[C@]1(OCCCc1ccccc1)CCC(=O)C3
CHEMBL2371977 oprd_human Human No 7.7 EC50 = 20.9 nM Funct
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
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
CHEMBL611400 oprd_human Human No 7.7 EC50 = 20.9 nM Funct
Stimulation of [35S]GTP-gamma-S binding to human recombinant DORStimulation of [35S]GTP-gamma-S binding to human recombinant DOR
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
CHEMBL4750006 oprd_human Human No 6.7 EC50 = 200 nM Funct
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
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
CHEMBL564922 oprd_human Human No 6.7 EC50 = 200 nM Funct
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
374 2 1 3 3.9 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1CCCC1
CHEMBL495278 oprd_human Human No 6.7 EC50 = 200 nM Funct
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
302 1 1 3 3.5 N#Cc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL3426788 oprd_human Human Yes 6.7 EC50 = 200 nM Bind
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
456 4 0 4 6.7 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccccc2)cc1
CHEMBL3426790 oprd_human Human Yes 6.7 EC50 = 200 nM Bind
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
470 4 0 4 7.0 Cc1cccc(COc2ccc(C3C4=C(CC(C)(C)CC4=O)OC4=C3C(=O)CC(C)(C)C4)cc2)c1
CHEMBL3426798 oprd_human Human No 6.7 EC50 = 200 nM Bind
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assayPositive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
522 6 0 5 7.3 CC1(C)CC(=O)C2=C(C1)OC1=C(C(=O)CC(C)(C)C1)C2c1ccc(OCc2ccccc2OC(F)F)cc1
CHEMBL290440 oprd_rat Rat No 6.7 EC50 = 200 nM Bind
The binding affinity was evaluated against [3H]dalamid binding to neuroblastoma X glioma hybrid cell NG108-15 (Opioid receptor delta 1)membranesThe binding affinity was evaluated against [3H]dalamid binding to neuroblastoma X glioma hybrid cell NG108-15 (Opioid receptor delta 1)membranes
486 11 1 5 4.7 CCOc1ccc(Cc2nc3cc(NC(=O)CBr)ccc3n2CCN(CC)CC)cc1
CHEMBL291099 oprd_rat Rat No 6.7 EC50 = 200 nM Bind
The binding affinity was evaluated against [3H]dalamid binding to neuroblastoma X glioma hybrid cell NG108-15 (Opioid receptor delta 1)membranesThe binding affinity was evaluated against [3H]dalamid binding to neuroblastoma X glioma hybrid cell NG108-15 (Opioid receptor delta 1)membranes
471 8 1 3 4.5 CCC(=O)N(c1ccccc1)C1CCN(CCc2ccc(NC(=O)CBr)cc2)CC1
CHEMBL1449023 oprd_human Human Yes 5.7 EC50 = 2000 nM Funct
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
368 5 1 4 4.0 O=C(Nc1nc2ccccc2n1CCN1CCCC1)c1ccc(Cl)cc1
CHEMBL1698841 oprd_human Human Yes 4.7 EC50 = 20454 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
334 5 2 3 3.7 CN(C)C(CN=C(S)Nc1cccc(Cl)c1)c1cccnc1
CHEMBL523358 oprd_human Human Yes 6.7 EC50 = 207 nM Funct
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
310 3 1 4 2.7 CC(=O)N(c1ccccc1)C1CCN(c2cc(N)ccn2)CC1
CHEMBL375359 oprd_human Human No 7.7 EC50 = 21 nM Funct
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
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
CHEMBL31421 oprd_human Human Yes 7.7 EC50 = 21 nM Funct
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
None None None None
CHEMBL19019 oprd_human Human Yes 7.7 EC50 = 21 nM Funct
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
341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O
CHEMBL557121 oprd_human Human No 7.7 EC50 = 21 nM Funct
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
378 4 1 3 4.2 CCN(CC)C(=O)c1ccc(C2CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL238017 oprd_human Human No 7.7 EC50 = 21 nM Funct
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
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
CHEMBL2371977 oprd_human Human No 7.7 EC50 = 21 nM Funct
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
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
CHEMBL13403 oprd_human Human No 7.7 EC50 = 21 nM Funct
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
391 8 0 3 5.0 C=CCN1CCC(N(c2ccccc2)c2ccc(C(=O)N(CC)CC)cc2)CC1
CHEMBL4451186 oprd_rat Rat No 7.7 EC50 = 21.1 nM Funct
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
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
CHEMBL110461 oprd_human Human No 7.7 EC50 = 21.8 nM Funct
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
488 3 2 3 6.3 CN1CC[C@]23c4c5ccc(O)c4O[C@@]2(C)c2[nH]c4ccccc4c2C[C@@]3(C/C=C/c2ccccc2)C1C5
CHEMBL13470 oprd_human Human Yes 6.7 EC50 = 210 nM Funct
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
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
CHEMBL392269 oprd_human Human No 6.7 EC50 = 210 nM Funct
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
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
CHEMBL143592 oprd_mouse Mouse No 6.7 EC50 = 210 nM Funct
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
414 5 1 3 5.6 CC(C)(C)c1ccc(C(c2cccc(O)c2)N2CCN(Cc3ccccc3)CC2)cc1
CHEMBL124642 oprd_human Human No 6.7 EC50 = 211 nM Bind
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
365 6 0 3 3.5 CCN(CC)C(=O)c1ccc(C(c2ccccc2)N2CCN(C)CC2)cc1
CHEMBL555571 oprd_human Human No 6.7 EC50 = 211 nM Bind
Agonist potency was measured using GTP gamma-[35S] binding assayAgonist potency was measured using GTP gamma-[35S] binding assay
365 6 0 3 3.5 CCN(CC)C(=O)c1ccc(C(c2ccccc2)N2CCN(C)CC2)cc1
CHEMBL107207 oprd_human Human No 6.7 EC50 = 211 nM Funct
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
440 1 2 3 5.4 COc1ccc2c(c1O)[C@]13CCN(C)C(C2)[C@@]12CC(=C(C)C)[C@@H]3c1[nH]c3ccccc3c1C2
CHEMBL4106544 oprd_human Human No 6.7 EC50 = 211.4 nM Funct
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.
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
CHEMBL4746919 oprd_human Human No 6.7 EC50 = 218 nM Funct
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
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
CHEMBL65772 oprd_human Human No 6.7 EC50 = 218 nM Funct
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
508 9 0 3 6.8 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCc2ccccc2)c2cccc(OC)c2)cc1
CHEMBL4746919 oprd_human Human No 6.7 EC50 = 218.8 nM Funct
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
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
CHEMBL4761246 oprd_human Human No 6.7 EC50 = 218.8 nM Funct
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
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
CHEMBL4761246 oprd_human Human No 6.7 EC50 = 219 nM Funct
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
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
CHEMBL518950 oprd_human Human No 5.7 EC50 = 2190 nM Funct
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
422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1
CHEMBL427214 oprd_mouse Mouse No 7.7 EC50 = 22 nM Funct
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
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
CHEMBL427214 oprd_human Human No 7.7 EC50 = 22 nM Funct
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
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
CHEMBL3759294 oprd_rat Rat No 7.7 EC50 = 22 nM Funct
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
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
CHEMBL3759831 oprd_rat Rat No 7.7 EC50 = 22 nM Funct
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
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
CHEMBL4111717 oprd_human Human No 7.7 EC50 = 22 nM Funct
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.
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
CHEMBL4111224 oprd_human Human No 7.7 EC50 = 22.3 nM Funct
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.
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
CHEMBL4749747 oprd_human Human No 7.7 EC50 = 22.4 nM Bind
Agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
1450 52 13 18 4.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCSC)NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(N)=O)C1=O
CHEMBL206974 oprd_human Human No 7.6 EC50 = 22.9 nM Funct
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
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
CHEMBL494266 oprd_human Human No 6.7 EC50 = 220 nM Funct
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
321 2 2 3 3.3 O=C(O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL495074 oprd_human Human No 6.7 EC50 = 220 nM Funct
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
293 1 2 3 3.3 Oc1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1
CHEMBL3596365 oprd_human Human No 6.7 EC50 = 220 nM Funct
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
406 2 3 4 3.1 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314
CHEMBL3598301 oprd_human Human No 6.7 EC50 = 220 nM Funct
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
406 2 3 4 3.1 Oc1ccc2c3c1O[C@H]1c4[nH]c5ccccc5c4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314
CHEMBL134652 oprd_mouse Mouse No 5.7 EC50 = 2200 nM Funct
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
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
CHEMBL320306 oprd_human Human No 6.7 EC50 = 221 nM Funct
Agonistic activity towards Opioid receptor delta 1Agonistic activity towards Opioid receptor delta 1
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
CHEMBL4102093 oprd_human Human No 5.7 EC50 = 2238.7 nM Bind
Agonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to beta-arrestin-2 assessed as increase in DOR/beta-arrestin-2 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assayAgonist activity at Rluc-tagged DOR receptor (unknown origin) expressed in human SH-5YSY cells co-expressing RGFP-fused to beta-arrestin-2 assessed as increase in DOR/beta-arrestin-2 protein interaction incubated for 5 mins in presence of coelenterazine by BRET assay
351 4 1 3 4.3 COC(CN1CC[C@@]2(C)c3cc(O)ccc3C[C@@H]1[C@@H]2C)c1ccccc1
CHEMBL4449491 oprd_human Human No 5.7 EC50 = 2240 nM Funct
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
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
CHEMBL4742666 oprd_human Human No 6.6 EC50 = 227 nM Funct
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
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
CHEMBL67734 oprd_human Human No 6.6 EC50 = 228 nM Funct
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
484 8 0 2 7.6 CCN(CC)C(=O)c1ccc(C(=C2CC3CCC(C2)N3CCC2CCCCC2)c2ccccc2)cc1
CHEMBL4112472 oprd_human Human No 6.6 EC50 = 229.3 nM Funct
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.
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
CHEMBL206974 oprd_human Human No 7.6 EC50 = 23 nM Funct
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
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
CHEMBL3409762 oprd_human Human No 7.6 EC50 = 23 nM Bind
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology measured over 30 mins by label free binding assayAgonist activity at delta opioid receptor (unknown origin) expressed in CHO cells assessed as change in cell morphology measured over 30 mins by label free binding assay
691 13 6 7 2.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCc2ccccc2C1C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
CHEMBL375503 oprd_human Human No 7.6 EC50 = 23 nM Funct
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
412 3 1 2 5.3 COc1ccc2c(c1)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1Cc1c([nH]c2ccccc12)C3
CHEMBL129693 oprd_human Human No 7.6 EC50 = 23.4 nM Funct
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.
394 6 1 3 5.1 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(SC)cc2)cc1
CHEMBL2113670 oprd_human Human No 7.6 EC50 = 23.6 nM Bind
EC50 for binding of [35S]- GTPdeltaS in cloned human oOpioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human oOpioid receptor delta 1 (Cl-DPDPE) transfected onto CHO cells
397 4 1 5 3.0 CCO[C@H](C)[C@@H]1C[C@@]23C=C[C@]1(OC)[C@H]1Oc4c(O)ccc5c4C12CCN(C)[C@@H]3C5
CHEMBL4108066 oprd_human Human No 6.6 EC50 = 231.3 nM Funct
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.
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
CHEMBL2375656 oprd_human Human No 6.6 EC50 = 239 nM Funct
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
348 1 1 6 3.0 COc1cc(O)c2c(c1)CC(=O)CCCC(=O)CCC[C@@H](C)OC2=O
CHEMBL493743 oprd_human Human No 7.6 EC50 = 24 nM Funct
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
437 4 1 6 2.5 CCOC(=O)N1CCN(C(=O)C2(c3ccccc3)CCN(c3cc(N)ccn3)CC2)CC1
CHEMBL246572 oprd_human Human No 7.6 EC50 = 24 nM Funct
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
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
CHEMBL3609621 oprd_human Human No 7.6 EC50 = 24 nM Funct
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
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
CHEMBL112656 oprd_human Human No 7.6 EC50 = 24 nM Funct
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
413 1 2 6 2.8 CN1CCC23c4c5ccc(O)c4OC2c2nc(-c4ccccc4)ncc2CC3(O)C1C5
CHEMBL4777389 oprd_human Human No 7.6 EC50 = 24.3 nM Bind
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
388 4 3 6 1.3 CO[C@@]12CC[C@H](N[C@H](C)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5
CHEMBL3596370 oprd_human Human No 7.6 EC50 = 24.7 nM Funct
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
418 2 2 5 3.2 Oc1ccc2c3c1O[C@H]1c4nc5ccccc5cc4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314
CHEMBL3598212 oprd_human Human No 7.6 EC50 = 24.7 nM Funct
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
418 2 2 5 3.2 Oc1ccc2c3c1O[C@H]1c4nc5ccccc5cc4C[C@@]4(O)[C@@H](C2)N(CCF)CC[C@]314
CHEMBL551414 oprd_human Human No 6.6 EC50 = 240 nM Funct
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
390 2 1 4 3.1 O=C(c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1)N1CCOCC1
CHEMBL289488 oprd_rat Rat No 6.6 EC50 = 240 nM Bind
The binding affinity was evaluated against [3H]dalamid binding to neuroblastoma X glioma hybrid cell NG108-15 (Opioid receptor delta 1)membranesThe binding affinity was evaluated against [3H]dalamid binding to neuroblastoma X glioma hybrid cell NG108-15 (Opioid receptor delta 1)membranes
478 12 1 7 4.0 CCOc1ccc(Cc2nc3cc(NC(=O)/C=C/C(=O)OC)ccc3n2CCN(CC)CC)cc1
CHEMBL4130069 oprd_human Human No 6.6 EC50 = 245 nM Funct
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
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
CHEMBL4130069 oprd_human Human No 6.6 EC50 = 245.5 nM Funct
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
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
CHEMBL4749016 oprd_human Human No 6.6 EC50 = 248 nM Funct
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
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
CHEMBL3609615 oprd_human Human No 7.6 EC50 = 25 nM Funct
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
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
CHEMBL3824042 oprd_rat Rat No 7.6 EC50 = 25 nM Funct
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
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
CHEMBL361274 oprd_human Human No 7.6 EC50 = 25 nM Funct
Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranesInhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
438 5 3 4 4.0 N[C@@H](Cc1ccc(O)cc1)C(=O)N1Cc2ccccc2C[C@H]1c1nc(-c2ccccc2)c[nH]1
CHEMBL112035 oprd_human Human No 7.6 EC50 = 25.0 nM Funct
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
325 0 3 5 1.0 CN1CCC23c4c5ccc(O)c4OC2c2n[nH]cc2CC3(O)C1C5
CHEMBL374325 oprd_human Human No 7.6 EC50 = 25.1 nM Funct
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
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
CHEMBL3309506 oprd_human Human No 7.6 EC50 = 25.5 nM Funct
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
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
CHEMBL127007 oprd_human Human No 7.6 EC50 = 25.5 nM Funct
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.
382 5 1 2 5.0 CCN(CC)C(=O)c1ccc(C(=C2CCNCC2)c2ccc(Cl)cc2)cc1
CHEMBL571324 oprd_human Human No 7.6 EC50 = 25.6 nM Funct
Agonist activity at human delta opioid receptor by [35S]GTPgammaS binding assayAgonist activity at human delta opioid receptor by [35S]GTPgammaS binding assay
381 6 1 4 4.1 CCN(CC)C(=O)c1ccc(N(c2cccc(O)c2)C2CCN(C)CC2)cc1
CHEMBL1649945 oprd_human Human No 7.6 EC50 = 25.7 nM Funct
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
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
CHEMBL4641588 oprd_human Human No 6.6 EC50 = 250 nM Funct
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
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
CHEMBL4650776 oprd_human Human No 6.6 EC50 = 250 nM Funct
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
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
CHEMBL2418743 oprd_human Human No 5.6 EC50 = 2500 nM Funct
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
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
CHEMBL4078283 oprd_rat Rat No 6.6 EC50 = 253 nM Funct
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
349 4 2 3 4.0 Oc1cccc([C@@]23CCC[C@@H]([C@@H]2O)N(C/C=C/c2ccccc2)CC3)c1
CHEMBL4116647 oprd_rat Rat No 6.6 EC50 = 253 nM Funct
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
349 4 2 3 4.0 Oc1cccc([C@@]23CCC[C@@H]([C@@H]2O)N(C/C=C/c2ccccc2)CC3)c1
CHEMBL190785 oprd_human Human No 5.6 EC50 = 2530 nM Funct
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
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
CHEMBL1717557 oprd_human Human Yes 4.6 EC50 = 25596 nM Funct
PUBCHEM_BIOASSAY: Counterscreen for agonists of heterodimerization of the mu 1 (OPRM1) and delta 1 (OPRD1) opioid receptors: Luminescence-based cell-based high 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]
332 8 1 4 3.1 COc1ccc(C(CNC(=O)CCc2ccsc2)N(C)C)cc1
CHEMBL1649945 oprd_human Human No 7.6 EC50 = 26 nM Funct
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
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
CHEMBL557458 oprd_human Human No 7.6 EC50 = 26 nM Funct
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
392 4 2 4 3.8 CCN(CC)C(=O)c1ccc(C2=CC3(CCNCC3)Oc3ccccc32)cc1O
CHEMBL200940 oprd_human Human No 7.6 EC50 = 26 nM Funct
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
450 5 0 5 6.1 c1ccc(Cn2ccnc2C2(c3ccccc3)CCN(c3nc4ccccc4s3)CC2)cc1
CHEMBL374325 oprd_human Human No 7.6 EC50 = 26 nM Funct
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
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
CHEMBL273820 oprd_human Human No 7.6 EC50 = 26.3 nM Bind
Agonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at DOP (unknown origin) expressed in SH-SY5Y cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
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(=O)O
CHEMBL4128945 oprd_rat Rat No 7.6 EC50 = 26.8 nM Funct
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 asses