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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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GPCRdb ID #Vendors UniProt IUPHAR Species p-value
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Assay Type Assay Description Source Mol
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H don H acc LogP Smiles DOI
13544016 3660 0 OPRM μ receptor Rat - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 328 3 0 2 3.9 CN([C@@H]1CCCC[C@H]1N(C(=O)c1ccc(c(c1)Cl)Cl)C)C 2999404
9282 3660 0 OPRM μ receptor Rat - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 328 3 0 2 3.9 CN([C@@H]1CCCC[C@H]1N(C(=O)c1ccc(c(c1)Cl)Cl)C)C 2999404
CHEMBL277572 3660 0 OPRM μ receptor Rat - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 328 3 0 2 3.9 CN([C@@H]1CCCC[C@H]1N(C(=O)c1ccc(c(c1)Cl)Cl)C)C 2999404
145953986 160534 0 OPRM μ receptor Rat 10.9 pEC50 = 10.9 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 484 11 6 6 0.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
CHEMBL4126050 160534 0 OPRM μ receptor Rat 10.9 pEC50 = 10.9 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 484 11 6 6 0.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1016/j.bmcl.2018.05.015
145961883 160540 0 OPRM μ receptor Rat 10.9 pEC50 = 10.9 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 594 16 9 7 -0.4 C=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4126102 160540 0 OPRM μ receptor Rat 10.9 pEC50 = 10.9 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 594 16 9 7 -0.4 C=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
155567284 175125 0 OPRM μ receptor Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 410 7 1 5 3.4 CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CCc2cccc(O)c2)CC1 10.1021/acsmedchemlett.9b00404
CHEMBL4588535 175125 0 OPRM μ receptor Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 410 7 1 5 3.4 CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CCc2cccc(O)c2)CC1 10.1021/acsmedchemlett.9b00404
CHEMBL4798954 182574 0 OPRM μ receptor Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL 337 4 2 3 3.5 Oc1cccc([C@@]23CCC[C@H]([C@H]2O)N(CCc2ccccc2)CC3)c1 10.1039/d0md00104j
155564874 174680 0 OPRM μ receptor Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 410 7 1 5 3.4 CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CCc2ccc(O)cc2)CC1 10.1021/acsmedchemlett.9b00404
CHEMBL4578287 174680 0 OPRM μ receptor Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 410 7 1 5 3.4 CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CCc2ccc(O)cc2)CC1 10.1021/acsmedchemlett.9b00404
60168107 81064 0 OPRM μ receptor Human 10.5 pEC50 = 10.5 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 612 12 6 7 2.0 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1 10.1021/jm300664y
CHEMBL2163916 81064 0 OPRM μ receptor Human 10.5 pEC50 = 10.5 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 612 12 6 7 2.0 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccco1 10.1021/jm300664y
60170775 81065 0 OPRM μ receptor Human 10.5 pEC50 = 10.5 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 612 12 6 7 2.0 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccoc1 10.1021/jm300664y
CHEMBL2163917 81065 0 OPRM μ receptor Human 10.5 pEC50 = 10.5 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 612 12 6 7 2.0 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccoc1 10.1021/jm300664y
71605418 86829 0 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at FLAG-tagged mu-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 FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
ChEMBL 622 12 6 6 2.2 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccccc1 10.1021/jm400195y
CHEMBL2334770 86829 0 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Agonist activity at FLAG-tagged mu-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 FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
ChEMBL 622 12 6 6 2.2 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccccc1 10.1021/jm400195y
3668 1457 30 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None None 10.1021/jm060998u
5311081 1457 30 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None None 10.1021/jm060998u
CHEMBL333357 1457 30 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None None 10.1021/jm060998u
CHEMBL589982 1457 30 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None None 10.1021/jm060998u
145961816 160786 0 OPRM μ receptor Rat 10.4 pEC50 = 10.4 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 650 16 9 8 0.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1-c1ccsc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4129689 160786 0 OPRM μ receptor Rat 10.4 pEC50 = 10.4 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 650 16 9 8 0.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1-c1ccsc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
3668 1457 30 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assayAntagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay
ChEMBL None None None None 10.1016/j.bmcl.2008.01.009
5311081 1457 30 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assayAntagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay
ChEMBL None None None None 10.1016/j.bmcl.2008.01.009
CHEMBL333357 1457 30 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assayAntagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay
ChEMBL None None None None 10.1016/j.bmcl.2008.01.009
CHEMBL589982 1457 30 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Antagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assayAntagonist activity at mu opioid receptor expressed in CHO cells assessed as release of intracellular calcium ions by aequorin luminescence-based calcium assay
ChEMBL None None None None 10.1016/j.bmcl.2008.01.009
71456262 78811 0 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 448 3 1 4 3.5 CN1CC[C@]23c4c5cccc4O[C@H]2C(=O)CC[C@@]3(NC(=O)/C=C/c2ccccc2Cl)[C@H]1C5 10.1021/jm0604777
CHEMBL2113666 78811 0 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 448 3 1 4 3.5 CN1CC[C@]23c4c5cccc4O[C@H]2C(=O)CC[C@@]3(NC(=O)/C=C/c2ccccc2Cl)[C@H]1C5 10.1021/jm0604777
11849285 195434 0 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 444 3 2 5 2.9 Cc1ccccc1/C=C/C(=O)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/jm0604777
CHEMBL607125 195434 0 OPRM μ receptor Human 10.4 pEC50 = 10.4 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 444 3 2 5 2.9 Cc1ccccc1/C=C/C(=O)N[C@@]12CCC(=O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/jm0604777
71605420 86827 0 OPRM μ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at FLAG-tagged mu-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 FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
ChEMBL 622 12 6 6 2.2 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccccc1 10.1021/jm400195y
CHEMBL2334768 86827 0 OPRM μ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at FLAG-tagged mu-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 FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
ChEMBL 622 12 6 6 2.2 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccccc1 10.1021/jm400195y
50994602 56707 0 OPRM μ receptor Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 820 13 4 7 4.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649948 56707 0 OPRM μ receptor Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 820 13 4 7 4.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
50994602 56707 0 OPRM μ receptor Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 820 13 4 7 4.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649948 56707 0 OPRM μ receptor Rat 10.2 pEC50 = 10.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 820 13 4 7 4.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
122194218 123202 0 OPRM μ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 628 12 6 7 2.4 C=C(C(N)=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1cccs1 10.1016/j.bmcl.2015.09.025
CHEMBL3629337 123202 0 OPRM μ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 628 12 6 7 2.4 C=C(C(N)=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1cccs1 10.1016/j.bmcl.2015.09.025
122194219 123110 0 OPRM μ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 628 12 6 7 2.4 C=C(C(N)=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccsc1 10.1016/j.bmcl.2015.09.025
CHEMBL3627737 123110 0 OPRM μ receptor Human 10.2 pEC50 = 10.2 Functional
Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 628 12 6 7 2.4 C=C(C(N)=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccsc1 10.1016/j.bmcl.2015.09.025
CHEMBL2151734 202813 0 OPRM μ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N(C)[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)CC(N)=O 10.1021/jm200894e
54757387 65100 0 OPRM μ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
ChEMBL 495 8 5 6 -0.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/jm200894e
CHEMBL1834247 65100 0 OPRM μ receptor Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation countingAgonist activity at human MOR expressed in HEK293 cell membrane assessed as inhibition of forskolin-induced cAMP accumulation by by liquid scintillation counting
ChEMBL 495 8 5 6 -0.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@H]1Cc2ccccc2CN(CC(N)=O)C1=O 10.1021/jm200894e
25232542 184944 0 OPRM μ receptor Human 10.1 pEC50 = 10.1 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 497 4 3 6 3.3 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2n1 10.1021/jm801272c
CHEMBL494853 184944 0 OPRM μ receptor Human 10.1 pEC50 = 10.1 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 497 4 3 6 3.3 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2n1 10.1021/jm801272c
71605421 86828 0 OPRM μ receptor Human 10.0 pEC50 = 10.0 Functional
Agonist activity at FLAG-tagged mu-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 FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
ChEMBL 612 12 6 7 1.8 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccco1 10.1021/jm400195y
CHEMBL2334769 86828 0 OPRM μ receptor Human 10.0 pEC50 = 10.0 Functional
Agonist activity at FLAG-tagged mu-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 FLAG-tagged mu-type opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by liquid scintillation counting analysis
ChEMBL 612 12 6 7 1.8 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCN(C(=O)[C@@H](N)Cc2ccc(O)cc2)C1)c1ccco1 10.1021/jm400195y
71625280 87219 0 OPRM μ receptor Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 6 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338726 87219 0 OPRM μ receptor Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 6 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
118731120 117428 0 OPRM μ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 594 13 8 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O 10.1021/acs.jmedchem.8b01282
CHEMBL3408737 117428 0 OPRM μ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 594 13 8 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O 10.1021/acs.jmedchem.8b01282
53233475 165994 0 OPRM μ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 630 17 7 7 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01282
CHEMBL4284813 165994 0 OPRM μ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 630 17 7 7 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01282
CHEMBL331325 204876 1 OPRM μ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01282
CHEMBL412923 206546 0 OPRM μ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01282
118731120 117428 0 OPRM μ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human MOR 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 MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay
ChEMBL 594 13 8 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O 10.1021/acs.jmedchem.0c01376
CHEMBL3408737 117428 0 OPRM μ receptor Human 10.0 pEC50 = 10 Functional
Agonist activity at human MOR 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 MOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay
ChEMBL 594 13 8 7 -0.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(N)=O)C1=O 10.1021/acs.jmedchem.0c01376
145961895 160558 0 OPRM μ receptor Rat 10.0 pEC50 = 10 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 622 16 9 7 0.4 CC(C)=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4126322 160558 0 OPRM μ receptor Rat 10.0 pEC50 = 10 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 622 16 9 7 0.4 CC(C)=Cc1ccccc1C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
9848990 186324 1 OPRM μ receptor Human 10.0 pEC50 = 10.0 Functional
Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1016/j.bmcl.2008.10.134
CHEMBL2368861 186324 1 OPRM μ receptor Human 10.0 pEC50 = 10.0 Functional
Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1016/j.bmcl.2008.10.134
CHEMBL511142 186324 1 OPRM μ receptor Human 10.0 pEC50 = 10.0 Functional
Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1016/j.bmcl.2008.10.134
50994380 56697 0 OPRM μ receptor Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 740 17 5 7 3.8 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649938 56697 0 OPRM μ receptor Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 740 17 5 7 3.8 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
50994380 56697 0 OPRM μ receptor Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 740 17 5 7 3.8 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649938 56697 0 OPRM μ receptor Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 740 17 5 7 3.8 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
155545412 175738 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 562 7 3 6 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(CN3CCc4ccccc4C3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4548498 175738 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 562 7 3 6 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(CN3CCc4ccccc4C3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597549 175738 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 562 7 3 6 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(CN3CCc4ccccc4C3)cc21 10.1021/acs.jmedchem.9b00378
145961040 160570 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 559 12 6 6 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1-c1ccccc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4126470 160570 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 559 12 6 6 1.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1-c1ccccc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
145961135 160743 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 636 15 9 7 -0.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(C(F)(F)F)cc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
CHEMBL4128945 160743 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL 636 15 9 7 -0.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(C(F)(F)F)cc1)C(=O)NCC(N)=O 10.1016/j.bmcl.2018.05.015
71625279 87218 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 5 2 5 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338725 87218 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 5 2 5 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
137657725 158788 0 OPRM μ receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 377 3 1 4 3.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2CCC[C@@]3(OCc2ccccc2)[C@H]1C5 10.1021/acs.jmedchem.7b01363
CHEMBL4103328 158788 0 OPRM μ receptor Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 377 3 1 4 3.8 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2CCC[C@@]3(OCc2ccccc2)[C@H]1C5 10.1021/acs.jmedchem.7b01363
123924 3413 31 OPRM μ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
1611 3413 31 OPRM μ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
CHEMBL13470 3413 31 OPRM μ receptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 449 9 0 4 4.8 C=CCN1C[C@H](C)N(C[C@H]1C)[C@@H](c1cccc(c1)OC)c1ccc(cc1)C(=O)N(CC)CC 10.1021/ml400491k
50994459 56700 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 774 17 5 7 4.5 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649941 56700 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 774 17 5 7 4.5 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
50994459 56700 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 774 17 5 7 4.5 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649941 56700 0 OPRM μ receptor Rat 9.9 pEC50 = 9.9 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 774 17 5 7 4.5 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
58443234 83522 0 OPRM μ receptor Human 9.8 pEC50 = 9.8 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 522 7 1 4 6.0 CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc6c(c5)OCO6)cc4)cc3C1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
CHEMBL2208351 83522 0 OPRM μ receptor Human 9.8 pEC50 = 9.8 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 522 7 1 4 6.0 CC1C2Cc3ccc(C(=O)NCCc4ccc(-c5ccc6c(c5)OCO6)cc4)cc3C1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
CHEMBL4792012 182009 0 OPRM μ receptor Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 579 9 5 8 2.3 CO[C@@]12CC[C@@H](N[C@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
1639 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.07.043
1765 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.07.043
5360515 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.07.043
CHEMBL19019 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.07.043
DB00704 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.07.043
60170609 81070 0 OPRM μ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 622 12 6 6 2.4 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1 10.1021/jm300664y
CHEMBL2163921 81070 0 OPRM μ receptor Human 9.8 pEC50 = 9.8 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 622 12 6 6 2.4 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1 10.1021/jm300664y
71625152 87214 0 OPRM μ receptor Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 467 7 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338721 87214 0 OPRM μ receptor Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 467 7 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
71625277 87216 0 OPRM μ receptor Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 6 2 5 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338723 87216 0 OPRM μ receptor Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 6 2 5 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
71625278 87217 0 OPRM μ receptor Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 7 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338724 87217 0 OPRM μ receptor Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 7 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
1639 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
1765 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
5360515 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
CHEMBL19019 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
DB00704 2563 39 OPRM μ receptor Mouse 9.8 pEC50 = 9.8 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmc.2015.02.055
25259490 173055 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 517 6 3 7 3.1 O=C(/C=C/c1cccc([N+](=O)[O-])c1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm8015552
CHEMBL454018 173055 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 517 6 3 7 3.1 O=C(/C=C/c1cccc([N+](=O)[O-])c1)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm8015552
44323614 167173 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor.Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor.
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NC1CCNc2ccc(Cc3ccccc3)cc21 10.1016/s0960-894x(98)00472-7
CHEMBL432045 167173 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor.Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor.
ChEMBL 429 6 4 4 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NC1CCNc2ccc(Cc3ccccc3)cc21 10.1016/s0960-894x(98)00472-7
145984911 165572 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 658 17 9 7 0.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01282
CHEMBL4276875 165572 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 658 17 9 7 0.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01282
71624447 87239 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 481 7 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338745 87239 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 481 7 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
155559128 175396 0 OPRM μ receptor Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2sccc2c1 10.1021/acs.jmedchem.9b01767
CHEMBL4562210 175396 0 OPRM μ receptor Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2sccc2c1 10.1021/acs.jmedchem.9b01767
CHEMBL4594861 175396 0 OPRM μ receptor Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2sccc2c1 10.1021/acs.jmedchem.9b01767
155548948 173380 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 408 7 0 5 3.3 CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CC(=O)c2ccccc2)CC1 10.1021/acsmedchemlett.9b00404
CHEMBL4548662 173380 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 408 7 0 5 3.3 CCC(=O)N(c1ccccc1)C1(C(=O)OC)CCN(CC(=O)c2ccccc2)CC1 10.1021/acsmedchemlett.9b00404
118562375 168753 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 392 5 0 3 4.2 CC(C)C1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O 10.1021/acs.jmedchem.9b01256
CHEMBL4436170 168753 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 392 5 0 3 4.2 CC(C)C1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O 10.1021/acs.jmedchem.9b01256
CHEMBL3326228 119798 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545629 119798 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL2387215 203919 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)NCCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)O 10.1016/j.bmcl.2013.03.065
71625281 87220 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 507 7 2 5 5.3 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338727 87220 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 507 7 2 5 5.3 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CCC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
155517331 175397 0 OPRM μ receptor Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccsc2c1 10.1021/acs.jmedchem.9b01767
CHEMBL4444746 175397 0 OPRM μ receptor Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccsc2c1 10.1021/acs.jmedchem.9b01767
CHEMBL4594862 175397 0 OPRM μ receptor Mouse 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccsc2c1 10.1021/acs.jmedchem.9b01767
122179053 120627 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581743 120627 0 OPRM μ receptor Rat 9.7 pEC50 = 9.7 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
24873473 83528 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 508 8 1 3 6.3 COc1cccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)c1 10.1016/j.bmcl.2012.10.081
CHEMBL2208358 83528 0 OPRM μ receptor Human 9.7 pEC50 = 9.7 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 508 8 1 3 6.3 COc1cccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)c1 10.1016/j.bmcl.2012.10.081
155542413 175445 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 507 7 3 5 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4521319 175445 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 507 7 3 5 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4595172 175445 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 507 7 3 5 3.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccccc3)cc21 10.1021/acs.jmedchem.9b00378
155567469 175708 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 557 7 3 5 4.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4588807 175708 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 557 7 3 5 4.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597299 175708 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 557 7 3 5 4.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
71625394 87221 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 487 6 2 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338728 87221 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 487 6 2 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL4747769 179186 0 OPRM μ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL 421 8 1 4 5.1 CCOC(=O)CC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
71583725 86178 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 469 6 4 4 4.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3Cc4ccccc4C3)cc21 10.1021/jm400050y
CHEMBL2322563 86178 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 469 6 4 4 4.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3Cc4ccccc4C3)cc21 10.1021/jm400050y
71230156 120626 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581742 120626 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
71583725 86178 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 469 6 4 4 4.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3Cc4ccccc4C3)cc21 10.1021/acs.jmedchem.5b01270
CHEMBL2322563 86178 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 469 6 4 4 4.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CC3Cc4ccccc4C3)cc21 10.1021/acs.jmedchem.5b01270
118709689 112748 0 OPRM μ receptor Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2s1 10.1021/acs.jmedchem.9b01767
CHEMBL3319616 112748 0 OPRM μ receptor Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2s1 10.1021/acs.jmedchem.9b01767
CHEMBL4458688 112748 0 OPRM μ receptor Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2s1 10.1021/acs.jmedchem.9b01767
71449133 78492 0 OPRM μ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 500 5 2 5 4.0 CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1021/jm070255o
CHEMBL2113304 78492 0 OPRM μ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 500 5 2 5 4.0 CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1021/jm070255o
155535194 175465 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 558 7 3 6 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4471560 175465 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 558 7 3 6 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4595286 175465 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 558 7 3 6 4.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
1647 1232 33 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None None 10.1016/j.bmcl.2018.05.015
5462471 1232 33 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None None 10.1016/j.bmcl.2018.05.015
CHEMBL113995 1232 33 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None None 10.1016/j.bmcl.2018.05.015
CHEMBL38874 1232 33 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat mu-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 mu-opioid receptor expressed in HEK293 cells co-expressing Rluc2-EPAC-GFP10 biosenser assessed as inhibition of forskolin-induced cAMP level after 10 mins by fluorescence based assay
ChEMBL None None None None 10.1016/j.bmcl.2018.05.015
71625026 87235 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 5 2 5 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338741 87235 0 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 5 2 5 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
25233083 187650 0 OPRM μ receptor Human 9.6 pEC50 = 9.6 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 497 4 3 6 3.3 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2cn1 10.1021/jm801272c
CHEMBL521854 187650 0 OPRM μ receptor Human 9.6 pEC50 = 9.6 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 497 4 3 6 3.3 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2cn1 10.1021/jm801272c
9848990 186324 1 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2368861 186324 1 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL511142 186324 1 OPRM μ receptor Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
145992101 166204 0 OPRM μ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 787 22 11 9 -0.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/acs.jmedchem.8b01282
CHEMBL4288649 166204 0 OPRM μ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 787 22 11 9 -0.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/acs.jmedchem.8b01282
155520187 172393 0 OPRM μ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 410 8 1 5 2.7 COC(=O)C1(N(C(=O)CCO)c2ccccc2)CCN(CCc2ccccc2)CC1 10.1021/acsmedchemlett.9b00404
CHEMBL4524446 172393 0 OPRM μ receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 410 8 1 5 2.7 COC(=O)C1(N(C(=O)CCO)c2ccccc2)CCN(CCc2ccccc2)CC1 10.1021/acsmedchemlett.9b00404
50994460 56701 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 758 17 5 7 4.0 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649942 56701 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 758 17 5 7 4.0 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
71625393 87215 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 465 5 2 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338722 87215 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 465 5 2 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
50994460 56701 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 758 17 5 7 4.0 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
CHEMBL1649942 56701 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 758 17 5 7 4.0 CCCC[C@@H](NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC(N(C(=O)CC)c2ccccc2)CC1 10.1021/jm100982d
1647 1232 33 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL None None None None 10.1039/d0md00104j
5462471 1232 33 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL None None None None 10.1039/d0md00104j
CHEMBL113995 1232 33 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL None None None None 10.1039/d0md00104j
CHEMBL38874 1232 33 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL None None None None 10.1039/d0md00104j
71461666 78493 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 520 5 2 5 4.3 CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccccc1Cl)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1021/jm070255o
CHEMBL2113305 78493 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 520 5 2 5 4.3 CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccccc1Cl)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1021/jm070255o
25233081 184762 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human mu-opioid receptor expressed in HEK293 cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu-opioid receptor expressed in HEK293 cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 496 4 3 5 3.9 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2c1 10.1021/acs.jmedchem.6b01807
CHEMBL493846 184762 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human mu-opioid receptor expressed in HEK293 cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu-opioid receptor expressed in HEK293 cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 496 4 3 5 3.9 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2c1 10.1021/acs.jmedchem.6b01807
118988707 145114 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 467 4 2 5 4.3 CO[C@@H]1C([C@](C)(O)C(C)(C)C)[C@H]2CC[C@@]13Oc1c(O)ccc4c1[C@@]31CCN(CC3CC3)[C@H](C4)C21 nan
CHEMBL3917891 145114 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 467 4 2 5 4.3 CO[C@@H]1C([C@](C)(O)C(C)(C)C)[C@H]2CC[C@@]13Oc1c(O)ccc4c1[C@@]31CCN(CC3CC3)[C@H](C4)C21 nan
50925450 56702 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 732 14 5 7 3.3 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649943 56702 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 732 14 5 7 3.3 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
71625029 87209 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 487 6 2 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338717 87209 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 487 6 2 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)Cc1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
11773726 195472 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 391 3 1 5 3.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2C(=O)CC[C@@]3(OCc2ccccc2)[C@H]1C5 10.1021/acs.jmedchem.7b01363
CHEMBL607351 195472 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human MOR expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 391 3 1 5 3.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2C(=O)CC[C@@]3(OCc2ccccc2)[C@H]1C5 10.1021/acs.jmedchem.7b01363
155564088 175830 0 OPRM μ receptor Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12 10.1021/acs.jmedchem.9b01767
CHEMBL4575933 175830 0 OPRM μ receptor Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12 10.1021/acs.jmedchem.9b01767
CHEMBL4598304 175830 0 OPRM μ receptor Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12 10.1021/acs.jmedchem.9b01767
25232539 178395 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 447 4 3 6 2.2 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccnc1 10.1021/jm801272c
CHEMBL472937 178395 0 OPRM μ receptor Human 9.5 pEC50 = 9.5 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 447 4 3 6 2.2 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccnc1 10.1021/jm801272c
155527203 175446 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 6 4.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4459271 175446 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 6 4.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4595173 175446 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 6 4.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(S(C)(=O)=O)c2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
155538529 175677 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 548 7 3 5 5.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4476818 175677 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 548 7 3 5 5.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597054 175677 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 548 7 3 5 5.0 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
50925450 56702 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 732 14 5 7 3.3 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649943 56702 0 OPRM μ receptor Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 732 14 5 7 3.3 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
155524410 175615 0 OPRM μ receptor Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1csc2ccccc12 10.1021/acs.jmedchem.9b01767
CHEMBL4455793 175615 0 OPRM μ receptor Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1csc2ccccc12 10.1021/acs.jmedchem.9b01767
CHEMBL4596517 175615 0 OPRM μ receptor Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1csc2ccccc12 10.1021/acs.jmedchem.9b01767
12038832 179764 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 464 6 3 6 2.5 CO[C@@]12CC[C@H](N[C@@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4754944 179764 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 464 6 3 6 2.5 CO[C@@]12CC[C@H](N[C@@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
1639 2563 39 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] bindingAgonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.05.027
1765 2563 39 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] bindingAgonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.05.027
5360515 2563 39 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] bindingAgonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.05.027
CHEMBL19019 2563 39 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] bindingAgonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.05.027
DB00704 2563 39 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] bindingAgonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1016/j.bmcl.2013.05.027
127053153 140257 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 537 6 3 5 5.5 COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21 10.1021/acs.jmedchem.6b00308
CHEMBL3824356 140257 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 537 6 3 5 5.5 COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21 10.1021/acs.jmedchem.6b00308
118709690 112749 0 OPRM μ receptor Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2o1 10.1021/acs.jmedchem.9b01767
CHEMBL3319617 112749 0 OPRM μ receptor Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2o1 10.1021/acs.jmedchem.9b01767
CHEMBL4570108 112749 0 OPRM μ receptor Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cc2ccccc2o1 10.1021/acs.jmedchem.9b01767
86291189 149655 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 368 3 2 4 2.5 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1CCC(=O)C3 nan
CHEMBL3954177 149655 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 368 3 2 4 2.5 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@@H]1CCC(=O)C3 nan
CHEMBL4795492 182293 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 ADMET
Agonist activity at EA-fragment beta-arrestin-tagged human MOR 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 MOR expressed in human U2OS cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 60 mins by beta-galactosidase based scintillation counting method
ChEMBL 515 11 1 3 5.0 CCC(=O)N(Cc1ccccc1)C1(C(=O)NCCc2cccc(F)c2)CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.0c00901
118716009 114041 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 485 5 3 6 2.5 O=C(NCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5 10.1016/j.bmcl.2014.09.029
CHEMBL3339378 114041 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 485 5 3 6 2.5 O=C(NCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5 10.1016/j.bmcl.2014.09.029
16720749 84714 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 367 2 2 5 3.1 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm0701674
CHEMBL226217 84714 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 367 2 2 5 3.1 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm0701674
CHEMBL3086304 84714 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 367 2 2 5 3.1 Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm0701674
155532589 175779 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 484 6 4 5 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CN3CCc4ccccc4C3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4467875 175779 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 484 6 4 5 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CN3CCc4ccccc4C3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597899 175779 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 484 6 4 5 4.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CN3CCc4ccccc4C3)cc21 10.1021/acs.jmedchem.9b00378
155528038 175480 0 OPRM μ receptor Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2occc2c1 10.1021/acs.jmedchem.9b01767
CHEMBL4460495 175480 0 OPRM μ receptor Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2occc2c1 10.1021/acs.jmedchem.9b01767
CHEMBL4595439 175480 0 OPRM μ receptor Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2occc2c1 10.1021/acs.jmedchem.9b01767
134338859 175548 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 4 5.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4446945 175548 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 4 5.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4595985 175548 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 547 7 3 4 5.6 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
71624776 87225 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 481 7 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338731 87225 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 481 7 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
71624554 87243 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338749 87243 0 OPRM μ receptor Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
44427178 151584 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding
ChEMBL 416 4 1 3 5.8 O=C(Nc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3 10.1016/j.bmcl.2007.01.013
CHEMBL397035 151584 0 OPRM μ receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding
ChEMBL 416 4 1 3 5.8 O=C(Nc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CC1)CC3 10.1016/j.bmcl.2007.01.013
9848990 186324 1 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL2368861 186324 1 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL511142 186324 1 OPRM μ receptor Human 9.4 pEC50 = 9.4 Binding
μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL208479 202723 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
CHEMBL208479 202723 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Activity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cellsActivity against [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in HN9.10 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
CHEMBL4754352 179720 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL 407 7 1 4 4.7 COC(=O)CC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
155531530 175628 0 OPRM μ receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1coc2ccccc12 10.1021/acs.jmedchem.9b01767
CHEMBL4466064 175628 0 OPRM μ receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1coc2ccccc12 10.1021/acs.jmedchem.9b01767
CHEMBL4596625 175628 0 OPRM μ receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1coc2ccccc12 10.1021/acs.jmedchem.9b01767
122195960 123434 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 521 6 3 4 5.2 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cccc4ccccc34)ccc21 10.1021/acs.jmedchem.5b01270
CHEMBL3634254 123434 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 521 6 3 4 5.2 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cccc4ccccc34)ccc21 10.1021/acs.jmedchem.5b01270
71625151 87213 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 453 6 2 5 4.0 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338720 87213 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 453 6 2 5 4.0 CO[C@]12CC[C@@]3(C[C@@H]1[C@@H](O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
71454361 83518 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 494 7 2 3 6.0 C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(O)cc5)cc4)cc3[C@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
CHEMBL2208347 83518 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 494 7 2 3 6.0 C[C@H]1[C@H]2Cc3ccc(C(=O)NCCc4ccc(-c5ccc(O)cc5)cc4)cc3[C@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2012.10.081
11849361 195406 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 478 4 1 5 3.5 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5Cl)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
CHEMBL607016 195406 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 478 4 1 5 3.5 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5Cl)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
11849284 195407 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 458 4 1 5 3.2 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
CHEMBL607017 195407 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 458 4 1 5 3.2 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccccc5C)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
69272828 179788 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 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 10.1021/acs.jmedchem.8b01327
CHEMBL4755067 179788 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 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 10.1021/acs.jmedchem.8b01327
1164 1516 23 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acsmedchemlett.9b00404
1626 1516 23 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acsmedchemlett.9b00404
3345 1516 23 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acsmedchemlett.9b00404
CHEMBL596 1516 23 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acsmedchemlett.9b00404
DB00813 1516 23 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assayAgonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acsmedchemlett.9b00404
72711408 102869 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 409 3 2 5 3.5 CC(=O)Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm401290y
CHEMBL3086305 102869 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 409 3 2 5 3.5 CC(=O)Nc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm401290y
72711412 105687 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 381 3 2 5 3.6 CNc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm401290y
CHEMBL3086308 105687 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 381 3 2 5 3.6 CNc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm401290y
CHEMBL3139481 105687 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human mu opioid receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 381 3 2 5 3.6 CNc1nc2c(s1)C[C@H]1[C@H]3Cc4ccc(O)cc4[C@@]1(CCN3CC1CC1)C2 10.1021/jm401290y
155555694 175610 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 552 7 3 5 4.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(CN3CCc4ccccc4C3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4553931 175610 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 552 7 3 5 4.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(CN3CCc4ccccc4C3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4596478 175610 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 552 7 3 5 4.4 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(CN3CCc4ccccc4C3)cc21 10.1021/acs.jmedchem.9b00378
71583625 86177 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/jm400050y
CHEMBL2322562 86177 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/jm400050y
71583625 86177 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.5b01270
CHEMBL2322562 86177 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3ccc4ccccc4c3)cc21 10.1021/acs.jmedchem.5b01270
153536692 172651 0 OPRM μ receptor Mouse 9.3 pEC50 = 9.3 Functional
Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins
ChEMBL 492 5 3 8 2.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1[N+](=O)[O-] 10.1021/acs.jmedchem.8b01158
CHEMBL4530500 172651 0 OPRM μ receptor Mouse 9.3 pEC50 = 9.3 Functional
Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins
ChEMBL 492 5 3 8 2.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1[N+](=O)[O-] 10.1021/acs.jmedchem.8b01158
86582596 149037 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 366 3 2 3 3.5 C=C1CC[C@H]2[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC2CCC2)C1 nan
CHEMBL3948892 149037 0 OPRM μ receptor Human 9.3 pEC50 = 9.3 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 366 3 2 3 3.5 C=C1CC[C@H]2[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC2CCC2)C1 nan
122195962 123436 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 511 6 3 4 4.5 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3Cc4ccccc4C3)ccc21 10.1021/acs.jmedchem.5b01270
CHEMBL3634256 123436 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 511 6 3 4 4.5 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3Cc4ccccc4C3)ccc21 10.1021/acs.jmedchem.5b01270
71625027 87236 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 6 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338742 87236 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 6 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
71624552 87241 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 6 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338747 87241 0 OPRM μ receptor Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 493 6 2 5 4.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
44177570 60710 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1219 27 10 10 6.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766204 60710 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1219 27 10 10 6.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
44177570 60710 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1219 27 10 10 6.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766204 60710 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1219 27 10 10 6.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1021/jm101023r
71625601 89892 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 888 22 7 9 3.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
CHEMBL2387341 89892 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 888 22 7 9 3.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2013.03.065
155526174 175616 0 OPRM μ receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccoc2c1 10.1021/acs.jmedchem.9b01767
CHEMBL4457013 175616 0 OPRM μ receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccoc2c1 10.1021/acs.jmedchem.9b01767
CHEMBL4596531 175616 0 OPRM μ receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccoc2c1 10.1021/acs.jmedchem.9b01767
155544776 175629 0 OPRM μ receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12 10.1021/acs.jmedchem.9b01767
CHEMBL4565323 175629 0 OPRM μ receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12 10.1021/acs.jmedchem.9b01767
CHEMBL4596626 175629 0 OPRM μ receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12 10.1021/acs.jmedchem.9b01767
1639 2563 39 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
1765 2563 39 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
5360515 2563 39 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
CHEMBL19019 2563 39 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
DB00704 2563 39 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Effective concentration agonistic activity towards Opioid receptor mu 1Effective concentration agonistic activity towards Opioid receptor mu 1
ChEMBL 341 2 2 5 1.5 O=C1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O 10.1021/jm030801n
1647 1232 33 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human mu 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 mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01235
5462471 1232 33 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human mu 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 mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01235
CHEMBL113995 1232 33 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human mu 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 mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01235
CHEMBL38874 1232 33 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human mu 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 mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01235
25256965 178329 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 512 8 2 5 4.4 C=CCO[C@@]12CC[C@@H](NC(=O)/C=C/c3ccccc3)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5 10.1021/jm8015552
CHEMBL472410 178329 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 512 8 2 5 4.4 C=CCO[C@@]12CC[C@@H](NC(=O)/C=C/c3ccccc3)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5 10.1021/jm8015552
71625025 87234 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 465 5 2 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338740 87234 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 465 5 2 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
71459962 78815 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Binding
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor mu 1 (DAMGO) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor mu 1 (DAMGO) transfected onto CHO cells
ChEMBL 459 5 1 5 4.2 CO[C@]12C=C[C@@]3(C[C@H]1[C@@H](C)OCc1ccccc1)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm990951r
CHEMBL2113671 78815 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Binding
EC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor mu 1 (DAMGO) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human Opioid receptor mu 1 (DAMGO) transfected onto CHO cells
ChEMBL 459 5 1 5 4.2 CO[C@]12C=C[C@@]3(C[C@H]1[C@@H](C)OCc1ccccc1)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm990951r
58443217 83523 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 522 8 1 3 6.6 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1C 10.1016/j.bmcl.2012.10.081
CHEMBL2208352 83523 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 522 8 1 3 6.6 COc1ccc(-c2ccc(CCNC(=O)c3ccc4c(c3)C3(C)CCN(CC5CC5)C(C4)C3C)cc2)cc1C 10.1016/j.bmcl.2012.10.081
122195956 123430 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 477 6 3 4 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3CCCCC3)ccc21 10.1021/acs.jmedchem.5b01270
CHEMBL3634250 123430 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 477 6 3 4 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(CC3CCCCC3)ccc21 10.1021/acs.jmedchem.5b01270
155539282 171990 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assayAgonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assay
ChEMBL 633 12 5 6 2.5 Cc1cc(O)c(Cl)c(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2019.06.077
CHEMBL4514319 171990 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assayAgonist activity at human recombinant MOR expressed in CHO cells co-expressing C-terminally modified Galphaqi5 assessed as induction of calcium mobilization by Fluo-4AM dye-based fluorescence assay
ChEMBL 633 12 5 6 2.5 Cc1cc(O)c(Cl)c(C)c1C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2019.06.077
56945125 159044 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.
ChEMBL 514 8 1 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C(N)=O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL4106746 159044 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.Functional Assay: [35S]GTPgammaS functional assays were conducted using freshly thawed u-receptor membranes (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPgammaS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 ul/well) was transferred to 96-shallow well polypropylene plates containing 10 ul of 20x concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 2001 of ice-cold binding buffer.
ChEMBL 514 8 1 5 4.2 CO[C@]12CC[C@@]3(C[C@@H]1COCc1ccccc1)[C@H]1Cc4ccc(C(N)=O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
44408526 136159 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL374325 136159 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
44408526 136159 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL374325 136159 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cellsInhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
49799969 10274 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Binding
EC50 for binding of [35S]- GTPdeltaS in cloned human oOpioid receptor mu 1 (DAMGO) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human oOpioid receptor mu 1 (DAMGO) transfected onto CHO cells
ChEMBL 411 4 2 5 3.2 CCC[C@@](C)(O)[C@@H]1CC23C=C[C@]1(OC)[C@H]1Oc4c(O)ccc5c4C12CCN(C)C3C5 10.1021/jm990951r
CHEMBL1169585 10274 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Binding
EC50 for binding of [35S]- GTPdeltaS in cloned human oOpioid receptor mu 1 (DAMGO) transfected onto CHO cellsEC50 for binding of [35S]- GTPdeltaS in cloned human oOpioid receptor mu 1 (DAMGO) transfected onto CHO cells
ChEMBL 411 4 2 5 3.2 CCC[C@@](C)(O)[C@@H]1CC23C=C[C@]1(OC)[C@H]1Oc4c(O)ccc5c4C12CCN(C)C3C5 10.1021/jm990951r
CHEMBL4783612 181376 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 464 6 3 6 2.5 CO[C@@]12CC[C@@H](N[C@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
25232543 184945 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 497 4 3 6 3.3 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2n1 10.1021/jm801272c
CHEMBL494854 184945 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 497 4 3 6 3.3 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc2ccccc2n1 10.1021/jm801272c
51003219 59576 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins
ChEMBL 518 10 3 6 3.7 O=C(O)CN[C@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm101211p
CHEMBL1739441 59576 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins
ChEMBL 518 10 3 6 3.7 O=C(O)CN[C@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm101211p
CHEMBL3216476 59576 0 OPRM μ receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins
ChEMBL 518 10 3 6 3.7 O=C(O)CN[C@H]1CC[C@@]2(OCCCc3ccccc3)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm101211p
50994530 56705 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 716 14 5 7 2.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649946 56705 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 716 14 5 7 2.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
25259489 171618 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 517 6 3 7 3.1 O=C(/C=C/c1ccccc1[N+](=O)[O-])N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm8015552
CHEMBL448145 171618 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 517 6 3 7 3.1 O=C(/C=C/c1ccccc1[N+](=O)[O-])N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/jm8015552
50994530 56705 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 716 14 5 7 2.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649946 56705 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 716 14 5 7 2.8 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
155520861 169654 0 OPRM μ receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysisAgonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
ChEMBL 409 4 1 7 2.7 CC[C@@H]1CN2CC[C@]3(Nc4cccc(C#N)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.6b00748
CHEMBL4449284 169654 0 OPRM μ receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysisAgonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
ChEMBL 409 4 1 7 2.7 CC[C@@H]1CN2CC[C@]3(Nc4cccc(C#N)c4C3=O)[C@@H]2C[C@@H]1/C(=C\OC)C(=O)OC 10.1021/acs.jmedchem.6b00748
9848990 186324 1 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL2368861 186324 1 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL511142 186324 1 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
24768353 97059 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay
ChEMBL 941 22 9 9 2.7 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm070332f
CHEMBL271619 97059 0 OPRM μ receptor Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assayAgonist activity at rat mu opioid receptor by [35S]GTP-gamma-S binding assay
ChEMBL 941 22 9 9 2.7 CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1 10.1021/jm070332f
1651 2556 17 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
4673 2556 17 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
6445230 2556 17 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
CHEMBL267495 2556 17 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
DB13471 2556 17 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 10.1016/j.bmcl.2014.09.029
60170689 81060 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 656 12 6 6 3.0 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1cccc(Cl)c1 10.1021/jm300664y
CHEMBL2163912 81060 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 656 12 6 6 3.0 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1cccc(Cl)c1 10.1021/jm300664y
50994531 56706 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 804 13 4 7 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649947 56706 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 804 13 4 7 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
54581461 60713 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1143 29 10 12 4.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1 10.1021/jm101023r
CHEMBL1766207 60713 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1143 29 10 12 4.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1 10.1021/jm101023r
71624778 87227 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 507 6 2 5 5.3 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338733 87227 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 507 6 2 5 5.3 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CC1CCCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
50994531 56706 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 804 13 4 7 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649947 56706 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 804 13 4 7 4.2 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)CNC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
132961503 160213 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu 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 mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 382 5 2 5 3.4 O=[N+]([O-])c1ccc(CCN2CC[C@@]3(c4cccc(O)c4)CCC[C@@H]2[C@H]3O)cc1 10.1016/j.bmc.2017.02.064
CHEMBL4085431 160213 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu 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 mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 382 5 2 5 3.4 O=[N+]([O-])c1ccc(CCN2CC[C@@]3(c4cccc(O)c4)CCC[C@@H]2[C@H]3O)cc1 10.1016/j.bmc.2017.02.064
CHEMBL4116456 160213 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu 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 mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
ChEMBL 382 5 2 5 3.4 O=[N+]([O-])c1ccc(CCN2CC[C@@]3(c4cccc(O)c4)CCC[C@@H]2[C@H]3O)cc1 10.1016/j.bmc.2017.02.064
CHEMBL4757240 179984 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 464 6 3 6 2.5 CO[C@@]12CC[C@H](N[C@H](Cc3ccccc3)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
155538317 175447 0 OPRM μ receptor Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12 10.1021/acs.jmedchem.9b01767
CHEMBL4476318 175447 0 OPRM μ receptor Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12 10.1021/acs.jmedchem.9b01767
CHEMBL4595175 175447 0 OPRM μ receptor Mouse 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2occc12 10.1021/acs.jmedchem.9b01767
127049274 140217 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 487 6 3 5 4.3 COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
CHEMBL3823830 140217 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 487 6 3 5 4.3 COC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccccc3)ccc21 10.1021/acs.jmedchem.6b00308
5359966 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm050577x
CHEMBL49269 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayActivity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm050577x
5359966 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm101542c
CHEMBL49269 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm101542c
5359966 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1016/j.bmcl.2007.01.013
CHEMBL49269 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1016/j.bmcl.2007.01.013
5359966 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm3001086
CHEMBL49269 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm3001086
5359966 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1016/j.bmc.2007.03.076
CHEMBL49269 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 minsAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1016/j.bmc.2007.03.076
CHEMBL2419542 203958 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assayAgonist activity at rat MOR expressed in HN9.10 cell membranes by [35S]GTPgammaS binding assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2013.06.065
5359966 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranesAgonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranes
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm049978n
CHEMBL49269 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranesAgonistic activity against Opioid receptor mu 1 in Chinese hamster ovary membranes
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm049978n
44279594 106392 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells
ChEMBL 423 1 2 5 3.2 CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm991165p
CHEMBL31605 106392 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
GTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cellsGTPgammaS binding in cloned human Opioid receptor mu 1 transfected into hamster ovary cells
ChEMBL 423 1 2 5 3.2 CO[C@]12C=CC3(CC14CCC(C)(C)[C@H]4O)C1Cc4ccc(O)c5c4C3(CCN1C)[C@@H]2O5 10.1021/jm991165p
5359966 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
Inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cell membranes was determinedInhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cell membranes was determined
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm030139v
CHEMBL49269 184578 7 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
Inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cell membranes was determinedInhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cell membranes was determined
ChEMBL 297 2 1 2 3.9 Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm030139v
56668839 66076 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
ChEMBL 481 4 3 6 2.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Cl)c1 10.1016/j.bmcl.2011.06.135
CHEMBL1824509 66076 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
ChEMBL 481 4 3 6 2.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Cl)c1 10.1016/j.bmcl.2011.06.135
CHEMBL1852788 66076 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
ChEMBL 481 4 3 6 2.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Cl)c1 10.1016/j.bmcl.2011.06.135
69122105 180379 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 431 6 4 7 0.1 CO[C@@]12CC[C@H](N[C@@H](CC(N)=O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL4761784 180379 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 431 6 4 7 0.1 CO[C@@]12CC[C@H](N[C@@H](CC(N)=O)C(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
56668839 66076 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 481 4 3 6 2.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Cl)c1 10.1021/jm301247n
CHEMBL1824509 66076 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 481 4 3 6 2.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Cl)c1 10.1021/jm301247n
CHEMBL1852788 66076 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 481 4 3 6 2.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Cl)c1 10.1021/jm301247n
44177670 60712 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1151 27 10 10 5.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766206 60712 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1151 27 10 10 5.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1 10.1021/jm101023r
44177670 60712 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1151 27 10 10 5.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1 10.1021/jm101023r
CHEMBL1766206 60712 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1151 27 10 10 5.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(F)(F)F)c1 10.1021/jm101023r
71453373 81061 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 656 12 6 6 3.0 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1Cl 10.1021/jm300664y
CHEMBL2163913 81061 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counterAgonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter
ChEMBL 656 12 6 6 3.0 C=C(C(N)=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1Cl 10.1021/jm300664y
71720457 86176 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21 10.1021/jm400050y
CHEMBL2322561 86176 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21 10.1021/jm400050y
71720457 86176 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21 10.1021/acs.jmedchem.5b01270
CHEMBL2322561 86176 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 479 6 4 4 5.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cccc4ccccc34)cc21 10.1021/acs.jmedchem.5b01270
77104977 149013 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
[35S]GTPγS Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared from a cell line expressing recombinant μ opioid receptor in a HEK-293, CHO or U-2 OS cell background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.[35S]GTPγS Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared from a cell line expressing recombinant μ opioid receptor in a HEK-293, CHO or U-2 OS cell background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 353 3 1 3 3.9 CC(C)[C@@H]1C[C@H]2[C@H]3Cc4ccc(O)cc4[C@@]2(CCN3CC2CC2)CC1=O nan
CHEMBL3948713 149013 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
[35S]GTPγS Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared from a cell line expressing recombinant μ opioid receptor in a HEK-293, CHO or U-2 OS cell background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.[35S]GTPγS Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared from a cell line expressing recombinant μ opioid receptor in a HEK-293, CHO or U-2 OS cell background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.; or DiscovRx, Fremont, Calif.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 353 3 1 3 3.9 CC(C)[C@@H]1C[C@H]2[C@H]3Cc4ccc(O)cc4[C@@]2(CCN3CC2CC2)CC1=O nan
71624892 87224 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 467 6 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338730 87224 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 467 6 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
57900041 87495 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting
ChEMBL 479 7 1 3 5.7 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5cccnc5)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2013.01.117
CHEMBL2347236 87495 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Partial agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation countingPartial agonist activity at human mu opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting
ChEMBL 479 7 1 3 5.7 C[C@H]1C2Cc3ccc(C(=O)NCCc4ccc(-c5cccnc5)cc4)cc3[C@@]1(C)CCN2CC1CC1 10.1016/j.bmcl.2013.01.117
44592015 186399 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 386 3 4 5 1.4 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3 10.1016/j.bmcl.2009.02.078
CHEMBL511645 186399 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 386 3 4 5 1.4 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3 10.1016/j.bmcl.2009.02.078
73211769 159149 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 465 2 1 5 4.8 CC(C)(C)[C@@]1(C)OCO[C@]23CC[C@@]4(C[C@H]12)[C@H]1Cc2ccc(O)c5c2[C@@]4(CCN1CC1CC1)[C@H]3O5 nan
CHEMBL4107585 159149 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.μ-Opioid Receptor Functional Assay: [35S]GTPγS functional assays were conducted using freshly thawed μ-receptor membranes prepared in-house from a cell line expressing recombinant μ opioid receptor in a HEK293 background or purchased from a commercial source (Perkin Elmer, Shelton, Conn.). Assay reactions were prepared by sequentially adding the following reagents to binding buffer (100 mM NaCl, 10 mM MgCl2, 20 mM HEPES, pH 7.4) on ice (final concentrations indicated): membrane protein (0.026 mg/mL), saponin (10 mg/mL), GDP (3 mM) and [35S]GTPγS (0.20 nM; Perkin Elmer, Shelton, Conn.). The prepared membrane solution (190 μl/well) was transferred to 96-shallow well polypropylene plates containing 10 μl of 20× concentrated stock solutions of the agonist [D-Ala2, N-methyl-Phe4 Gly-ol5]-enkephalin (DAMGO) prepared in dimethyl sulfoxide (DMSO). Plates were incubated for 30 min at 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 (Perkin Elmer, Shelton, Conn.) followed by three filtration washes with 200 μl of ice-cold wash buffer (10 mM NaH2PO4, 10 mM Na2HPO4, pH 7.4). Filter plates were subsequently dried at 50 °C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 μl/well) and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 465 2 1 5 4.8 CC(C)(C)[C@@]1(C)OCO[C@]23CC[C@@]4(C[C@H]12)[C@H]1Cc2ccc(O)c5c2[C@@]4(CCN1CC1CC1)[C@H]3O5 nan
24768397 145617 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 698 14 5 7 2.7 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL392185 145617 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 698 14 5 7 2.7 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
44436084 87840 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 845 18 6 8 3.4 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm061465o
CHEMBL235109 87840 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 845 18 6 8 3.4 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm061465o
CHEMBL4789014 181788 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 579 9 5 8 2.3 CO[C@@]12CC[C@H](N[C@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)O)C(C)C)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
86582908 159229 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 324 3 1 2 3.3 NC(=O)c1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CC1)CC3 nan
CHEMBL4108288 159229 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 324 3 1 2 3.3 NC(=O)c1ccc2c(c1)[C@@]13CCCCC1[C@@H](C2)N(CC1CC1)CC3 nan
24768397 145617 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 698 14 5 7 2.7 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL392185 145617 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 698 14 5 7 2.7 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
44436084 87840 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 845 18 6 8 3.4 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm061465o
CHEMBL235109 87840 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assayAgonist activity at rat mu-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
ChEMBL 845 18 6 8 3.4 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm061465o
127050834 140226 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 549 8 3 4 6.0 CCCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21 10.1021/acs.jmedchem.6b00308
CHEMBL3823891 140226 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assayAgonist activity at rat MOR transfected in rat C6 cell membranes after 1 hr by [35S]GTPgammaS assay
ChEMBL 549 8 3 4 6.0 CCCC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21 10.1021/acs.jmedchem.6b00308
73355099 90955 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis
ChEMBL 729 11 3 6 5.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
CHEMBL2408014 90955 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis
ChEMBL 729 11 3 6 5.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
155522441 175642 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 537 7 3 5 5.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4451910 175642 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 537 7 3 5 5.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4596711 175642 0 OPRM μ receptor Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 537 7 3 5 5.2 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)C2CC2)c2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
11849360 195423 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 478 4 1 5 3.5 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(Cl)cc5)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
CHEMBL607069 195423 0 OPRM μ receptor Human 9.1 pEC50 = 9.1 Functional
Stimulation of [35S]GTPgammaS binding to human recombinant MORStimulation of [35S]GTPgammaS binding to human recombinant MOR
ChEMBL 478 4 1 5 3.5 COc1ccc2c3c1O[C@H]1C(=O)CC[C@@]4(NC(=O)/C=C/c5ccc(Cl)cc5)[C@@H](C2)N(C)CC[C@]314 10.1021/jm0604777
73355099 90955 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis
ChEMBL 729 11 3 6 5.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
CHEMBL2408014 90955 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysisAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 90 mins by liquid scintillation counting analysis
ChEMBL 729 11 3 6 5.0 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2Cc3ccccc3CN2C(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/ml400115n
122195958 123432 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 521 6 3 4 5.2 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21 10.1021/acs.jmedchem.5b01270
CHEMBL3634252 123432 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysisAgonist activity at rat mu-opioid receptor expressed in C6 cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
ChEMBL 521 6 3 4 5.2 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3ccc4ccccc4c3)ccc21 10.1021/acs.jmedchem.5b01270
50994458 56699 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 641 12 4 6 3.5 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649940 56699 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 641 12 4 6 3.5 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
50994458 56699 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 641 12 4 6 3.5 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
CHEMBL1649940 56699 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 641 12 4 6 3.5 CCC(=O)N(c1ccccc1)C1CCN(C(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)CC1 10.1021/jm100982d
155771777 181228 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL 363 6 1 2 5.5 CCC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
CHEMBL4781853 181228 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL 363 6 1 2 5.5 CCC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
155567281 175782 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12 10.1021/acs.jmedchem.9b01767
CHEMBL4588474 175782 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12 10.1021/acs.jmedchem.9b01767
CHEMBL4597924 175782 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12 10.1021/acs.jmedchem.9b01767
54581461 60713 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1143 29 10 12 4.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1 10.1021/jm101023r
CHEMBL1766207 60713 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
ChEMBL 1143 29 10 12 4.0 CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(OC)c(OC)c1 10.1021/jm101023r
155515704 175814 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12 10.1021/acs.jmedchem.9b01767
CHEMBL4442161 175814 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12 10.1021/acs.jmedchem.9b01767
CHEMBL4598179 175814 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 486 4 3 6 3.5 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2ccoc12 10.1021/acs.jmedchem.9b01767
44592015 186399 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 386 3 4 5 1.4 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3 nan
CHEMBL511645 186399 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 386 3 4 5 1.4 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CC[C@@H](O)C3 nan
1647 1232 33 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assayActivation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1074/jbc.m703272200
5462471 1232 33 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assayActivation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1074/jbc.m703272200
CHEMBL113995 1232 33 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assayActivation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1074/jbc.m703272200
CHEMBL38874 1232 33 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assayActivation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1074/jbc.m703272200
1647 1232 33 OPRM μ receptor Human 9.0 pEC50 = 9 Binding
Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uMActivation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM
ChEMBL None None None None 10.1074/jbc.m703272200
5462471 1232 33 OPRM μ receptor Human 9.0 pEC50 = 9 Binding
Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uMActivation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM
ChEMBL None None None None 10.1074/jbc.m703272200
CHEMBL113995 1232 33 OPRM μ receptor Human 9.0 pEC50 = 9 Binding
Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uMActivation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM
ChEMBL None None None None 10.1074/jbc.m703272200
CHEMBL38874 1232 33 OPRM μ receptor Human 9.0 pEC50 = 9 Binding
Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uMActivation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM
ChEMBL None None None None 10.1074/jbc.m703272200
9839245 100711 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 298 3 1 2 2.7 CC1C2Cc3ccc(C(N)=O)cc3C1(C)CCN2CC1CC1 10.1016/j.bmcl.2008.10.134
CHEMBL297428 100711 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Activity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at human cloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 298 3 1 2 2.7 CC1C2Cc3ccc(C(N)=O)cc3C1(C)CCN2CC1CC1 10.1016/j.bmcl.2008.10.134
118567608 169874 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 398 4 0 3 4.2 CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2Cl)C1=O 10.1021/acs.jmedchem.9b01256
CHEMBL4452042 169874 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 398 4 0 3 4.2 CC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2Cl)C1=O 10.1021/acs.jmedchem.9b01256
118562510 172050 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 378 5 0 3 3.9 CCC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O 10.1021/acs.jmedchem.9b01256
CHEMBL4515812 172050 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assayAgonist activity at human MOR expressed in CHOK1 cells assessed as stimulation of cAMP accumulation incubated for 45 mins by HTRF assay
ChEMBL 378 5 0 3 3.9 CCC1OC2(CCN(CCc3ccccc3)CC2)CN(c2ccccc2)C1=O 10.1021/acs.jmedchem.9b01256
11250029 1446 27 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 569 11 4 6 4.2 COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N 10.1016/j.bmcl.2012.05.042
130406582 1446 27 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 569 11 4 6 4.2 COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N 10.1016/j.bmcl.2012.05.042
5001 1446 27 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 569 11 4 6 4.2 COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N 10.1016/j.bmcl.2012.05.042
7691 1446 27 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 569 11 4 6 4.2 COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N 10.1016/j.bmcl.2012.05.042
CHEMBL2159122 1446 27 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 569 11 4 6 4.2 COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N 10.1016/j.bmcl.2012.05.042
DB09272 1446 27 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assayAgonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay
ChEMBL 569 11 4 6 4.2 COc1ccc(cc1C(=O)O)CN([C@H](c1ncc([nH]1)c1ccccc1)C)C(=O)[C@H](Cc1c(C)cc(cc1C)C(=O)N)N 10.1016/j.bmcl.2012.05.042
25256967 178351 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 514 6 2 6 3.7 CC(=O)O[C@@]12CC[C@@H](NC(=O)/C=C/c3ccccc3)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5 10.1021/jm8015552
CHEMBL472583 178351 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at rat mu opioid receptor expressed in rat C6 cell membrane assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 514 6 2 6 3.7 CC(=O)O[C@@]12CC[C@@H](NC(=O)/C=C/c3ccccc3)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(CC1CC1)[C@@H]2C5 10.1021/jm8015552
155551874 175710 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 584 7 3 5 5.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4569709 175710 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 584 7 3 5 5.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597300 175710 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 584 7 3 5 5.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCN(C(=O)c2ccccc2)c2ccc(Cc3cnc4ccccc4c3)cc21 10.1021/acs.jmedchem.9b00378
71717732 87206 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 7 2 5 4.6 CO[C@]12C=C[C@@]3(C[C@@H]1[C@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338714 87206 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 7 2 5 4.6 CO[C@]12C=C[C@@]3(C[C@@H]1[C@](C)(O)CCC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
71624777 87226 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 5 2 5 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338732 87226 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 479 5 2 5 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C1CCCC1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
71624894 87231 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 439 5 2 5 3.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338737 87231 0 OPRM μ receptor Rat 9.0 pEC50 = 9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 439 5 2 5 3.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@H](O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
5487663 72260 7 OPRM μ receptor Human 9.0 pEC50 = 9 Binding
Binding affinity to MOR (unknown origin)Binding affinity to MOR (unknown origin)
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/acsmedchemlett.7b00210
CHEMBL200199 72260 7 OPRM μ receptor Human 9.0 pEC50 = 9 Binding
Binding affinity to MOR (unknown origin)Binding affinity to MOR (unknown origin)
ChEMBL 908 22 12 12 -1.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/acsmedchemlett.7b00210
44401457 131974 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 384 3 3 5 1.6 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CCC(=O)C3 nan
CHEMBL370029 131974 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 384 3 3 5 1.6 NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CCC4)[C@H](C2)[C@]1(O)CCC(=O)C3 nan
25232367 186756 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 447 4 3 6 2.2 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccnc1 10.1021/jm801272c
CHEMBL514769 186756 0 OPRM μ receptor Human 9.0 pEC50 = 9 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 447 4 3 6 2.2 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccnc1 10.1021/jm801272c
155530151 175686 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12 10.1021/acs.jmedchem.9b01767
CHEMBL4463978 175686 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12 10.1021/acs.jmedchem.9b01767
CHEMBL4597107 175686 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting methodAgonist activity at recombinant mouse mu opioid receptor expressed in CHO cell membrane assessed as [35]-GTPgammaS binding incubated for 1.5 hrs by scintillation counting method
ChEMBL 502 4 3 6 4.0 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1cccc2sccc12 10.1021/acs.jmedchem.9b01767
72164177 91339 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 513 4 4 7 3.0 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc2ccccc2c1O 10.1016/j.bmcl.2013.07.043
CHEMBL2417568 91339 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 513 4 4 7 3.0 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc2ccccc2c1O 10.1016/j.bmcl.2013.07.043
72164177 91339 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 513 4 4 7 3.0 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc2ccccc2c1O 10.1016/j.bmc.2015.02.055
CHEMBL2417568 91339 0 OPRM μ receptor Mouse 9.0 pEC50 = 9.0 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 513 4 4 7 3.0 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ncc2ccccc2c1O 10.1016/j.bmc.2015.02.055
118716010 114042 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 499 6 3 6 2.5 O=C(NCCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5 10.1016/j.bmcl.2014.09.029
CHEMBL3339379 114042 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 499 6 3 6 2.5 O=C(NCCc1ccccc1)C1=N[C@@]23CC[C@]1(O)C1Oc4c(O)ccc5c4C12CCN(CC1CC1)C3C5 10.1016/j.bmcl.2014.09.029
57412942 75252 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 445 6 1 4 6.1 O=[N+]([O-])c1cccc(CNc2ccc3c(c2)[C@@]24CCCC[C@H]2[C@@H](C3)N(CC2CCC2)CC4)c1 10.1021/jm3001086
CHEMBL2048767 75252 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 445 6 1 4 6.1 O=[N+]([O-])c1cccc(CNc2ccc3c(c2)[C@@]24CCCC[C@H]2[C@@H](C3)N(CC2CCC2)CC4)c1 10.1021/jm3001086
71583623 86175 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 443 7 4 4 4.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CCc3ccccc3)cc21 10.1021/jm400050y
CHEMBL2322560 86175 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysisAgonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
ChEMBL 443 7 4 4 4.3 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(CCc3ccccc3)cc21 10.1021/jm400050y
134345539 175693 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 469 6 4 5 4.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4529363 175693 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 469 6 4 5 4.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597172 175693 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 469 6 4 5 4.9 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@@H]1CCNc2ccc(Cc3cc4ccccc4o3)cc21 10.1021/acs.jmedchem.9b00378
155555053 175711 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 522 6 3 5 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cnc4ccccc4c3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL4550332 175711 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 522 6 3 5 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cnc4ccccc4c3)ccc21 10.1021/acs.jmedchem.9b00378
CHEMBL4597317 175711 0 OPRM μ receptor Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hrAgonist activity at rat mu opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr
ChEMBL 522 6 3 5 4.6 CC(=O)N1CC[C@@H](NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)c2cc(Cc3cnc4ccccc4c3)ccc21 10.1021/acs.jmedchem.9b00378
86582595 159291 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 382 3 3 4 2.6 C=C1CC[C@@]2(O)[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC2CCC2)C1 nan
CHEMBL4108846 159291 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes.
ChEMBL 382 3 3 4 2.6 C=C1CC[C@@]2(O)[C@H]3Cc4ccc(C(N)=O)c(O)c4[C@@]2(CCN3CC2CCC2)C1 nan
CHEMBL4640139 176687 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 586 8 2 6 6.5 Oc1cccc(-c2cnc3c(c2)C[C@@]2(OCCCc4ccccc4)[C@H]4Cc5ccc(O)c6c5[C@@]2(CCN4CC2CC2)[C@H]3O6)c1 10.1021/acs.jmedchem.0c00503
56672310 66025 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
ChEMBL 461 4 3 6 2.5 Cc1cc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)ccn1 10.1016/j.bmcl.2011.06.135
CHEMBL1824512 66025 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
ChEMBL 461 4 3 6 2.5 Cc1cc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)ccn1 10.1016/j.bmcl.2011.06.135
CHEMBL1852558 66025 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Functional
Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
ChEMBL 461 4 3 6 2.5 Cc1cc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)ccn1 10.1016/j.bmcl.2011.06.135
56672310 66025 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 461 4 3 6 2.5 Cc1cc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)ccn1 10.1021/jm301247n
CHEMBL1824512 66025 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 461 4 3 6 2.5 Cc1cc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)ccn1 10.1021/jm301247n
CHEMBL1852558 66025 0 OPRM μ receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 461 4 3 6 2.5 Cc1cc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)ccn1 10.1021/jm301247n
25232540 187687 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 447 4 3 6 2.2 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1 10.1021/jm801272c
CHEMBL522143 187687 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 447 4 3 6 2.2 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1 10.1021/jm801272c
72164055 91389 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 525 6 3 6 3.6 O=C(CCc1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1016/j.bmcl.2013.07.043
CHEMBL2419119 91389 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 525 6 3 6 3.6 O=C(CCc1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1016/j.bmcl.2013.07.043
72164055 91389 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 525 6 3 6 3.6 O=C(CCc1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1016/j.bmc.2015.02.055
CHEMBL2419119 91389 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 525 6 3 6 3.6 O=C(CCc1cc2ccccc2cn1)N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1016/j.bmc.2015.02.055
CHEMBL375068 205724 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assayActivity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
ChEMBL None None None Cc1cc(C[C@H](N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2cccc3ccccc23)C(N)=O)cc(C)c1O 10.1021/jm060998u
12038839 57358 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 374 4 3 6 0.9 CO[C@@]12CC[C@H](NCC(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
CHEMBL1672084 57358 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assayAgonist activity at human MOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
ChEMBL 374 4 3 6 0.9 CO[C@@]12CC[C@H](NCC(=O)O)[C@@H]3Oc4c(O)ccc5c4[C@@]31CCN(C)[C@@H]2C5 10.1021/acs.jmedchem.8b01327
56679008 65966 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
ChEMBL 525 4 3 6 2.9 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Br)c1 10.1016/j.bmcl.2011.06.135
CHEMBL1824510 65966 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
ChEMBL 525 4 3 6 2.9 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Br)c1 10.1016/j.bmcl.2011.06.135
CHEMBL1852385 65966 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS bindingAgonist activity against mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
ChEMBL 525 4 3 6 2.9 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Br)c1 10.1016/j.bmcl.2011.06.135
56679008 65966 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 525 4 3 6 2.9 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Br)c1 10.1021/jm301247n
CHEMBL1824510 65966 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 525 4 3 6 2.9 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Br)c1 10.1021/jm301247n
CHEMBL1852385 65966 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS bindingAgonist activity at mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding
ChEMBL 525 4 3 6 2.9 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccnc(Br)c1 10.1021/jm301247n
72735760 105595 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 438 2 2 5 4.1 Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL3139108 105595 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 438 2 2 5 4.1 Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
CHEMBL4296726 105595 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assayAgonist activity at human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by [35S]GTPgammaS binding assay
ChEMBL 438 2 2 5 4.1 Oc1ccc2c(c1)[C@]13CCN(Cc4ccco4)[C@H](C2)[C@]1(O)Cc1cc2ccccc2nc1C3 10.1016/j.bmc.2013.10.032
44380504 58537 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay
ChEMBL 427 2 2 5 3.6 CO[C@@]12CCC3(C[C@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@H]2O5 10.1016/s0960-894x(99)00085-2
CHEMBL169552 58537 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Activity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assayActivity was evaluated in human mu opioid receptors transfected with CHO cells by [35S]GTP-gamma-S, assay
ChEMBL 427 2 2 5 3.6 CO[C@@]12CCC3(C[C@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4C3(CCN1C)[C@H]2O5 10.1016/s0960-894x(99)00085-2
156043182 182262 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL 379 7 2 3 4.5 OCCC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
CHEMBL4795160 182262 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assayAgonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay
ChEMBL 379 7 2 3 4.5 OCCC[C@H]1[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1039/d0md00104j
132079904 181594 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu 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 mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay
ChEMBL 492 4 0 8 4.4 COC(=O)[C@@H]1C=C(OC(=O)c2ccccc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C 10.1021/acs.jmedchem.6b01235
CHEMBL4786506 181594 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu 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 mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay
ChEMBL 492 4 0 8 4.4 COC(=O)[C@@H]1C=C(OC(=O)c2ccccc2)C(=O)[C@H]2[C@@]1(C)CC[C@H]1C(=O)O[C@H](c3ccoc3)C[C@@]12C 10.1021/acs.jmedchem.6b01235
90655828 110482 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 486 3 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1c1ccccc1 10.1021/ml400491k
CHEMBL3264747 110482 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey methodAgonist activity at human mu opioid receptor expressed in HEK293 cells by CellKey method
ChEMBL 486 3 1 6 3.3 O=C1[C@H]2O[C@@]34CC[C@@]5(OCOc6c(O)ccc7c6[C@@]3(CCN(CC3CC3)[C@@H]4C7)[C@H]25)N1c1ccccc1 10.1021/ml400491k
54580938 61526 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 805 15 1 7 10.2 O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@@]1(O)[C@@H](C2)N(CC1CCC1)CC3 10.1016/j.bmc.2011.03.052
CHEMBL1774949 61526 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingAgonist activity at human mu-opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 805 15 1 7 10.2 O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@@]1(O)[C@@H](C2)N(CC1CCC1)CC3 10.1016/j.bmc.2011.03.052
11848225 831 42 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 831 42 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 831 42 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 831 42 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3325961 119791 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3545622 119791 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant MOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
44598284 191445 0 OPRM μ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 742 9 7 9 1.8 NC(=O)[C@@H]1CSCSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1 10.1021/jm9007483
CHEMBL572525 191445 0 OPRM μ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at rat mu opioid receptor expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
ChEMBL 742 9 7 9 1.8 NC(=O)[C@@H]1CSCSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1 10.1021/jm9007483
71624446 87238 0 OPRM μ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 467 6 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338744 87238 0 OPRM μ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 467 6 2 5 4.4 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
11848225 831 42 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
8866 831 42 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL2364605 831 42 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3962932 831 42 OPRM μ receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
146408960 172992 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins
ChEMBL 465 4 3 6 2.3 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1F 10.1021/acs.jmedchem.8b01158
CHEMBL4538841 172992 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins
ChEMBL 465 4 3 6 2.3 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1F 10.1021/acs.jmedchem.8b01158
5486554 31030 15 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assayInverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assay
ChEMBL 343 2 3 5 1.3 Oc1ccc2c3c1O[C@H]1[C@H](O)CC[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1016/j.bmcl.2012.06.056
CHEMBL140278 31030 15 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assayInverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assay
ChEMBL 343 2 3 5 1.3 Oc1ccc2c3c1O[C@H]1[C@H](O)CC[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1016/j.bmcl.2012.06.056
CHEMBL558140 31030 15 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assayInverse agonist activity at human recombinant mu opioid receptor expressed in CHO cells after 3 hrs by [35S]GTPgammaS binding assay
ChEMBL 343 2 3 5 1.3 Oc1ccc2c3c1O[C@H]1[C@H](O)CC[C@@]4(O)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1016/j.bmcl.2012.06.056
72164176 91392 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 547 4 4 7 3.7 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1nc(Cl)c2ccccc2c1O 10.1016/j.bmcl.2013.07.043
CHEMBL2419122 91392 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrsAgonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
ChEMBL 547 4 4 7 3.7 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1nc(Cl)c2ccccc2c1O 10.1016/j.bmcl.2013.07.043
72164176 91392 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 547 4 4 7 3.7 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1nc(Cl)c2ccccc2c1O 10.1016/j.bmc.2015.02.055
CHEMBL2419122 91392 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assayStimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
ChEMBL 547 4 4 7 3.7 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1nc(Cl)c2ccccc2c1O 10.1016/j.bmc.2015.02.055
25233258 186894 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 447 4 3 6 2.2 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1 10.1021/jm801272c
CHEMBL515864 186894 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 447 4 3 6 2.2 O=C(N[C@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccncc1 10.1021/jm801272c
CHEMBL4633209 176243 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 570 8 1 5 6.8 Oc1ccc2c3c1O[C@H]1c4ncc(-c5ccccc5)cc4C[C@@]4(OCCCc5ccccc5)[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/acs.jmedchem.0c00503
71624665 87250 0 OPRM μ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 453 5 2 5 4.0 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
CHEMBL2338756 87250 0 OPRM μ receptor Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hrAgonist activity at rat recombinant MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr
ChEMBL 453 5 2 5 4.0 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm301543e
146405163 173048 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins
ChEMBL 472 4 3 7 2.0 N#Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/acs.jmedchem.8b01158
CHEMBL4540013 173048 0 OPRM μ receptor Mouse 8.9 pEC50 = 8.9 Functional
Antagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 minsAntagonist activity at mouse MOR expressed in CHO cell membranes assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding after 90 mins
ChEMBL 472 4 3 7 2.0 N#Cc1cnccc1C(=O)N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5 10.1021/acs.jmedchem.8b01158
16100408 140990 0 OPRM μ receptor Rat 8.9 pEC50 = 8.9 Functional
Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL386186 140990 0 OPRM μ receptor Rat 8.9 pEC50 = 8.9 Functional
Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assayActivity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
2491 3474 18 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 386 8 0 4 4.2 COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC 10.1021/acs.jmedchem.8b00435
3534 3474 18 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 386 8 0 4 4.2 COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC 10.1021/acs.jmedchem.8b00435
41693 3474 18 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 386 8 0 4 4.2 COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC 10.1021/acs.jmedchem.8b00435
CHEMBL658 3474 18 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 386 8 0 4 4.2 COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC 10.1021/acs.jmedchem.8b00435
DB00708 3474 18 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assayAgonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
ChEMBL 386 8 0 4 4.2 COCC1(CCN(CC1)CCc1cccs1)N(c1ccccc1)C(=O)CC 10.1021/acs.jmedchem.8b00435
44427183 91466 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding
ChEMBL 430 4 1 3 6.2 O=C(Nc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CCC1)CC3 10.1016/j.bmcl.2007.01.013
CHEMBL242048 91466 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTP-gamma-S binding
ChEMBL 430 4 1 3 6.2 O=C(Nc1ccccc1)Oc1ccc2c(c1)C13CCCCC1C(C2)N(CC1CCC1)CC3 10.1016/j.bmcl.2007.01.013
71454514 78496 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 531 6 2 7 3.6 CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1021/jm070255o
CHEMBL2113308 78496 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 531 6 2 7 3.6 CO[C@@]12CC[C@@]3(C[C@@H]1CNC(=O)/C=C/c1ccc([N+](=O)[O-])cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1C)[C@H]2O5 10.1021/jm070255o
9897164 39250 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 789 15 0 6 11.0 O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3 10.1021/jm900379p
CHEMBL147511 39250 0 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 789 15 0 6 11.0 O=C(CCCCCCCCC(=O)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3)Oc1ccc2c(c1)[C@@]13CCCC[C@H]1[C@@H](C2)N(CC1CCC1)CC3 10.1021/jm900379p
1613 2159 34 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu 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 mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530
3903 2159 34 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu 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 mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530
461776 2159 34 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu 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 mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530
CHEMBL15038 2159 34 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu 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 mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530
CHEMBL8234 2159 34 OPRM μ receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mu 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 mu opioid receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00530