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Ligand source activities (1 row/activity)

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11711282 2240 0 AA3R A3 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 410 3 2 3 7.2 Clc1ccc(cc1Cl)Nc1nc2ccccc2c2c1[nH]c(n2)C1CCCCC1 16722654
9446 2240 0 AA3R A3 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 410 3 2 3 7.2 Clc1ccc(cc1Cl)Nc1nc2ccccc2c2c1[nH]c(n2)C1CCCCC1 16722654
CHEMBL475346 2240 0 AA3R A3 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 410 3 2 3 7.2 Clc1ccc(cc1Cl)Nc1nc2ccccc2c2c1[nH]c(n2)C1CCCCC1 16722654
25191023 2241 0 AA3R A3 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 413 4 2 3 6.8 O=C(C1CCCCC1)Nc1cc(Nc2ccc(c(c2)Cl)Cl)nc2c1cccc2 19161279
9447 2241 0 AA3R A3 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 413 4 2 3 6.8 O=C(C1CCCCC1)Nc1cc(Nc2ccc(c(c2)Cl)Cl)nc2c1cccc2 19161279
CHEMBL472925 2241 0 AA3R A3 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 413 4 2 3 6.8 O=C(C1CCCCC1)Nc1cc(Nc2ccc(c(c2)Cl)Cl)nc2c1cccc2 19161279
154730931 170684 0 AA3R A3 receptor Human 10.2 pEC50 = 10.2 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 462 4 3 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)c4cccc(Cl)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL4464176 170684 0 AA3R A3 receptor Human 10.2 pEC50 = 10.2 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 462 4 3 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)c4cccc(Cl)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
3035850 898 55 AA3R A3 receptor Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm4007966
457 898 55 AA3R A3 receptor Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm4007966
CHEMBL431733 898 55 AA3R A3 receptor Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm4007966
DB12885 898 55 AA3R A3 receptor Mouse 9.8 pEC50 = 9.8 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm4007966
154730931 170684 0 AA3R A3 receptor Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 462 4 3 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)c4cccc(Cl)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL4464176 170684 0 AA3R A3 receptor Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 462 4 3 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)c4cccc(Cl)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
57523714 76102 0 AA3R A3 receptor Human 9.7 pEC50 = 9.7 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 528 5 4 8 2.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064653 76102 0 AA3R A3 receptor Human 9.7 pEC50 = 9.7 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 528 5 4 8 2.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
118730350 117390 0 AA3R A3 receptor Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 424 3 4 9 0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cccs4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407783 117390 0 AA3R A3 receptor Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 424 3 4 9 0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cccs4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
57523251 76108 0 AA3R A3 receptor Human 9.6 pEC50 = 9.6 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 604 6 4 8 4.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(-c5ccccc5)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064660 76108 0 AA3R A3 receptor Human 9.6 pEC50 = 9.6 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 604 6 4 8 4.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(-c5ccccc5)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
123683 2931 50 AA3R A3 receptor Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
422 2931 50 AA3R A3 receptor Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
CHEMBL119709 2931 50 AA3R A3 receptor Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
DB05511 2931 50 AA3R A3 receptor Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
154730931 170684 0 AA3R A3 receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 462 4 3 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)c4cccc(Cl)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL4464176 170684 0 AA3R A3 receptor Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 462 4 3 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(N(C)c4cccc(Cl)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
57523213 2514 13 AA3R A3 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
8421 2514 13 AA3R A3 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
CHEMBL2064657 2514 13 AA3R A3 receptor Human 9.5 pEC50 = 9.5 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
91799687 117380 0 AA3R A3 receptor Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 420 3 4 10 -0.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cnccn4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407774 117380 0 AA3R A3 receptor Mouse 9.5 pEC50 = 9.5 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 420 3 4 10 -0.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cnccn4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
123683 2931 50 AA3R A3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
422 2931 50 AA3R A3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
CHEMBL119709 2931 50 AA3R A3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
DB05511 2931 50 AA3R A3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
118730350 117390 0 AA3R A3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 424 3 4 9 0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cccs4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407783 117390 0 AA3R A3 receptor Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 424 3 4 9 0.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cccs4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
3035850 898 55 AA3R A3 receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.5b01998
457 898 55 AA3R A3 receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.5b01998
CHEMBL431733 898 55 AA3R A3 receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.5b01998
DB12885 898 55 AA3R A3 receptor Mouse 9.3 pEC50 = 9.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.5b01998
57523714 76102 0 AA3R A3 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 528 5 4 8 2.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064653 76102 0 AA3R A3 receptor Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 528 5 4 8 2.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
123683 2931 50 AA3R A3 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
422 2931 50 AA3R A3 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
CHEMBL119709 2931 50 AA3R A3 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
DB05511 2931 50 AA3R A3 receptor Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
118730351 117391 0 AA3R A3 receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 458 3 4 9 1.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407784 117391 0 AA3R A3 receptor Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at mouse A3 adenosine receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 458 3 4 9 1.0 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4ccc(Cl)s4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
123683 2931 50 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
422 2931 50 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
CHEMBL119709 2931 50 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
DB05511 2931 50 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.8b00435
76336527 105344 0 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 5 5 10 0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(Cl)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133161 105344 0 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 5 5 10 0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(Cl)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
9893136 98061 0 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 527 5 4 8 2.0 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
CHEMBL27809 98061 0 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 527 5 4 8 2.0 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
9805713 162021 0 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 493 5 4 8 1.3 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
CHEMBL417292 162021 0 AA3R A3 receptor Human 9.2 pEC50 = 9.2 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 493 5 4 8 1.3 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
57523714 76102 0 AA3R A3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 528 5 4 8 2.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064653 76102 0 AA3R A3 receptor Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 528 5 4 8 2.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
123683 2931 50 AA3R A3 receptor Human 9.0 pEC50 = 9 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm0255724
422 2931 50 AA3R A3 receptor Human 9.0 pEC50 = 9 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm0255724
CHEMBL119709 2931 50 AA3R A3 receptor Human 9.0 pEC50 = 9 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm0255724
DB05511 2931 50 AA3R A3 receptor Human 9.0 pEC50 = 9 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm0255724
3035850 898 55 AA3R A3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMPAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1016/j.bmcl.2008.01.070
457 898 55 AA3R A3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMPAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1016/j.bmcl.2008.01.070
CHEMBL431733 898 55 AA3R A3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMPAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1016/j.bmcl.2008.01.070
DB12885 898 55 AA3R A3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMPAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1016/j.bmcl.2008.01.070
57523213 2514 13 AA3R A3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/jm300396n
8421 2514 13 AA3R A3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/jm300396n
CHEMBL2064657 2514 13 AA3R A3 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassayAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 30 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/jm300396n
44359213 118702 0 AA3R A3 receptor Human 8.9 pEC50 = 8.9 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 352 3 4 8 -0.5 CNC(=O)C12CC1C(n1cnc3c(NC)nc(Cl)nc31)C(O)C2O 10.1021/jm020211+
CHEMBL345076 118702 0 AA3R A3 receptor Human 8.9 pEC50 = 8.9 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 352 3 4 8 -0.5 CNC(=O)C12CC1C(n1cnc3c(NC)nc(Cl)nc31)C(O)C2O 10.1021/jm020211+
91799687 117380 0 AA3R A3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 420 3 4 10 -0.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cnccn4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
CHEMBL3407774 117380 0 AA3R A3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 minsAgonist activity at human recombinant A3 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 15 mins
ChEMBL 420 3 4 10 -0.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(C#Cc4cnccn4)nc31)[C@H](O)[C@@H]2O 10.1021/jm501021n
122188579 122408 0 AA3R A3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP productionAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP production
ChEMBL 471 4 4 8 2.0 CCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.5b00150
CHEMBL3612940 122408 0 AA3R A3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP productionAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP production
ChEMBL 471 4 4 8 2.0 CCNc1cc(C#Cc2ccc(Cl)s2)nc2c1ncn2[C@H]1[C@H](O)[C@H](O)[C@]2(C(=O)NC)C[C@H]12 10.1021/acsmedchemlett.5b00150
76311194 105327 0 AA3R A3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 525 5 5 10 -0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133078 105327 0 AA3R A3 receptor Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 525 5 5 10 -0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
44387284 131625 0 AA3R A3 receptor Human 8.8 pEC50 = 8.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 568 8 6 11 -0.4 CNCC(=O)NC[C@H]1O[C@@H](n2cnc3c(NCc4ccc(N)c(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm020211+
CHEMBL369744 131625 0 AA3R A3 receptor Human 8.8 pEC50 = 8.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 568 8 6 11 -0.4 CNCC(=O)NC[C@H]1O[C@@H](n2cnc3c(NCc4ccc(N)c(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm020211+
44436082 147118 0 AA3R A3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
ChEMBL 524 6 3 9 1.1 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](OC)[C@@H]1O 10.1016/j.bmc.2007.05.056
CHEMBL393362 147118 0 AA3R A3 receptor Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
ChEMBL 524 6 3 9 1.1 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](OC)[C@@H]1O 10.1016/j.bmc.2007.05.056
3086599 858 30 AA3R A3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
375 858 30 AA3R A3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
424 858 30 AA3R A3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
CHEMBL331372 858 30 AA3R A3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
76336525 105337 0 AA3R A3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 337 4 5 10 -1.8 CCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133154 105337 0 AA3R A3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 337 4 5 10 -1.8 CCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
76336526 105338 0 AA3R A3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 351 5 5 10 -1.4 CCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133155 105338 0 AA3R A3 receptor Human 8.0 pEC50 = 8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 351 5 5 10 -1.4 CCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
76314797 105330 0 AA3R A3 receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 5 5 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(NC)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133081 105330 0 AA3R A3 receptor Human 7.0 pEC50 = 7 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 5 5 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(NC)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
57523253 76083 0 AA3R A3 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cc5cccc6ccc7cccc4c7c65)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064634 76083 0 AA3R A3 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cc5cccc6ccc7cccc4c7c65)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
118732979 117770 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414945 117770 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
2844 269 95 AA3R A3 receptor Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
60961 269 95 AA3R A3 receptor Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
90 269 95 AA3R A3 receptor Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
CHEMBL477 269 95 AA3R A3 receptor Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
DB00640 269 95 AA3R A3 receptor Human 6.0 pEC50 = 6.0 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
377 2590 39 AA3R A3 receptor Human 5.0 pEC50 = 5.0 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
425 2590 39 AA3R A3 receptor Human 5.0 pEC50 = 5.0 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
448222 2590 39 AA3R A3 receptor Human 5.0 pEC50 = 5.0 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
CHEMBL464859 2590 39 AA3R A3 receptor Human 5.0 pEC50 = 5.0 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
11574573 193102 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 386 5 4 8 0.5 CCCCC#Cc1nc(N)c2ncn([C@@H]3C[C@H](NC(=O)CC)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2009.11.131
CHEMBL591999 193102 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 386 5 4 8 0.5 CCCCC#Cc1nc(N)c2ncn([C@@H]3C[C@H](NC(=O)CC)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2009.11.131
137661670 158511 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 509 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4100130 158511 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 509 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
23643558 85402 0 AA3R A3 receptor Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 498 5 0 6 6.1 COc1ccc(-n2cc3c(n2)c(N(C(=O)c2ccccc2)C(=O)c2ccccc2)nc2ccccc23)cc1 10.1021/jm070123v
CHEMBL230854 85402 0 AA3R A3 receptor Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 498 5 0 6 6.1 COc1ccc(-n2cc3c(n2)c(N(C(=O)c2ccccc2)C(=O)c2ccccc2)nc2ccccc23)cc1 10.1021/jm070123v
45482870 191619 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 454 5 4 11 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NOC)nc(C#Cc4ccc(OC)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
CHEMBL573950 191619 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 454 5 4 11 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NOC)nc(C#Cc4ccc(OC)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
44579714 184307 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECAAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA
ChEMBL 497 4 3 7 2.6 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(I)c3)nc(Cl)nc21 10.1021/jm900426g
CHEMBL490605 184307 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECAAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA
ChEMBL 497 4 3 7 2.6 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(I)c3)nc(Cl)nc21 10.1021/jm900426g
137659441 158275 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4097468 158275 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
57523252 76109 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc5ccc6cccc7ccc4c5c67)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064661 76109 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc5ccc6cccc7ccc4c5c67)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
16115903 83609 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 424 4 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NOC)nc(C#Cc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
CHEMBL221206 83609 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 424 4 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NOC)nc(C#Cc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
44586227 187297 0 AA3R A3 receptor Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human adenosine A3 cells expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 cells expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 433 4 0 9 0.8 CS(=O)(=O)N(c1nc2ccccc2n2c(=O)n(-c3ccccc3)nc12)S(C)(=O)=O 10.1016/j.bmc.2008.04.039
CHEMBL519319 187297 0 AA3R A3 receptor Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human adenosine A3 cells expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 cells expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 433 4 0 9 0.8 CS(=O)(=O)N(c1nc2ccccc2n2c(=O)n(-c3ccccc3)nc12)S(C)(=O)=O 10.1016/j.bmc.2008.04.039
137661505 158670 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4101850 158670 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137650899 156387 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076003 156387 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
76325694 105342 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133159 105342 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
57524978 90596 0 AA3R A3 receptor Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 608 6 5 10 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(S(=O)(=O)O)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
CHEMBL2401954 90596 0 AA3R A3 receptor Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 608 6 5 10 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(S(=O)(=O)O)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
118732982 117773 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414948 117773 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
132991435 179928 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 558 8 5 12 0.8 O=C(NCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccc(S(=O)(=O)F)cc1 10.1021/acs.jmedchem.6b01561
CHEMBL4756472 179928 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 558 8 5 12 0.8 O=C(NCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccc(S(=O)(=O)F)cc1 10.1021/acs.jmedchem.6b01561
70695812 72703 0 AA3R A3 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human A3A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
CHEMBL2012686 72703 0 AA3R A3 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human A3A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 375 5 3 7 2.0 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NC(C3CC3)C3CC3)nc(Cl)nc21 10.1021/acs.jmedchem.8b01662
46230238 194489 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 595 12 6 10 3.0 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4c[nH]cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL601514 194489 0 AA3R A3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 595 12 6 10 3.0 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4c[nH]cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
10254700 197103 2 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
CHEMBL66393 197103 2 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
118732975 117766 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414941 117766 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
377 2590 39 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
425 2590 39 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
448222 2590 39 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
CHEMBL464859 2590 39 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
44232535 94931 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 538 8 5 9 1.7 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#CCCCC(=O)O)nc31)[C@H](O)[C@@H]2O 10.1016/j.bmcl.2008.04.001
CHEMBL257833 94931 0 AA3R A3 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 538 8 5 9 1.7 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#CCCCC(=O)O)nc31)[C@H](O)[C@@H]2O 10.1016/j.bmcl.2008.04.001
137657926 158942 0 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4105164 158942 0 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137646828 157186 0 AA3R A3 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 856 16 6 13 6.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCCCNC(=O)c4ccc(-c5sc(N)c(C(=O)c6ccccc6)c5-c5cccc(C(F)(F)F)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.8b00047
CHEMBL4085418 157186 0 AA3R A3 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 856 16 6 13 6.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCCCNC(=O)c4ccc(-c5sc(N)c(C(=O)c6ccccc6)c5-c5cccc(C(F)(F)F)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.8b00047
76318139 104968 0 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 355 5 3 7 1.7 CCCCC#Cc1nc(NCC)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125713 104968 0 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 355 5 3 7 1.7 CCCCC#Cc1nc(NCC)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
76329265 105341 0 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133158 105341 0 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
377 2590 39 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
425 2590 39 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
448222 2590 39 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
CHEMBL464859 2590 39 AA3R A3 receptor Human 7.8 pEC50 = 7.8 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
44598833 84 0 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 408 3 4 9 -0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(C#Cc1ccccc1)nc2NC 10.1021/jm900754g
5600 84 0 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 408 3 4 9 -0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(C#Cc1ccccc1)nc2NC 10.1021/jm900754g
CHEMBL574602 84 0 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 408 3 4 9 -0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(C#Cc1ccccc1)nc2NC 10.1021/jm900754g
377 2590 39 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9905965
425 2590 39 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9905965
448222 2590 39 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9905965
CHEMBL464859 2590 39 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9905965
44359420 32800 0 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 531 13 7 12 -2.2 NC(=O)CCNC1=C2N=CN([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C2N=CN1NCCc1ccc(CCC(=O)O)cc1 10.1021/jm020211+
CHEMBL141792 32800 0 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 531 13 7 12 -2.2 NC(=O)CCNC1=C2N=CN([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C2N=CN1NCCc1ccc(CCC(=O)O)cc1 10.1021/jm020211+
155562467 174374 0 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 497 6 4 9 2.5 COc1cc(CCNc2nc(C#Cc3ccccc3)nc3c2ncn3[C@H]2[C@H](O)[C@H](O)[C@@H]3C[C@@H]32)ccc1O 10.1021/acs.jmedchem.0c00235
CHEMBL4571380 174374 0 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 497 6 4 9 2.5 COc1cc(CCNc2nc(C#Cc3ccccc3)nc3c2ncn3[C@H]2[C@H](O)[C@H](O)[C@@H]3C[C@@H]32)ccc1O 10.1021/acs.jmedchem.0c00235
372 57 87 AA3R A3 receptor Human 5.8 pEC50 = 5.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm020211+
8974 57 87 AA3R A3 receptor Human 5.8 pEC50 = 5.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm020211+
CHEMBL285819 57 87 AA3R A3 receptor Human 5.8 pEC50 = 5.8 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm020211+
11533614 193171 0 AA3R A3 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 513 12 5 11 1.9 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NC(CC)CC)nc(NCCc4cn(CC)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL592541 193171 0 AA3R A3 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 513 12 5 11 1.9 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NC(CC)CC)nc(NCCc4cn(CC)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL4747947 179203 0 AA3R A3 receptor Rat 5.8 pEC50 = 5.8 Functional
Antagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 10 uM incubated for 2 hrs by fluorescence based assayAntagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 10 uM incubated for 2 hrs by fluorescence based assay
ChEMBL 524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
76318140 104974 0 AA3R A3 receptor Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 435 6 3 7 3.0 CCCCC#Cc1nc(NCc2cccc(F)c2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125719 104974 0 AA3R A3 receptor Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 435 6 3 7 3.0 CCCCC#Cc1nc(NCc2cccc(F)c2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
11584486 140108 0 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 525 6 5 9 0.3 NC(=O)N[C@@H]1[C@@H](CO)O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@@H]1O 10.1021/jm050968b
CHEMBL382194 140108 0 AA3R A3 receptor Human 6.8 pEC50 = 6.8 Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 525 6 5 9 0.3 NC(=O)N[C@@H]1[C@@H](CO)O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@@H]1O 10.1021/jm050968b
377 2590 39 AA3R A3 receptor Mouse 6.7 pEC50 = 6.7 Functional
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysisPartial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c00235
425 2590 39 AA3R A3 receptor Mouse 6.7 pEC50 = 6.7 Functional
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysisPartial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c00235
448222 2590 39 AA3R A3 receptor Mouse 6.7 pEC50 = 6.7 Functional
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysisPartial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c00235
CHEMBL464859 2590 39 AA3R A3 receptor Mouse 6.7 pEC50 = 6.7 Functional
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysisPartial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c00235
76314563 104969 0 AA3R A3 receptor Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 367 5 3 7 1.9 CCCCC#Cc1nc(NC2CC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125714 104969 0 AA3R A3 receptor Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 367 5 3 7 1.9 CCCCC#Cc1nc(NC2CC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
57523253 76083 0 AA3R A3 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cc5cccc6ccc7cccc4c7c65)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064634 76083 0 AA3R A3 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assayAgonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cc5cccc6ccc7cccc4c7c65)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
44598835 191536 0 AA3R A3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 426 3 4 9 -0.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(C#Cc4ccc(F)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
CHEMBL573269 191536 0 AA3R A3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 426 3 4 9 -0.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(C#Cc4ccc(F)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
57523252 76109 0 AA3R A3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc5ccc6cccc7ccc4c5c67)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064661 76109 0 AA3R A3 receptor Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc5ccc6cccc7ccc4c5c67)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
137647420 156883 0 AA3R A3 receptor Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4081876 156883 0 AA3R A3 receptor Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137638080 156021 0 AA3R A3 receptor Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4071338 156021 0 AA3R A3 receptor Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137648928 156588 0 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4078479 156588 0 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
71764235 90597 0 AA3R A3 receptor Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 608 6 5 10 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cccc(S(=O)(=O)O)c4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
CHEMBL2401955 90597 0 AA3R A3 receptor Mouse 8.6 pEC50 = 8.6 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 608 6 5 10 1.8 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cccc(S(=O)(=O)O)c4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
16109359 160952 0 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061279i
CHEMBL414055 160952 0 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061279i
132938348 157392 0 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as decrease in forskolin induced cAMP formation preincubated for 10 mins followed by forskolin challenge measured after 15 mins by AlphaScreen assayAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as decrease in forskolin induced cAMP formation preincubated for 10 mins followed by forskolin challenge measured after 15 mins by AlphaScreen assay
ChEMBL 574 5 4 8 0.5 CNC(=O)[C@H]1[Se][C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00241
CHEMBL4088081 157392 0 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as decrease in forskolin induced cAMP formation preincubated for 10 mins followed by forskolin challenge measured after 15 mins by AlphaScreen assayAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as decrease in forskolin induced cAMP formation preincubated for 10 mins followed by forskolin challenge measured after 15 mins by AlphaScreen assay
ChEMBL 574 5 4 8 0.5 CNC(=O)[C@H]1[Se][C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00241
45482610 191617 0 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonistic effect at human adenosine A3 receptor in CHO cellsAgonistic effect at human adenosine A3 receptor in CHO cells
ChEMBL 406 4 4 8 0.9 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC4CCCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm050726b
CHEMBL573937 191617 0 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Agonistic effect at human adenosine A3 receptor in CHO cellsAgonistic effect at human adenosine A3 receptor in CHO cells
ChEMBL 406 4 4 8 0.9 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NC4CCCC4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm050726b
3035850 898 55 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm020211+
457 898 55 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm020211+
CHEMBL431733 898 55 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm020211+
DB12885 898 55 AA3R A3 receptor Human 8.6 pEC50 = 8.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/jm020211+
127047826 139212 0 AA3R A3 receptor Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 403 2 3 7 0.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(C)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.5b01998
CHEMBL3800048 139212 0 AA3R A3 receptor Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 403 2 3 7 0.6 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(C)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.5b01998
16115616 165465 0 AA3R A3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 442 4 4 10 -0.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NOC)nc(C#Cc4ccc(F)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
CHEMBL427077 165465 0 AA3R A3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 442 4 4 10 -0.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NOC)nc(C#Cc4ccc(F)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
415 3430 7 AA3R A3 receptor Human 6.7 pEC50 = 6.7 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 10.1021/jm020211+
5312112 3430 7 AA3R A3 receptor Human 6.7 pEC50 = 6.7 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 10.1021/jm020211+
CHEMBL420705 3430 7 AA3R A3 receptor Human 6.7 pEC50 = 6.7 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 10.1021/jm020211+
45482874 191514 0 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 438 4 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(C#Cc4ccc(OC)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
CHEMBL573032 191514 0 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 438 4 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(C#Cc4ccc(OC)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
155537599 171483 0 AA3R A3 receptor Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 491 5 3 8 3.5 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCCc3ccccc3)nc(C#Cc3ccc(Cl)s3)nc21 10.1021/acs.jmedchem.0c00235
CHEMBL4475372 171483 0 AA3R A3 receptor Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 491 5 3 8 3.5 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCCc3ccccc3)nc(C#Cc3ccc(Cl)s3)nc21 10.1021/acs.jmedchem.0c00235
380 1207 42 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm020211+
657378 1207 42 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm020211+
CHEMBL68738 1207 42 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm020211+
57523251 76108 0 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 604 6 4 8 4.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(-c5ccccc5)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064660 76108 0 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 604 6 4 8 4.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(-c5ccccc5)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
137657841 158744 0 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4102750 158744 0 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
76332918 105335 0 AA3R A3 receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 7 4 10 0.4 CCN(CC)c1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
CHEMBL3133152 105335 0 AA3R A3 receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 7 4 10 0.4 CCN(CC)c1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
11699353 193170 0 AA3R A3 receptor Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 527 12 5 11 2.4 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NC(CC)CC)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL592540 193170 0 AA3R A3 receptor Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 527 12 5 11 2.4 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NC(CC)CC)nc(NCCc4cn(C(C)C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
10450691 98756 0 AA3R A3 receptor Human 4.6 pEC50 = 4.6 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 352 3 4 8 -0.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
CHEMBL283057 98756 0 AA3R A3 receptor Human 4.6 pEC50 = 4.6 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 352 3 4 8 -0.5 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
377 2590 39 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm020211+
425 2590 39 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm020211+
448222 2590 39 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm020211+
CHEMBL464859 2590 39 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm020211+
8975 99694 73 AA3R A3 receptor Human 5.6 pEC50 = 5.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 285 2 4 9 -1.8 Nc1nc(F)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm020211+
CHEMBL290077 99694 73 AA3R A3 receptor Human 5.6 pEC50 = 5.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 285 2 4 9 -1.8 Nc1nc(F)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm020211+
414 3180 23 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10.1021/jm020211+
93205 3180 23 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10.1021/jm020211+
CHEMBL139000 3180 23 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10.1021/jm020211+
11756182 78579 0 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 513 6 3 9 2.0 CSC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
CHEMBL2113427 78579 0 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 513 6 3 9 2.0 CSC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
76332686 104970 0 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 395 5 3 7 2.6 CCCCC#Cc1nc(NC2CCCC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125715 104970 0 AA3R A3 receptor Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 395 5 3 7 2.6 CCCCC#Cc1nc(NC2CCCC2)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
144852560 170097 0 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human A3AR expressed in CHO cells assessed as suppression of NECA-induced reduction in cAMP accumulationAntagonist activity at human A3AR expressed in CHO cells assessed as suppression of NECA-induced reduction in cAMP accumulation
ChEMBL 343 2 2 5 3.8 Clc1ccc(C#Cc2nc(NC3CCCC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
CHEMBL4455344 170097 0 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human A3AR expressed in CHO cells assessed as suppression of NECA-induced reduction in cAMP accumulationAntagonist activity at human A3AR expressed in CHO cells assessed as suppression of NECA-induced reduction in cAMP accumulation
ChEMBL 343 2 2 5 3.8 Clc1ccc(C#Cc2nc(NC3CCCC3)c3nc[nH]c3n2)s1 10.1039/C8MD00317C
137639588 156070 0 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccccc2C(=O)NCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4072009 156070 0 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccccc2C(=O)NCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137646655 156809 0 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 711 13 6 12 4.8 Nc1cc(-c2cccc(C(F)(F)F)c2)c(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4081224 156809 0 AA3R A3 receptor Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 711 13 6 12 4.8 Nc1cc(-c2cccc(C(F)(F)F)c2)c(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)s1 10.1021/acs.jmedchem.8b00047
2844 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
60961 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
90 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
CHEMBL477 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
DB00640 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
2844 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
60961 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
90 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
CHEMBL477 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
DB00640 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
2844 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
60961 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
90 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
CHEMBL477 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
DB00640 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A3 receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
2844 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
60961 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
90 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
CHEMBL477 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
DB00640 269 95 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
11068963 191711 1 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm900754g
CHEMBL574597 191711 1 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm900754g
377 2590 39 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
425 2590 39 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
448222 2590 39 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
CHEMBL464859 2590 39 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
44354130 23131 0 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 554 5 4 8 1.7 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)C(O)C2O 10.1021/jm020211+
CHEMBL133387 23131 0 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 554 5 4 8 1.7 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)C(O)C2O 10.1021/jm020211+
71764237 90601 0 AA3R A3 receptor Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 508 6 4 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccccc4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
CHEMBL2402024 90601 0 AA3R A3 receptor Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISAAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA
ChEMBL 508 6 4 8 1.9 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCCc4ccccc4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/jm4007966
9828356 10249 4 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 528 8 4 12 1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cc(Cl)ccc4OCc4cc(C)no4)ncnc32)[C@H](O)[C@@H]1N 10.1021/jm0255724
CHEMBL116878 10249 4 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptorInhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
ChEMBL 528 8 4 12 1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cc(Cl)ccc4OCc4cc(C)no4)ncnc32)[C@H](O)[C@@H]1N 10.1021/jm0255724
137642036 157330 0 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4087306 157330 0 AA3R A3 receptor Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
123683 2931 50 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm020211+
422 2931 50 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm020211+
CHEMBL119709 2931 50 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm020211+
DB05511 2931 50 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm020211+
23643659 91638 0 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 454 5 1 4 6.3 O=C(Nc1nc2ccccc2c2cn(-c3ccccc3)nc12)C(c1ccccc1)c1ccccc1 10.1021/jm070123v
CHEMBL242849 91638 0 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation
ChEMBL 454 5 1 4 6.3 O=C(Nc1nc2ccccc2c2cn(-c3ccccc3)nc12)C(c1ccccc1)c1ccccc1 10.1021/jm070123v
76329263 105328 0 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133079 105328 0 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
44563977 186850 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assayAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay
ChEMBL 574 6 4 10 1.7 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm8014052
CHEMBL515442 186850 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assayAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay
ChEMBL 574 6 4 10 1.7 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm8014052
137651747 156664 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4079433 156664 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
76329266 105343 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133160 105343 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
56627882 117762 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414937 117762 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
57523253 76083 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cc5cccc6ccc7cccc4c7c65)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064634 76083 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4cc5cccc6ccc7cccc4c7c65)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
10046345 191513 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 397 4 4 10 -0.2 CONc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm900754g
CHEMBL573030 191513 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 397 4 4 10 -0.2 CONc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm900754g
118732980 117771 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414946 117771 0 AA3R A3 receptor Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
137652475 156331 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 829 16 6 13 6.5 Nc1sc(-c2ccc(C(=O)NCCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4075186 156331 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 829 16 6 13 6.5 Nc1sc(-c2ccc(C(=O)NCCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137641858 157485 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 696 13 5 11 5.3 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2sccc2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
CHEMBL4089092 157485 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 696 13 5 11 5.3 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2sccc2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
377 2590 39 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2008.04.001
425 2590 39 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2008.04.001
448222 2590 39 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2008.04.001
CHEMBL464859 2590 39 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2008.04.001
CHEMBL4741079 178631 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 414 6 4 11 0.8 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CN=C=S)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
46230239 192736 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 649 13 5 11 4.1 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C5CC5)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
CHEMBL589348 192736 0 AA3R A3 receptor Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 649 13 5 11 4.1 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C5CC5)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
42626221 178548 7 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 412 4 1 8 2.7 COc1ccc(-n2nc3c(NC(=O)c4ccccc4)nc4ncccc4n3c2=O)cc1 10.1021/jm8014876
CHEMBL474016 178548 7 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 412 4 1 8 2.7 COc1ccc(-n2nc3c(NC(=O)c4ccccc4)nc4ncccc4n3c2=O)cc1 10.1021/jm8014876
11957503 191658 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccc(I)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
CHEMBL574181 191658 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccc(I)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
118732981 117772 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 495 5 3 12 2.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414947 117772 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 495 5 3 12 2.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
98567 187370 14 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP productionAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP production
ChEMBL 294 2 4 9 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/acsmedchemlett.5b00150
CHEMBL519809 187370 14 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP productionAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP production
ChEMBL 294 2 4 9 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/acsmedchemlett.5b00150
92208 141553 44 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 357 5 4 9 0.1 OC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
CHEMBL388757 141553 44 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 357 5 4 9 0.1 OC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
118732975 117766 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414941 117766 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
76329264 105334 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 6 5 10 -0.0 CCNc1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
CHEMBL3133151 105334 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 6 5 10 -0.0 CCNc1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1 10.1039/C3MD00364G
76311197 105339 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 365 6 5 10 -1.0 CCCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133156 105339 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 365 6 5 10 -1.0 CCCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
3035850 898 55 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.0c00235
457 898 55 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.0c00235
CHEMBL431733 898 55 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.0c00235
DB12885 898 55 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I 10.1021/acs.jmedchem.0c00235
9869857 66268 3 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1016/j.bmcl.2009.11.131
CHEMBL186113 66268 3 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1016/j.bmcl.2009.11.131
44579716 184308 0 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECAAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA
ChEMBL 449 4 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(Br)c3)nc(Cl)nc21 10.1021/jm900426g
CHEMBL490606 184308 0 AA3R A3 receptor Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECAAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA
ChEMBL 449 4 3 7 2.8 O[C@@H]1[C@H](O)[C@@H]2C[C@@H]2[C@H]1n1cnc2c(NCc3cccc(Br)c3)nc(Cl)nc21 10.1021/jm900426g
377 2590 39 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
425 2590 39 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
448222 2590 39 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
CHEMBL464859 2590 39 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cellsActivity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
136048802 139222 0 AA3R A3 receptor Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 507 4 4 8 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(/C=C(\O)c4ccccc4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.5b01998
CHEMBL3800106 139222 0 AA3R A3 receptor Mouse 8.3 pEC50 = 8.3 Functional
Agonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassayAgonist activity at mouse adenosine A3 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forsolkin addition measured after 15 mins by immunoassay
ChEMBL 507 4 4 8 2.3 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(/C=C(\O)c4ccccc4)nc(C#Cc4ccccc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.5b01998
137649841 156613 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 656 14 5 12 3.8 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cc(C(=O)c3ccccc3)cs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4078771 156613 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 656 14 5 12 3.8 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cc(C(=O)c3ccccc3)cs2)c1 10.1021/acs.jmedchem.8b00047
46230237 193034 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 609 12 5 11 3.0 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL591423 193034 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 609 12 5 11 3.0 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(C)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
46230236 193027 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 623 13 5 11 3.5 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(CC)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL591356 193027 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 623 13 5 11 3.5 CCC(=O)N[C@H]1C[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4cn(CC)cn4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2009.11.131
132991434 179092 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 564 8 6 12 2.4 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CNC(=S)Nc5ccc(N=C=S)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
CHEMBL4746617 179092 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 564 8 6 12 2.4 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CNC(=S)Nc5ccc(N=C=S)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
137650221 156439 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076561 156439 0 AA3R A3 receptor Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137650918 156429 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 671 14 6 13 3.4 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076495 156429 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 671 14 6 13 3.4 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137650461 156440 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 857 16 6 13 6.4 CC(=O)Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076565 156440 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 857 16 6 13 6.4 CC(=O)Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
46230151 193130 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 464 7 5 11 0.8 Cc1cnn([C@H]2C[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
CHEMBL592246 193130 0 AA3R A3 receptor Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 464 7 5 11 0.8 Cc1cnn([C@H]2C[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
76321824 104967 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 341 4 3 7 1.3 CCCCC#Cc1nc(NC)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
CHEMBL3125712 104967 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Functional
Partial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminasePartial agonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as stimulation of forskolin-induced intracellular cAMP production preincubated for 45 mins followed by forskolin challenge measured after 15 mins by liquid scintillation counting analysis in presence of rolipram and adenosine deaminase
ChEMBL 341 4 3 7 1.3 CCCCC#Cc1nc(NC)c2ncn([C@H]3[C@H](O)[C@H](O)[C@@H]4C[C@@H]43)c2n1 10.1021/jm4015313
44436080 87972 0 AA3R A3 receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
ChEMBL 308 3 3 9 -1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](OC)[C@@H]1O 10.1016/j.bmc.2007.05.056
CHEMBL235742 87972 0 AA3R A3 receptor Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
ChEMBL 308 3 3 9 -1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](OC)[C@@H]1O 10.1016/j.bmc.2007.05.056
44598836 191776 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 409 3 4 10 -1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(C#Cc4ccccn4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
CHEMBL575027 191776 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 409 3 4 10 -1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(C#Cc4ccccn4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
10407895 78572 0 AA3R A3 receptor Human 6.3 pEC50 = 6.3 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 387 6 3 9 1.4 CSC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
CHEMBL2113420 78572 0 AA3R A3 receptor Human 6.3 pEC50 = 6.3 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 387 6 3 9 1.4 CSC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm981090+
46230240 194490 0 AA3R A3 receptor Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 663 13 5 11 4.5 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C5CCC5)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
CHEMBL601515 194490 0 AA3R A3 receptor Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 663 13 5 11 4.5 CC(C)n1cnc(CCNc2nc(NCC(c3ccccc3)c3ccccc3)c3ncn([C@@H]4C[C@H](NC(=O)C5CCC5)[C@@H](O)[C@H]4O)c3n2)c1 10.1016/j.bmcl.2009.11.131
76322076 105329 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 489 7 5 10 1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133080 105329 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 489 7 5 10 1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76332919 105336 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 323 3 5 10 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133153 105336 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 323 3 5 10 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76318403 105340 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133157 105340 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
57523213 2514 13 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
8421 2514 13 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
CHEMBL2064657 2514 13 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
10254700 197103 2 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9905965
CHEMBL66393 197103 2 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9905965
CHEMBL4747947 179203 0 AA3R A3 receptor Rat 8.3 pEC50 = 8.3 Functional
Antagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 2 hrs by fluorescence based assayAntagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 2 hrs by fluorescence based assay
ChEMBL 524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
118732974 117765 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414940 117765 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
44359364 30225 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 520 5 4 8 1.1 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)ncnc31)C(O)C2O 10.1021/jm020211+
CHEMBL139417 30225 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 520 5 4 8 1.1 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)ncnc31)C(O)C2O 10.1021/jm020211+
9996279 109627 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Effective concentration for inhibition of NECA-stimulated [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cellsEffective concentration for inhibition of NECA-stimulated [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells
ChEMBL 323 2 1 7 1.2 O=c1[nH]c2ccccc2n2c(=O)n(-c3ccc([N+](=O)[O-])cc3)nc12 10.1021/jm031136l
CHEMBL324095 109627 0 AA3R A3 receptor Human 8.3 pEC50 = 8.3 Functional
Effective concentration for inhibition of NECA-stimulated [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cellsEffective concentration for inhibition of NECA-stimulated [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells
ChEMBL 323 2 1 7 1.2 O=c1[nH]c2ccccc2n2c(=O)n(-c3ccc([N+](=O)[O-])cc3)nc12 10.1021/jm031136l
118732974 117765 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414940 117765 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
16115614 84182 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 425 4 4 11 -1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NOC)nc(C#Cc4ccccn4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
CHEMBL223514 84182 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric methodAgonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method
ChEMBL 425 4 4 11 -1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NOC)nc(C#Cc4ccccn4)nc32)[C@H](O)[C@@H]1O 10.1021/jm900754g
137641990 157257 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4086325 157257 0 AA3R A3 receptor Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
9850648 97458 0 AA3R A3 receptor Human 5.3 pEC50 = 5.3 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 554 5 4 8 1.7 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
CHEMBL27376 97458 0 AA3R A3 receptor Human 5.3 pEC50 = 5.3 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 554 5 4 8 1.7 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
CHEMBL4747947 179203 0 AA3R A3 receptor Rat 7.3 pEC50 = 7.3 Functional
Antagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 3 uM incubated for 2 hrs by fluorescence based assayAntagonist activity at rat A3AR expressed in CHO cells assessed as reduction in NECA-induced inhibition of forskolin-stimulated cAMP accumulation at 3 uM incubated for 2 hrs by fluorescence based assay
ChEMBL 524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
137642153 157546 0 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4089741 157546 0 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
118732972 117763 0 AA3R A3 receptor Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414938 117763 0 AA3R A3 receptor Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
118732978 117769 0 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414944 117769 0 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
3086599 858 30 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1016/j.bmcl.2009.11.131
375 858 30 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1016/j.bmcl.2009.11.131
424 858 30 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1016/j.bmcl.2009.11.131
CHEMBL331372 858 30 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1016/j.bmcl.2009.11.131
377 2590 39 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
425 2590 39 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
448222 2590 39 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
CHEMBL464859 2590 39 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
377 2590 39 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Binding
Agonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
425 2590 39 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Binding
Agonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
448222 2590 39 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Binding
Agonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
CHEMBL464859 2590 39 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Binding
Agonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
57523252 76109 0 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc5ccc6cccc7ccc4c5c67)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064661 76109 0 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 652 5 4 8 5.4 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc5ccc6cccc7ccc4c5c67)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
76325693 105331 0 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 5 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N(C)C)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133082 105331 0 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 405 5 4 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N(C)C)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
137653409 158213 0 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 567 12 6 12 2.2 Nc1ccc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4096796 158213 0 AA3R A3 receptor Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 567 12 6 12 2.2 Nc1ccc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)s1 10.1021/acs.jmedchem.8b00047
10256116 98382 0 AA3R A3 receptor Human 5.2 pEC50 = 5.2 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 520 5 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
CHEMBL280580 98382 0 AA3R A3 receptor Human 5.2 pEC50 = 5.2 Functional
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptorAgonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor
ChEMBL 520 5 4 8 1.1 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1016/s0960-894x(01)00213-x
155540779 171673 0 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 581 6 4 10 3.3 COc1cc(CCNc2nc(C#Cc3ccc(Br)s3)nc3c2ncn3[C@H]2[C@H](O)[C@H](O)[C@@H]3C[C@@H]32)ccc1O 10.1021/acs.jmedchem.0c00235
CHEMBL4483546 171673 0 AA3R A3 receptor Human 6.2 pEC50 = 6.2 Functional
Partial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assayPartial agonist activity at recombinant human A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins in presence of A2BAR blocker PSB-603 by Glo-sensor assay
ChEMBL 581 6 4 10 3.3 COc1cc(CCNc2nc(C#Cc3ccc(Br)s3)nc3c2ncn3[C@H]2[C@H](O)[C@H](O)[C@@H]3C[C@@H]32)ccc1O 10.1021/acs.jmedchem.0c00235
137661132 158351 0 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 491 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4098377 158351 0 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 491 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
118732973 117764 0 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414939 117764 0 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
57523213 2514 13 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
8421 2514 13 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
CHEMBL2064657 2514 13 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
ChEMBL 564 5 4 8 2.8 CNC(=O)[C@@]12C[C@@H]1[C@H]([C@@H]([C@@H]2O)O)n1cnc2c1nc(C#Cc1ccc(c(c1)F)F)nc2NCc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00435
57523251 76108 0 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 604 6 4 8 4.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(-c5ccccc5)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
CHEMBL2064660 76108 0 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assayAgonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay
ChEMBL 604 6 4 8 4.2 CNC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#Cc4ccc(-c5ccccc5)cc4)nc31)[C@H](O)[C@@H]2O 10.1021/acs.jmedchem.8b00435
118732977 117768 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 461 5 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414943 117768 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 461 5 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
11662965 194206 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 478 8 5 11 1.1 CCc1cnn([C@H]2C[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
CHEMBL599387 194206 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 478 8 5 11 1.1 CCc1cnn([C@H]2C[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)c1 10.1016/j.bmcl.2009.11.131
377 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
425 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
448222 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
CHEMBL464859 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assayActivity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm050968b
46230290 194974 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 552 13 5 13 2.1 CCC(CC)CNc1nc(NCCc2cn(CC)cn2)nc2c1ncn2[C@@H]1C[C@H](n2cc(CO)cn2)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2009.11.131
CHEMBL604591 194974 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assayAgonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
ChEMBL 552 13 5 13 2.1 CCC(CC)CNc1nc(NCCc2cn(CC)cn2)nc2c1ncn2[C@@H]1C[C@H](n2cc(CO)cn2)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2009.11.131
71657835 158911 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4104819 158911 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
380 1207 42 AA3R A3 receptor Human 5.1 pEC50 = 5.1 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm9905965
657378 1207 42 AA3R A3 receptor Human 5.1 pEC50 = 5.1 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm9905965
CHEMBL68738 1207 42 AA3R A3 receptor Human 5.1 pEC50 = 5.1 Functional
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm9905965
11962166 77286 0 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Functional
Inhibition of isoproterenol-induced increase of cAMP in HEK293 cell expressing human adenosine A3 receptorInhibition of isoproterenol-induced increase of cAMP in HEK293 cell expressing human adenosine A3 receptor
ChEMBL 559 8 5 12 -0.8 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cc(Cl)ccc4OCC(=O)N4CCNCC4)ncnc32)[C@H](O)[C@@H]1N 10.1016/j.bmcl.2006.01.088
CHEMBL209352 77286 0 AA3R A3 receptor Human 8.1 pEC50 = 8.1 Functional
Inhibition of isoproterenol-induced increase of cAMP in HEK293 cell expressing human adenosine A3 receptorInhibition of isoproterenol-induced increase of cAMP in HEK293 cell expressing human adenosine A3 receptor
ChEMBL 559 8 5 12 -0.8 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cc(Cl)ccc4OCC(=O)N4CCNCC4)ncnc32)[C@H](O)[C@@H]1N 10.1016/j.bmcl.2006.01.088
44359214 116014 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 311 2 4 8 -0.7 Nc1nc(Cl)nc2c1ncn2C1C(O)C(O)C2(CO)CC12 10.1021/jm020211+
CHEMBL337602 116014 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 311 2 4 8 -0.7 Nc1nc(Cl)nc2c1ncn2C1C(O)C(O)C2(CO)CC12 10.1021/jm020211+
11743031 29423 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 423 8 3 10 -0.7 CCCCn1c(=O)c2c(ncn2[C@@H]2O[C@H](C(=O)NC)[C@@H](O)[C@H]2O)n(CCCC)c1=O 10.1021/jm020211+
CHEMBL138746 29423 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 423 8 3 10 -0.7 CCCCn1c(=O)c2c(ncn2[C@@H]2O[C@H](C(=O)NC)[C@@H](O)[C@H]2O)n(CCCC)c1=O 10.1021/jm020211+
118732976 117767 0 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 427 5 3 12 0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414942 117767 0 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 427 5 3 12 0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
137643164 157279 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4086624 157279 0 AA3R A3 receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1 10.1021/acs.jmedchem.8b00047
377 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cellsEffective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031136l
425 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cellsEffective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031136l
448222 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cellsEffective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031136l
CHEMBL464859 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cellsEffective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031136l
10254700 197103 2 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm020211+
CHEMBL66393 197103 2 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptorEffect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm020211+
377 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm981090+
425 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm981090+
448222 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm981090+
CHEMBL464859 2590 39 AA3R A3 receptor Human 7.1 pEC50 = 7.1 Functional
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptorEffective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm981090+
137636099 155016 0 AA3R A3 receptor Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 535 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4059961 155016 0 AA3R A3 receptor Human 8.0 pEC50 = 8.0 Functional
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
ChEMBL 535 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
118732971 117761 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414936 117761 0 AA3R A3 receptor Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activityAntagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
ChEMBL 333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
123683 2931 50 AA3R A3 receptor Human 10.8 pIC50 = 10.8 Functional
Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
422 2931 50 AA3R A3 receptor Human 10.8 pIC50 = 10.8 Functional
Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
CHEMBL119709 2931 50 AA3R A3 receptor Human 10.8 pIC50 = 10.8 Functional
Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
DB05511 2931 50 AA3R A3 receptor Human 10.8 pIC50 = 10.8 Functional
Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
123683 2931 50 AA3R A3 receptor Human 10.7 pIC50 = 10.7 Functional
Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
422 2931 50 AA3R A3 receptor Human 10.7 pIC50 = 10.7 Functional
Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
CHEMBL119709 2931 50 AA3R A3 receptor Human 10.7 pIC50 = 10.7 Functional
Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
DB05511 2931 50 AA3R A3 receptor Human 10.7 pIC50 = 10.7 Functional
Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
123683 2931 50 AA3R A3 receptor Human 10.6 pIC50 = 10.6 Functional
Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
422 2931 50 AA3R A3 receptor Human 10.6 pIC50 = 10.6 Functional
Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
CHEMBL119709 2931 50 AA3R A3 receptor Human 10.6 pIC50 = 10.6 Functional
Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
DB05511 2931 50 AA3R A3 receptor Human 10.6 pIC50 = 10.6 Functional
Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
123683 2931 50 AA3R A3 receptor Human 10.6 pIC50 = 10.6 Functional
Agonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
422 2931 50 AA3R A3 receptor Human 10.6 pIC50 = 10.6 Functional
Agonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
CHEMBL119709 2931 50 AA3R A3 receptor Human 10.6 pIC50 = 10.6 Functional
Agonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
DB05511 2931 50 AA3R A3 receptor Human 10.6 pIC50 = 10.6 Functional
Agonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
123683 2931 50 AA3R A3 receptor Human 10.3 pIC50 = 10.3 Functional
Agonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
422 2931 50 AA3R A3 receptor Human 10.3 pIC50 = 10.3 Functional
Agonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
CHEMBL119709 2931 50 AA3R A3 receptor Human 10.3 pIC50 = 10.3 Functional
Agonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
DB05511 2931 50 AA3R A3 receptor Human 10.3 pIC50 = 10.3 Functional
Agonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
123683 2931 50 AA3R A3 receptor Human 10.3 pIC50 = 10.3 Functional
Agonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
422 2931 50 AA3R A3 receptor Human 10.3 pIC50 = 10.3 Functional
Agonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
CHEMBL119709 2931 50 AA3R A3 receptor Human 10.3 pIC50 = 10.3 Functional
Agonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
DB05511 2931 50 AA3R A3 receptor Human 10.3 pIC50 = 10.3 Functional
Agonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/acs.jmedchem.9b01164
46237929 8687 0 AA3R A3 receptor Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at adenosine A3 receptor in human U87MG cells assessed as inhibition of Cl-IB-MECA-mediated ERK1/2 phosphorylation after 30 mins by ELISAAntagonist activity at adenosine A3 receptor in human U87MG cells assessed as inhibition of Cl-IB-MECA-mediated ERK1/2 phosphorylation after 30 mins by ELISA
ChEMBL 359 4 1 6 3.3 COc1ccc(C(=O)Nc2nc(-c3ccccc3)nc3nn(C)cc23)cc1 10.1021/jm901785w
CHEMBL1098108 8687 0 AA3R A3 receptor Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at adenosine A3 receptor in human U87MG cells assessed as inhibition of Cl-IB-MECA-mediated ERK1/2 phosphorylation after 30 mins by ELISAAntagonist activity at adenosine A3 receptor in human U87MG cells assessed as inhibition of Cl-IB-MECA-mediated ERK1/2 phosphorylation after 30 mins by ELISA
ChEMBL 359 4 1 6 3.3 COc1ccc(C(=O)Nc2nc(-c3ccccc3)nc3nn(C)cc23)cc1 10.1021/jm901785w
127036560 136737 0 AA3R A3 receptor Human 10.0 pIC50 = 10.0 Functional
Antagonist activity at human A3 receptor expressed in CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by scintillation counting methodAntagonist activity at human A3 receptor expressed in CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by scintillation counting method
ChEMBL 427 5 1 7 4.8 COc1ccc(C(=O)Nc2nc(-c3cccs3)nc3cn(-c4ccccc4)nc23)cc1 10.1016/j.ejmech.2015.11.015
CHEMBL3754229 136737 0 AA3R A3 receptor Human 10.0 pIC50 = 10.0 Functional
Antagonist activity at human A3 receptor expressed in CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by scintillation counting methodAntagonist activity at human A3 receptor expressed in CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by scintillation counting method
ChEMBL 427 5 1 7 4.8 COc1ccc(C(=O)Nc2nc(-c3cccs3)nc3cn(-c4ccccc4)nc23)cc1 10.1016/j.ejmech.2015.11.015
123683 2931 50 AA3R A3 receptor Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human adenosine A3 receptor by radioligand displacement assayBinding affinity to human adenosine A3 receptor by radioligand displacement assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2013.01.044
422 2931 50 AA3R A3 receptor Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human adenosine A3 receptor by radioligand displacement assayBinding affinity to human adenosine A3 receptor by radioligand displacement assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2013.01.044
CHEMBL119709 2931 50 AA3R A3 receptor Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human adenosine A3 receptor by radioligand displacement assayBinding affinity to human adenosine A3 receptor by radioligand displacement assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2013.01.044
DB05511 2931 50 AA3R A3 receptor Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human adenosine A3 receptor by radioligand displacement assayBinding affinity to human adenosine A3 receptor by radioligand displacement assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2013.01.044
11611903 82448 0 AA3R A3 receptor Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counterAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counter
ChEMBL 439 6 4 9 1.1 OC[C@H]1O[C@@H](n2cnc3c(C(F)(F)F)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300087j
CHEMBL2181968 82448 0 AA3R A3 receptor Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counterAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counter
ChEMBL 439 6 4 9 1.1 OC[C@H]1O[C@@H](n2cnc3c(C(F)(F)F)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300087j
CHEMBL4128926 160742 0 AA3R A3 receptor Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]AB-MECA from human recombinant adenosine A3 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]AB-MECA from human recombinant adenosine A3 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
377 2590 39 AA3R A3 receptor Human 9.7 pIC50 = 9.7 Functional
Agonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
425 2590 39 AA3R A3 receptor Human 9.7 pIC50 = 9.7 Functional
Agonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
448222 2590 39 AA3R A3 receptor Human 9.7 pIC50 = 9.7 Functional
Agonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
CHEMBL464859 2590 39 AA3R A3 receptor Human 9.7 pIC50 = 9.7 Functional
Agonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
135543600 15971 0 AA3R A3 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 336 6 1 6 3.4 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCC)cc3)nn12 10.1021/jm010570p
CHEMBL122819 15971 0 AA3R A3 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 336 6 1 6 3.4 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCC)cc3)nn12 10.1021/jm010570p
135512752 16065 0 AA3R A3 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 322 5 1 6 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3cccc(OC)c3)nn12 10.1021/jm010570p
CHEMBL123172 16065 0 AA3R A3 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 322 5 1 6 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3cccc(OC)c3)nn12 10.1021/jm010570p
135537639 16112 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 278 3 1 5 2.6 CCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
CHEMBL123465 16112 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 278 3 1 5 2.6 CCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
135457998 15939 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 292 4 1 5 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1016/j.bmcl.2004.03.010
CHEMBL122512 15939 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 292 4 1 5 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1016/j.bmcl.2004.03.010
135457998 15939 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 292 4 1 5 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
CHEMBL122512 15939 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 292 4 1 5 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
135443744 113719 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 310 4 1 5 3.1 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(F)cc3)nn12 10.1021/jm010570p
CHEMBL333415 113719 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 310 4 1 5 3.1 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(F)cc3)nn12 10.1021/jm010570p
135457998 15939 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cellsDisplacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 292 4 1 5 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1016/j.bmcl.2004.04.099
CHEMBL122512 15939 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cellsDisplacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 292 4 1 5 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1016/j.bmcl.2004.04.099
377 2590 39 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Functional
Agonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
425 2590 39 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Functional
Agonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
448222 2590 39 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Functional
Agonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
CHEMBL464859 2590 39 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Functional
Agonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
135479920 15959 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 306 4 1 5 3.3 CCCCc1nc2[nH]cnc2c2nc(-c3cccc(C)c3)nn12 10.1021/jm010570p
CHEMBL122685 15959 0 AA3R A3 receptor Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 306 4 1 5 3.3 CCCCc1nc2[nH]cnc2c2nc(-c3cccc(C)c3)nn12 10.1021/jm010570p
135542443 16475 0 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3Cl)nn12 10.1021/jm010570p
CHEMBL124788 16475 0 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3Cl)nn12 10.1021/jm010570p
377 2590 39 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Functional
Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
425 2590 39 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Functional
Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
448222 2590 39 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Functional
Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
CHEMBL464859 2590 39 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Functional
Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
135450786 15938 0 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 306 5 1 5 3.4 CCCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
CHEMBL122511 15938 0 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 306 5 1 5 3.4 CCCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
135444614 113997 0 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 350 7 1 6 3.8 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCCC)cc3)nn12 10.1021/jm010570p
CHEMBL333860 113997 0 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 350 7 1 6 3.8 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCCC)cc3)nn12 10.1021/jm010570p
135440607 113366 0 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 306 4 1 5 3.3 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C)cc3)nn12 10.1021/jm010570p
CHEMBL332742 113366 0 AA3R A3 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 306 4 1 5 3.3 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C)cc3)nn12 10.1021/jm010570p
9863617 72938 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Functional
Inhibitory concentration against human Adenosine A3 receptor mediated inhibition of cyclic AMP in transfected CHO cellsInhibitory concentration against human Adenosine A3 receptor mediated inhibition of cyclic AMP in transfected CHO cells
ChEMBL 358 3 4 9 -0.4 CNC(=O)[C@H]1S[C@@H](n2cnc3c(NC)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm034098e
CHEMBL201706 72938 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Functional
Inhibitory concentration against human Adenosine A3 receptor mediated inhibition of cyclic AMP in transfected CHO cellsInhibitory concentration against human Adenosine A3 receptor mediated inhibition of cyclic AMP in transfected CHO cells
ChEMBL 358 3 4 9 -0.4 CNC(=O)[C@H]1S[C@@H](n2cnc3c(NC)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm034098e
135405211 14940 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(Cl)cc3)nn12 10.1021/jm010570p
CHEMBL121339 14940 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(Cl)cc3)nn12 10.1021/jm010570p
135447756 112136 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 312 2 1 5 3.3 c1ccc(-c2nc3c4[nH]cnc4nc(-c4ccccc4)n3n2)cc1 10.1021/jm010570p
CHEMBL330982 112136 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 312 2 1 5 3.3 c1ccc(-c2nc3c4[nH]cnc4nc(-c4ccccc4)n3n2)cc1 10.1021/jm010570p
135405211 14940 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Binding
Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cellsDisplacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(Cl)cc3)nn12 10.1016/j.bmcl.2004.04.099
CHEMBL121339 14940 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Binding
Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cellsDisplacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(Cl)cc3)nn12 10.1016/j.bmcl.2004.04.099
135475602 112107 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 264 2 1 5 2.2 CCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
CHEMBL330873 112107 0 AA3R A3 receptor Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 264 2 1 5 2.2 CCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
377 2590 39 AA3R A3 receptor Human 9.3 pIC50 = 9.3 Functional
Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysisAgonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
425 2590 39 AA3R A3 receptor Human 9.3 pIC50 = 9.3 Functional
Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysisAgonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
448222 2590 39 AA3R A3 receptor Human 9.3 pIC50 = 9.3 Functional
Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysisAgonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
CHEMBL464859 2590 39 AA3R A3 receptor Human 9.3 pIC50 = 9.3 Functional
Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysisAgonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
377 2590 39 AA3R A3 receptor Human 9.3 pIC50 = 9.3 Functional
Agonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
425 2590 39 AA3R A3 receptor Human 9.3 pIC50 = 9.3 Functional
Agonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
448222 2590 39 AA3R A3 receptor Human 9.3 pIC50 = 9.3 Functional
Agonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
CHEMBL464859 2590 39 AA3R A3 receptor Human 9.3 pIC50 = 9.3 Functional
Agonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
23656936 154089 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 425 4 1 7 3.6 COc1ccc(C(=O)Nc2nc3ccccc3n3c(=O)c(-c4ccc(C)cc4)nn23)cc1 10.1021/jm0708376
CHEMBL400812 154089 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 425 4 1 7 3.6 COc1ccc(C(=O)Nc2nc3ccccc3n3c(=O)c(-c4ccc(C)cc4)nn23)cc1 10.1021/jm0708376
377 2590 39 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
425 2590 39 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
448222 2590 39 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
CHEMBL464859 2590 39 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
123683 2931 50 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmc.2016.11.014
422 2931 50 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmc.2016.11.014
CHEMBL119709 2931 50 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmc.2016.11.014
DB05511 2931 50 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmc.2016.11.014
123683 2931 50 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cells
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmc.2016.03.006
422 2931 50 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cells
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmc.2016.03.006
CHEMBL119709 2931 50 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cells
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmc.2016.03.006
DB05511 2931 50 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cells
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmc.2016.03.006
11813713 72403 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Inhibitory concentration against human Adenosine A3 receptor mediated inhibition of cyclic AMP in transfected CHO cellsInhibitory concentration against human Adenosine A3 receptor mediated inhibition of cyclic AMP in transfected CHO cells
ChEMBL 560 5 4 9 1.8 CNC(=O)[C@H]1S[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm034098e
CHEMBL200732 72403 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Inhibitory concentration against human Adenosine A3 receptor mediated inhibition of cyclic AMP in transfected CHO cellsInhibitory concentration against human Adenosine A3 receptor mediated inhibition of cyclic AMP in transfected CHO cells
ChEMBL 560 5 4 9 1.8 CNC(=O)[C@H]1S[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm034098e
135418454 16164 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counterAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counter
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1021/jm300087j
CHEMBL123705 16164 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counterAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counter
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1021/jm300087j
135418454 16164 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1016/j.bmcl.2004.03.010
CHEMBL123705 16164 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1016/j.bmcl.2004.03.010
135512751 16069 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 320 6 1 5 3.8 CCCCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
CHEMBL123203 16069 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 320 6 1 5 3.8 CCCCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12 10.1021/jm010570p
135418454 16164 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]CGS-21680 from human Adenosine A3 receptor expressed in HEK293 cells at 10000 nMDisplacement of [3H]CGS-21680 from human Adenosine A3 receptor expressed in HEK293 cells at 10000 nM
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1021/jm010570p
CHEMBL123705 16164 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]CGS-21680 from human Adenosine A3 receptor expressed in HEK293 cells at 10000 nMDisplacement of [3H]CGS-21680 from human Adenosine A3 receptor expressed in HEK293 cells at 10000 nM
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1021/jm010570p
135418454 16164 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cellsDisplacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1016/j.bmcl.2004.04.099
CHEMBL123705 16164 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cellsDisplacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK293 cells
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1016/j.bmcl.2004.04.099
377 2590 39 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
425 2590 39 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
448222 2590 39 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
CHEMBL464859 2590 39 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assayAgonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.9b01164
135409793 16111 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 335 5 1 6 3.1 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(N(C)C)cc3)nn12 10.1021/jm010570p
CHEMBL123462 16111 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells
ChEMBL 335 5 1 6 3.1 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(N(C)C)cc3)nn12 10.1021/jm010570p
9887859 112773 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counterAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counter
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300087j
CHEMBL118923 112773 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counterAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counter
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300087j
CHEMBL332091 112773 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counterAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation by scintillation counter
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300087j
9887859 112773 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Inhibitory activity against Human Adenosine A3 receptor expressed in CHO cellsInhibitory activity against Human Adenosine A3 receptor expressed in CHO cells
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
CHEMBL118923 112773 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Inhibitory activity against Human Adenosine A3 receptor expressed in CHO cellsInhibitory activity against Human Adenosine A3 receptor expressed in CHO cells
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
CHEMBL332091 112773 0 AA3R A3 receptor Human 9.2 pIC50 = 9.2 Binding
Inhibitory activity against Human Adenosine A3 receptor expressed in CHO cellsInhibitory activity against Human Adenosine A3 receptor expressed in CHO cells
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
46237928 8540 0 AA3R A3 receptor Human 9.1 pIC50 =