Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL475346 aa3r_human Human No - = Funct
UnclassifiedUnclassified
410 3 2 3 7.2 Clc1ccc(cc1Cl)Nc1nc2ccccc2c2c1[nH]c(n2)C1CCCCC1
CHEMBL472925 aa3r_human Human No - = Funct
UnclassifiedUnclassified
413 4 2 3 6.8 O=C(C1CCCCC1)Nc1cc(Nc2ccc(c(c2)Cl)Cl)nc2c1cccc2
CHEMBL4464176 aa3r_human Human No 10.2 EC50 = 0.1 nM Bind
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
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
CHEMBL431733 aa3r_mouse Mouse Yes 9.8 EC50 = 0.2 nM Funct
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
544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I
CHEMBL4464176 aa3r_human Human No 9.8 EC50 = 0.2 nM Bind
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
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
CHEMBL2064653 aa3r_human Human No 9.7 EC50 = 0.2 nM Bind
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
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
CHEMBL3407783 aa3r_mouse Mouse No 9.6 EC50 = 0.3 nM Funct
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
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
CHEMBL2064660 aa3r_human Human No 9.6 EC50 = 0.3 nM Bind
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
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
CHEMBL119709 aa3r_human Human Yes 9.6 EC50 = 0.3 nM Bind
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL4464176 aa3r_human Human No 9.6 EC50 = 0.3 nM Funct
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
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
CHEMBL2064657 aa3r_human Human Yes 9.5 EC50 = 0.3 nM Bind
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
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
CHEMBL3407774 aa3r_mouse Mouse No 9.5 EC50 = 0.3 nM Funct
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
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
CHEMBL119709 aa3r_human Human Yes 9.4 EC50 = 0.4 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL3407783 aa3r_human Human No 9.4 EC50 = 0.4 nM Funct
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
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
CHEMBL431733 aa3r_mouse Mouse Yes 9.3 EC50 = 0.5 nM Funct
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
544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I
CHEMBL2064653 aa3r_human Human No 9.3 EC50 = 0.5 nM Bind
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
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
CHEMBL119709 aa3r_human Human Yes 9.3 EC50 = 0.5 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL3407784 aa3r_mouse Mouse No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL119709 aa3r_human Human Yes 9.2 EC50 = 0.6 nM Bind
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL3133161 aa3r_human Human No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL27809 aa3r_human Human No 9.2 EC50 = 0.7 nM Funct
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
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
CHEMBL417292 aa3r_human Human No 9.2 EC50 = 0.7 nM Funct
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
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
CHEMBL2064653 aa3r_human Human No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL119709 aa3r_human Human Yes 9.0 EC50 = 1 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL431733 aa3r_human Human Yes 8.9 EC50 = 1.2 nM Funct
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
544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I
CHEMBL2064657 aa3r_human Human Yes 8.9 EC50 = 1.2 nM Funct
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
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
CHEMBL345076 aa3r_human Human No 8.9 EC50 = 1.4 nM Funct
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
352 3 4 8 -0.5 CNC(=O)C12CC1C(n1cnc3c(NC)nc(Cl)nc31)C(O)C2O
CHEMBL3407774 aa3r_human Human No 8.8 EC50 = 1.5 nM Funct
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
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
CHEMBL3612940 aa3r_human Human No 8.8 EC50 = 1.5 nM Funct
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
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
CHEMBL3133078 aa3r_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL369744 aa3r_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL393362 aa3r_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
524 6 3 9 1.1 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](OC)[C@@H]1O
CHEMBL331372 aa3r_human Human Yes 8.0 EC50 = 10 nM Funct
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
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
CHEMBL3133154 aa3r_human Human No 8.0 EC50 = 10 nM Funct
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
337 4 5 10 -1.8 CCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O
CHEMBL3133155 aa3r_human Human No 8.0 EC50 = 10 nM Funct
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
351 5 5 10 -1.4 CCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O
CHEMBL3133081 aa3r_human Human No 7.0 EC50 = 100 nM Funct
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
391 5 5 10 -0.4 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(NC)nc32)[C@H](O)[C@@H]1O
CHEMBL2064634 aa3r_human Human No 6.0 EC50 = 1000 nM Bind
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
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
CHEMBL3414945 aa3r_human Human No 7.0 EC50 = 104 nM Funct
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
437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL477 aa3r_human Human Yes 6.0 EC50 = 1040 nM Funct
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
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL464859 aa3r_human Human Yes 5.0 EC50 = 10400 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL591999 aa3r_human Human No 7.0 EC50 = 105 nM Bind
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
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
CHEMBL4100130 aa3r_human Human No 7.0 EC50 = 105 nM Funct
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
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
CHEMBL230854 aa3r_human Human No 8.0 EC50 = 11.2 nM Funct
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
498 5 0 6 6.1 COc1ccc(-n2cc3c(n2)c(N(C(=O)c2ccccc2)C(=O)c2ccccc2)nc2ccccc23)cc1
CHEMBL573950 aa3r_human Human No 7.0 EC50 = 112 nM Bind
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
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
CHEMBL490605 aa3r_human Human No 7.9 EC50 = 12 nM Funct
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
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
CHEMBL4097468 aa3r_human Human No 7.9 EC50 = 12.5 nM Funct
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
441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL2064661 aa3r_human Human No 7.9 EC50 = 12.6 nM Bind
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
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
CHEMBL221206 aa3r_human Human No 6.9 EC50 = 120 nM Bind
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
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
CHEMBL519319 aa3r_human Human No 4.9 EC50 = 12000 nM Funct
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
433 4 0 9 0.8 CS(=O)(=O)N(c1nc2ccccc2n2c(=O)n(-c3ccccc3)nc12)S(C)(=O)=O
CHEMBL4101850 aa3r_human Human No 6.9 EC50 = 123.0 nM Funct
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
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
CHEMBL4076003 aa3r_human Human No 6.9 EC50 = 125 nM Funct
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
413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL3133159 aa3r_human Human No 6.9 EC50 = 125.9 nM Funct
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
391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL2401954 aa3r_mouse Mouse No 7.9 EC50 = 13 nM Funct
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
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
CHEMBL3414948 aa3r_human Human No 7.9 EC50 = 13.3 nM Funct
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
583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL4756472 aa3r_human Human No 6.9 EC50 = 134.9 nM Funct
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
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
CHEMBL2012686 aa3r_human Human No 5.9 EC50 = 1370 nM Funct
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
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
CHEMBL601514 aa3r_human Human No 6.9 EC50 = 139 nM Bind
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
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
CHEMBL66393 aa3r_human Human Yes 7.9 EC50 = 14 nM Funct
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
483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL3414941 aa3r_human Human No 7.9 EC50 = 14.1 nM Funct
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
407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL464859 aa3r_human Human Yes 7.9 EC50 = 14.1 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL257833 aa3r_human Human No 7.9 EC50 = 14.1 nM Funct
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
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
CHEMBL4105164 aa3r_human Human No 7.8 EC50 = 14.4 nM Funct
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
421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL4085418 aa3r_human Human No 5.9 EC50 = 1412.5 nM Funct
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
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
CHEMBL3125713 aa3r_human Human No 7.8 EC50 = 15.5 nM Funct
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
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
CHEMBL3133158 aa3r_human Human No 7.8 EC50 = 15.9 nM Funct
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
377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL464859 aa3r_human Human Yes 7.8 EC50 = 15.9 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL574602 aa3r_human Human No 6.8 EC50 = 151 nM Bind
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
408 3 4 9 -0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(C#Cc1ccccc1)nc2NC
CHEMBL464859 aa3r_human Human Yes 6.8 EC50 = 155 nM Funct
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL141792 aa3r_human Human No 6.8 EC50 = 158 nM Funct
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
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
CHEMBL4571380 aa3r_human Human No 6.8 EC50 = 158 nM Funct
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
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
CHEMBL285819 aa3r_human Human Yes 5.8 EC50 = 1630 nM Funct
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
301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N
CHEMBL592541 aa3r_human Human No 5.8 EC50 = 1640 nM Bind
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
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
CHEMBL4747947 aa3r_rat Rat No 5.8 EC50 = 1720 nM Funct
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
524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1
CHEMBL3125719 aa3r_human Human No 7.7 EC50 = 18.9 nM Funct
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
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
CHEMBL382194 aa3r_human Human No 6.8 EC50 = 180 nM Funct
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
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
CHEMBL464859 aa3r_mouse Mouse Yes 6.7 EC50 = 188 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL3125714 aa3r_human Human No 7.7 EC50 = 19.8 nM Funct
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
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
CHEMBL2064634 aa3r_human Human No 7.7 EC50 = 20.0 nM Bind
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
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
CHEMBL573269 aa3r_human Human No 6.7 EC50 = 190 nM Bind
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
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
CHEMBL2064661 aa3r_human Human No 6.7 EC50 = 199.5 nM Funct
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
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
CHEMBL4081876 aa3r_human Human No 8.7 EC50 = 2.1 nM Funct
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
501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL4071338 aa3r_human Human No 8.7 EC50 = 2.2 nM Funct
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
457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL4078479 aa3r_human Human No 8.6 EC50 = 2.4 nM Funct
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
549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL2401955 aa3r_mouse Mouse No 8.6 EC50 = 2.6 nM Funct
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
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
CHEMBL414055 aa3r_human Human No 8.6 EC50 = 2.7 nM Funct
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
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
CHEMBL4088081 aa3r_human Human No 8.6 EC50 = 2.7 nM Funct
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
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
CHEMBL573937 aa3r_human Human No 8.6 EC50 = 2.8 nM Funct
Agonistic effect at human adenosine A3 receptor in CHO cellsAgonistic effect at human adenosine A3 receptor in CHO cells
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
CHEMBL431733 aa3r_human Human Yes 8.6 EC50 = 2.8 nM Funct
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
544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I
CHEMBL3800048 aa3r_mouse Mouse No 7.7 EC50 = 20.2 nM Funct
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
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
CHEMBL427077 aa3r_human Human No 6.7 EC50 = 210 nM Bind
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
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
CHEMBL420705 aa3r_human Human Yes 6.7 EC50 = 210 nM Funct
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
385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C
CHEMBL573032 aa3r_human Human No 6.6 EC50 = 240 nM Bind
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
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
CHEMBL4475372 aa3r_human Human No 5.6 EC50 = 2410 nM Funct
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
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
CHEMBL68738 aa3r_human Human Yes 6.6 EC50 = 242 nM Funct
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
335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1
CHEMBL2064660 aa3r_human Human No 7.6 EC50 = 25.1 nM Bind
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
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
CHEMBL4102750 aa3r_human Human No 7.6 EC50 = 25.4 nM Funct
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
475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL3133152 aa3r_human Human No 5.6 EC50 = 2511.9 nM Funct
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
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
CHEMBL592540 aa3r_human Human No 5.6 EC50 = 2520 nM Bind
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
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
CHEMBL283057 aa3r_human Human No 4.6 EC50 = 25500 nM Funct
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
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
CHEMBL464859 aa3r_human Human Yes 7.6 EC50 = 26 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL290077 aa3r_human Human Yes 5.6 EC50 = 2660 nM Funct
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
285 2 4 9 -1.8 Nc1nc(F)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL139000 aa3r_human Human Yes 7.6 EC50 = 27 nM Funct
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
385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C
CHEMBL2113427 aa3r_human Human No 7.6 EC50 = 27 nM Funct
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
513 6 3 9 2.0 CSC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL3125715 aa3r_human Human No 7.6 EC50 = 27.1 nM Funct
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
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
CHEMBL4455344 aa3r_human Human No 6.6 EC50 = 276 nM Funct
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
343 2 2 5 3.8 Clc1ccc(C#Cc2nc(NC3CCCC3)c3nc[nH]c3n2)s1
CHEMBL4072009 aa3r_human Human No 6.6 EC50 = 281.8 nM Funct
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
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
CHEMBL4081224 aa3r_human Human No 6.6 EC50 = 281.8 nM Funct
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
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
CHEMBL477 aa3r_human Human Yes 6.5 EC50 = 290 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cellsAgonist activity at human adenosine A3 receptor expressed in CHO cells
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL477 aa3r_human Human Yes 6.5 EC50 = 290 nM Funct
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
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL477 aa3r_human Human Yes 6.5 EC50 = 290 nM Funct
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
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL477 aa3r_human Human Yes 6.5 EC50 = 290 nM Funct
Agonist activity at human recombinant adenosine A3 receptor by cAMP assayAgonist activity at human recombinant adenosine A3 receptor by cAMP assay
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL574597 aa3r_human Human Yes 6.5 EC50 = 290 nM Bind
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
381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL464859 aa3r_human Human Yes 8.5 EC50 = 3.2 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL133387 aa3r_human Human No 8.5 EC50 = 3.3 nM Funct
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
554 5 4 8 1.7 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)C(O)C2O
CHEMBL2402024 aa3r_mouse Mouse No 8.5 EC50 = 3.3 nM Funct
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
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
CHEMBL116878 aa3r_human Human Yes 8.5 EC50 = 3.4 nM Funct
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
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
CHEMBL4087306 aa3r_human Human No 8.5 EC50 = 3.5 nM Funct
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
387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL119709 aa3r_human Human Yes 8.4 EC50 = 3.6 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL242849 aa3r_human Human No 8.4 EC50 = 3.8 nM Funct
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
454 5 1 4 6.3 O=C(Nc1nc2ccccc2c2cn(-c3ccccc3)nc12)C(c1ccccc1)c1ccccc1
CHEMBL3133079 aa3r_human Human No 8.4 EC50 = 4.0 nM Funct
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
413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL515442 aa3r_human Human No 7.5 EC50 = 31 nM Funct
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
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
CHEMBL4079433 aa3r_human Human No 7.5 EC50 = 31.5 nM Funct
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
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
CHEMBL3133160 aa3r_human Human No 7.5 EC50 = 31.6 nM Funct
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
399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL3414937 aa3r_human Human No 7.5 EC50 = 31.7 nM Funct
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
367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL2064634 aa3r_human Human No 6.5 EC50 = 316.2 nM Funct
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
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
CHEMBL573030 aa3r_human Human No 6.5 EC50 = 320 nM Bind
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
397 4 4 10 -0.2 CONc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
CHEMBL3414946 aa3r_human Human No 7.5 EC50 = 33.9 nM Funct
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
461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL4075186 aa3r_human Human No 6.5 EC50 = 331.1 nM Funct
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
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
CHEMBL4089092 aa3r_human Human No 6.5 EC50 = 346.7 nM Funct
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
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
CHEMBL464859 aa3r_human Human Yes 6.5 EC50 = 346.7 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL4741079 aa3r_human Human No 6.5 EC50 = 346.7 nM Funct
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
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
CHEMBL589348 aa3r_human Human No 6.5 EC50 = 357 nM Bind
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
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
CHEMBL474016 aa3r_human Human Yes 7.4 EC50 = 36.3 nM Funct
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
412 4 1 8 2.7 COc1ccc(-n2nc3c(NC(=O)c4ccccc4)nc4ncccc4n3c2=O)cc1
CHEMBL574181 aa3r_human Human No 6.4 EC50 = 363 nM Bind
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
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
CHEMBL3414947 aa3r_human Human No 7.4 EC50 = 37 nM Funct
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
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
CHEMBL519809 aa3r_human Human Yes 7.4 EC50 = 38 nM Funct
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
294 2 4 9 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O
CHEMBL388757 aa3r_human Human Yes 6.4 EC50 = 384 nM Funct
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
357 5 4 9 0.1 OC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL3414941 aa3r_human Human No 7.4 EC50 = 39.5 nM Funct
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
407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL3133151 aa3r_human Human No 7.4 EC50 = 39.8 nM Funct
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
405 6 5 10 -0.0 CCNc1nc(NC2CCCC2)c2ncn([C@@H]3O[C@H](C(=O)NC)[C@@H](O)[C@H]3O)c2n1
CHEMBL3133156 aa3r_human Human No 7.4 EC50 = 39.8 nM Funct
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
365 6 5 10 -1.0 CCCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O
CHEMBL431733 aa3r_human Human Yes 8.4 EC50 = 4.1 nM Funct
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
544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I
CHEMBL186113 aa3r_human Human Yes 8.4 EC50 = 4.2 nM Bind
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
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
CHEMBL490606 aa3r_human Human No 8.4 EC50 = 4.2 nM Funct
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
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
CHEMBL464859 aa3r_human Human Yes 8.3 EC50 = 4.6 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL3800106 aa3r_mouse Mouse No 8.3 EC50 = 4.9 nM Funct
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
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
CHEMBL4078771 aa3r_human Human No 6.4 EC50 = 407.4 nM Funct
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
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
CHEMBL591423 aa3r_human Human No 7.4 EC50 = 42 nM Bind
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
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
CHEMBL591356 aa3r_human Human No 7.4 EC50 = 44 nM Bind
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
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
CHEMBL4746617 aa3r_human Human No 7.4 EC50 = 44.7 nM Funct
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
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
CHEMBL4076561 aa3r_human Human No 7.4 EC50 = 44.7 nM Funct
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
463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL4076495 aa3r_human Human No 6.4 EC50 = 446.7 nM Funct
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
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
CHEMBL4076565 aa3r_human Human No 6.4 EC50 = 446.7 nM Funct
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
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
CHEMBL592246 aa3r_human Human No 6.4 EC50 = 449 nM Bind
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
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
CHEMBL3125712 aa3r_human Human No 7.3 EC50 = 45.8 nM Funct
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
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
CHEMBL235742 aa3r_human Human No 6.3 EC50 = 453 nM Funct
Agonist activity at human adenosine A3 receptor after 15 to 30 minsAgonist activity at human adenosine A3 receptor after 15 to 30 mins
308 3 3 9 -1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](OC)[C@@H]1O
CHEMBL575027 aa3r_human Human No 7.3 EC50 = 46 nM Bind
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
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
CHEMBL2113420 aa3r_human Human No 6.3 EC50 = 473 nM Funct
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
387 6 3 9 1.4 CSC[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL601515 aa3r_human Human No 6.3 EC50 = 480 nM Bind
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
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
CHEMBL3133080 aa3r_human Human No 8.3 EC50 = 5.0 nM Funct
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
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
CHEMBL3133153 aa3r_human Human No 8.3 EC50 = 5.0 nM Funct
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
323 3 5 10 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL3133157 aa3r_human Human No 8.3 EC50 = 5.0 nM Funct
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
363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O
CHEMBL2064657 aa3r_human Human Yes 8.3 EC50 = 5.0 nM Funct
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
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
CHEMBL66393 aa3r_human Human Yes 8.3 EC50 = 5.2 nM Funct
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL4747947 aa3r_rat Rat No 8.3 EC50 = 5.3 nM Funct
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
524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1
CHEMBL3414940 aa3r_human Human No 8.3 EC50 = 5.4 nM Funct
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
373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL139417 aa3r_human Human No 8.3 EC50 = 5.4 nM Funct
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
520 5 4 8 1.1 CNC(=O)C12CC1C(n1cnc3c(NCc4cccc(I)c4)ncnc31)C(O)C2O
CHEMBL324095 aa3r_human Human No 8.3 EC50 = 5.4 nM Funct
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
323 2 1 7 1.2 O=c1[nH]c2ccccc2n2c(=O)n(-c3ccc([N+](=O)[O-])cc3)nc12
CHEMBL3414940 aa3r_human Human No 7.3 EC50 = 51.5 nM Funct
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
373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL223514 aa3r_human Human No 7.3 EC50 = 52 nM Bind
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
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
CHEMBL4086325 aa3r_human Human No 7.3 EC50 = 52.4 nM Funct
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
447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL27376 aa3r_human Human No 5.3 EC50 = 5250 nM Funct
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
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
CHEMBL4747947 aa3r_rat Rat No 7.3 EC50 = 56.9 nM Funct
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
524 5 1 7 6.7 O=C(Nc1nc(-c2ccccc2)c(-c2nc3ccccc3c(=O)n2-c2ccc(Cl)cc2)s1)c1ccco1
CHEMBL4089741 aa3r_human Human No 7.2 EC50 = 59.7 nM Funct
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
429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL3414938 aa3r_human Human No 8.2 EC50 = 6.4 nM Funct
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
347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL3414944 aa3r_human Human No 7.2 EC50 = 61.9 nM Funct
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
403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL331372 aa3r_human Human Yes 6.2 EC50 = 613 nM Bind
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
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
CHEMBL464859 aa3r_human Human Yes 7.2 EC50 = 63 nM Bind
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL464859 aa3r_human Human Yes 7.2 EC50 = 63.1 nM Bind
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL2064661 aa3r_human Human No 6.2 EC50 = 631.0 nM Bind
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
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
CHEMBL3133082 aa3r_human Human No 6.2 EC50 = 631.0 nM Funct
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
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
CHEMBL4096796 aa3r_human Human No 7.2 EC50 = 64.6 nM Funct
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
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
CHEMBL280580 aa3r_human Human No 5.2 EC50 = 6800 nM Funct
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
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
CHEMBL4483546 aa3r_human Human No 6.2 EC50 = 692 nM Funct
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
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
CHEMBL4098377 aa3r_human Human No 8.1 EC50 = 7.6 nM Funct
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
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
CHEMBL3414939 aa3r_human Human No 8.1 EC50 = 7.7 nM Funct
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
381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL2064657 aa3r_human Human Yes 8.1 EC50 = 7.9 nM Bind
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
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
CHEMBL2064660 aa3r_human Human No 8.1 EC50 = 7.9 nM Funct
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
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
CHEMBL3414943 aa3r_human Human No 6.1 EC50 = 721 nM Funct
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
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
CHEMBL599387 aa3r_human Human No 6.1 EC50 = 776 nM Bind
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
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
CHEMBL464859 aa3r_human Human Yes 7.1 EC50 = 78 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL604591 aa3r_human Human No 6.1 EC50 = 789 nM Bind
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
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
CHEMBL4104819 aa3r_human Human No 6.1 EC50 = 794.3 nM Funct
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
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
CHEMBL68738 aa3r_human Human Yes 5.1 EC50 = 7980 nM Funct
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptorStimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor
335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1
CHEMBL209352 aa3r_human Human No 8.1 EC50 = 8.1 nM Funct
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
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
CHEMBL337602 aa3r_human Human No 6.1 EC50 = 803 nM Funct
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
311 2 4 8 -0.7 Nc1nc(Cl)nc2c1ncn2C1C(O)C(O)C2(CO)CC12
CHEMBL138746 aa3r_human Human No 6.1 EC50 = 828 nM Funct
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
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
CHEMBL3414942 aa3r_human Human No 7.1 EC50 = 83.9 nM Funct
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
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
CHEMBL4086624 aa3r_human Human No 6.1 EC50 = 831.8 nM Funct
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
552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1
CHEMBL464859 aa3r_human Human Yes 7.1 EC50 = 84.8 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL66393 aa3r_human Human Yes 7.1 EC50 = 85 nM Funct
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
483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL464859 aa3r_human Human Yes 7.1 EC50 = 89 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL4059961 aa3r_human Human No 8.0 EC50 = 9.6 nM Funct
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
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
CHEMBL3414936 aa3r_human Human No 7.0 EC50 = 93.6 nM Funct
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
333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1
CHEMBL119709 aa3r_human Human Yes 10.8 IC50 = 0.0 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL119709 aa3r_human Human Yes 10.7 IC50 = 0.0 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL119709 aa3r_human Human Yes 10.6 IC50 = 0.0 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL119709 aa3r_human Human Yes 10.6 IC50 = 0.0 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL119709 aa3r_human Human Yes 10.3 IC50 = 0.0 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL119709 aa3r_human Human Yes 10.3 IC50 = 0.1 nM Funct
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL1098108 aa3r_human Human No 10.2 IC50 = 0.1 nM Funct
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
359 4 1 6 3.3 COc1ccc(C(=O)Nc2nc(-c3ccccc3)nc3nn(C)cc23)cc1
CHEMBL3754229 aa3r_human Human No 10.0 IC50 = 0.1 nM Funct
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
427 5 1 7 4.8 COc1ccc(C(=O)Nc2nc(-c3cccs3)nc3cn(-c4ccccc4)nc23)cc1
CHEMBL119709 aa3r_human Human Yes 9.9 IC50 = 0.1 nM Bind
Binding affinity to human adenosine A3 receptor by radioligand displacement assayBinding affinity to human adenosine A3 receptor by radioligand displacement assay
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL2181968 aa3r_human Human No 9.8 IC50 = 0.2 nM Funct
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
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
CHEMBL4128926 aa3r_human Human No 9.8 IC50 = 0.2 nM Bind
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
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
CHEMBL464859 aa3r_human Human Yes 9.7 IC50 = 0.2 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL122819 aa3r_human Human No 9.7 IC50 = 0.2 nM Bind
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
336 6 1 6 3.4 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCC)cc3)nn12
CHEMBL123172 aa3r_human Human No 9.7 IC50 = 0.2 nM Bind
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
322 5 1 6 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3cccc(OC)c3)nn12
CHEMBL123465 aa3r_human Human No 9.6 IC50 = 0.2 nM Bind
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
278 3 1 5 2.6 CCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12
CHEMBL122512 aa3r_human Human No 9.6 IC50 = 0.3 nM Bind
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
292 4 1 5 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12
CHEMBL122512 aa3r_human Human No 9.6 IC50 = 0.3 nM Bind
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
292 4 1 5 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12
CHEMBL333415 aa3r_human Human No 9.6 IC50 = 0.3 nM Bind
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
310 4 1 5 3.1 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(F)cc3)nn12
CHEMBL122512 aa3r_human Human No 9.6 IC50 = 0.3 nM Bind
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
292 4 1 5 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12
CHEMBL464859 aa3r_human Human Yes 9.6 IC50 = 0.3 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL122685 aa3r_human Human No 9.6 IC50 = 0.3 nM Bind
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
306 4 1 5 3.3 CCCCc1nc2[nH]cnc2c2nc(-c3cccc(C)c3)nn12
CHEMBL124788 aa3r_human Human No 9.5 IC50 = 0.3 nM Bind
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
326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccccc3Cl)nn12
CHEMBL464859 aa3r_human Human Yes 9.5 IC50 = 0.3 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL122511 aa3r_human Human No 9.5 IC50 = 0.3 nM Bind
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
306 5 1 5 3.4 CCCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12
CHEMBL333860 aa3r_human Human No 9.5 IC50 = 0.3 nM Bind
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
350 7 1 6 3.8 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCCC)cc3)nn12
CHEMBL332742 aa3r_human Human No 9.5 IC50 = 0.3 nM Bind
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
306 4 1 5 3.3 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C)cc3)nn12
CHEMBL201706 aa3r_human Human No 9.4 IC50 = 0.4 nM Funct
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
358 3 4 9 -0.4 CNC(=O)[C@H]1S[C@@H](n2cnc3c(NC)nc(Cl)nc32)[C@H](O)[C@@H]1O
CHEMBL121339 aa3r_human Human No 9.4 IC50 = 0.4 nM Bind
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
326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(Cl)cc3)nn12
CHEMBL330982 aa3r_human Human No 9.4 IC50 = 0.4 nM Bind
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
312 2 1 5 3.3 c1ccc(-c2nc3c4[nH]cnc4nc(-c4ccccc4)n3n2)cc1
CHEMBL121339 aa3r_human Human No 9.4 IC50 = 0.4 nM Bind
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
326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(Cl)cc3)nn12
CHEMBL330873 aa3r_human Human No 9.4 IC50 = 0.5 nM Bind
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
264 2 1 5 2.2 CCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12
CHEMBL464859 aa3r_human Human Yes 9.3 IC50 = 0.5 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL464859 aa3r_human Human Yes 9.3 IC50 = 0.5 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL400812 aa3r_human Human No 9.2 IC50 = 0.6 nM Funct
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
425 4 1 7 3.6 COc1ccc(C(=O)Nc2nc3ccccc3n3c(=O)c(-c4ccc(C)cc4)nn23)cc1
CHEMBL464859 aa3r_human Human Yes 9.2 IC50 = 0.6 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL119709 aa3r_human Human Yes 9.2 IC50 = 0.6 nM Bind
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL119709 aa3r_human Human Yes 9.2 IC50 = 0.6 nM Bind
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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL200732 aa3r_human Human No 9.2 IC50 = 0.6 nM Funct
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
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
CHEMBL123705 aa3r_human Human No 9.2 IC50 = 0.6 nM Funct
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
360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12
CHEMBL123705 aa3r_human Human No 9.2 IC50 = 0.6 nM Bind
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12
CHEMBL123203 aa3r_human Human No 9.2 IC50 = 0.6 nM Bind
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
320 6 1 5 3.8 CCCCCCc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12
CHEMBL123705 aa3r_human Human No 9.2 IC50 = 0.6 nM Bind
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
360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12
CHEMBL123705 aa3r_human Human No 9.2 IC50 = 0.6 nM Bind
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
360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12
CHEMBL464859 aa3r_human Human Yes 9.2 IC50 = 0.6 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL123462 aa3r_human Human No 9.2 IC50 = 0.7 nM Bind
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
335 5 1 6 3.1 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(N(C)C)cc3)nn12
CHEMBL118923 aa3r_human Human No 9.2 IC50 = 0.7 nM Funct
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
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 9.2 IC50 = 0.7 nM Funct
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
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL118923 aa3r_human Human No 9.2 IC50 = 0.7 nM Bind
Inhibitory activity against Human Adenosine A3 receptor expressed in CHO cellsInhibitory activity against Human Adenosine A3 receptor expressed in CHO cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 9.2 IC50 = 0.7 nM Bind
Inhibitory activity against Human Adenosine A3 receptor expressed in CHO cellsInhibitory activity against Human Adenosine A3 receptor expressed in CHO cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL1096754 aa3r_human Human No 9.1 IC50 = 0.7 nM Funct
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
329 3 1 5 3.3 Cn1cc2c(NC(=O)c3ccccc3)nc(-c3ccccc3)nc2n1
CHEMBL464859 aa3r_human Human Yes 9.1 IC50 = 0.8 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL119709 aa3r_human Human Yes 9.1 IC50 = 0.8 nM Bind
Displacement of [3H]ABMECA from human recombinant adenosine receptor A3 expressed in CHOK1 cells after 60 minsDisplacement of [3H]ABMECA from human recombinant adenosine receptor A3 expressed in CHOK1 cells after 60 mins
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL125147 aa3r_human Human No 9.1 IC50 = 0.9 nM Bind
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
370 5 1 6 3.5 COCCc1nc2[nH]cnc2c2nc(-c3ccc(-c4ccccc4)cc3)nn12
CHEMBL339655 aa3r_human Human No 9.0 IC50 = 1 nM Bind
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
250 1 1 5 2.0 Cc1nc2[nH]cnc2c2nc(-c3ccccc3)nn12
CHEMBL1210154 aa3r_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [3H]AB-MECA from human recombinant A3 receptor expressed in HEK293 cellsDisplacement of [3H]AB-MECA from human recombinant A3 receptor expressed in HEK293 cells
336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1
CHEMBL203357 aa3r_human Human No 9.0 IC50 = 1 nM Funct
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
344 2 4 9 -0.9 CNC(=O)[C@H]1S[C@@H](n2cnc3c(N)nc(Cl)nc32)[C@H](O)[C@@H]1O
CHEMBL3753642 aa3r_human Human No 9.0 IC50 = 1.0 nM Funct
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
398 4 1 7 4.2 O=C(Nc1nc(-c2cccs2)nc2cn(-c3ccccc3)nc12)c1cccnc1
CHEMBL574212 aa3r_human Human No 9.0 IC50 = 1.1 nM Funct
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
1124 21 6 14 6.8 CCN1/C(=C\C=C\C=C\C2=[N+](CCCCCC(=O)NCCNC(=O)CCC#Cc3nc(NCc4cccc(Cl)c4)c4ncn([C@H]5[C@H](O)[C@H](O)[C@@]6(C(=O)NC)C[C@H]56)c4n3)c3ccccc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)[O-])ccc21
CHEMBL122667 aa3r_human Human No 9.0 IC50 = 1.1 nM Bind
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
326 4 1 5 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3cccc(Cl)c3)nn12
CHEMBL333535 aa3r_human Human No 9.0 IC50 = 1.1 nM Bind
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
382 7 1 8 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3cc(OC)c(OC)c(OC)c3)nn12
CHEMBL477 aa3r_human Human Yes 8.9 IC50 = 1.1 nM Funct
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
267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL464859 aa3r_human Human Yes 8.9 IC50 = 1.1 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL1766359 aa3r_human Human No 8.9 IC50 = 1.2 nM Funct
Antagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 minsAntagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 mins
370 4 2 4 3.7 O=C(NCc1ccccc1)Nc1nn(-c2ccccc2)c(=O)c2ccccc12
CHEMBL122632 aa3r_human Human No 8.9 IC50 = 1.2 nM Bind
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
348 4 1 5 4.3 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(C)(C)C)cc3)nn12
CHEMBL123195 aa3r_human Human No 8.9 IC50 = 1.2 nM Bind
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
293 4 1 6 2.4 CCCCc1nc2[nH]cnc2c2nc(-c3cccnc3)nn12
CHEMBL119709 aa3r_human Human Yes 8.9 IC50 = 1.2 nM Bind
Displacement of radiolabeled IB-MECA from human adenosine A3 receptorDisplacement of radiolabeled IB-MECA from human adenosine A3 receptor
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL119709 aa3r_human Human Yes 8.9 IC50 = 1.2 nM Bind
Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECAInhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL464859 aa3r_human Human Yes 8.9 IC50 = 1.2 nM Funct
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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL431733 aa3r_human Human Yes 8.9 IC50 = 1.2 nM Funct
Agonist activity at human recombinant A3AR expressed in CHO cells assessed as inhibition of forskolin-induced stimulation of cAMP productionAgonist activity at human recombinant A3AR expressed in CHO cells assessed as inhibition of forskolin-induced stimulation of cAMP production
544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I
CHEMBL429131 aa3r_human Human No 8.9 IC50 = 1.3 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced cAMP accumulation
331 8 1 5 3.6 CCCSc1nc(NC(C)=O)cc(OCCc2ccccc2)n1
CHEMBL3939800 aa3r_human Human Yes 8.8 IC50 = 1.6 nM Bind
Adenosine A3 Receptor Radioligand Binding Assay: .(R)- and (S)-(4-Fluorophenyl)(4-((5-methyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)methanol was tested in a radioligand binding assay, according to the procedure described in Olah et al., Mol. Pharmacol. 1994, 45, 978-982 and Salvatore et al., Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 10365-10369, in human recombinant CHO-K1 cells expressing the human adenosine A3 receptor. Incubations of a range of concentration of each compound were carried out in duplicates for 1 h at 25° C. in 25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA, in the presence of 0.5 nM [125I] AB-MECA. Non-specific binding was determined in the presence of 1 uM IB-MECA.Adenosine A3 Receptor Radioligand Binding Assay: .(R)- and (S)-(4-Fluorophenyl)(4-((5-methyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)methanol was tested in a radioligand binding assay, according to the procedure described in Olah et al., Mol. Pharmacol. 1994, 45, 978-982 and Salvatore et al., Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 10365-10369, in human recombinant CHO-K1 cells expressing the human adenosine A3 receptor. Incubations of a range of concentration of each compound were carried out in duplicates for 1 h at 25° C. in 25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA, in the presence of 0.5 nM [125I] AB-MECA. Non-specific binding was determined in the presence of 1 uM IB-MECA.
349 4 3 5 3.6 Cc1cc(Nc2nc([C@@H](O)c3ccc(F)cc3)nc3ccccc23)n[nH]1
CHEMBL428377 aa3r_human Human No 8.8 IC50 = 1.7 nM Funct
Antagonist activity at human adenosine A3 receptor after 15 to 30 minsAntagonist activity at human adenosine A3 receptor after 15 to 30 mins
497 6 3 9 1.3 CO[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(NCc3cccc(I)c3)ncnc21
CHEMBL123450 aa3r_human Human No 8.7 IC50 = 1.8 nM Bind
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
308 4 2 6 2.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(O)cc3)nn12
CHEMBL145767 aa3r_human Human No 8.7 IC50 = 1.8 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human A3 adenosine receptorInhibition of cAMP accumulation in CHO cells expressing human A3 adenosine receptor
390 4 3 8 2.9 COc1ccc(NC(=O)Nc2nc3n[nH]cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL272795 aa3r_human Human No 8.7 IC50 = 1.8 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced cAMP accumulation
337 6 1 5 3.8 CCSc1nc(NC(C)=O)cc(OCc2ccc(Cl)cc2)n1
CHEMBL1096754 aa3r_human Human No 8.7 IC50 = 1.9 nM Funct
Antagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
329 3 1 5 3.3 Cn1cc2c(NC(=O)c3ccccc3)nc(-c3ccccc3)nc2n1
CHEMBL123144 aa3r_human Human No 8.7 IC50 = 1.9 nM Bind
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
370 4 1 5 3.8 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(Br)cc3)nn12
CHEMBL339218 aa3r_human Human No 8.7 IC50 = 1.9 nM Bind
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
310 4 1 5 3.1 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(F)cc3)nn12
CHEMBL338057 aa3r_human Human No 8.0 IC50 = 10 nM Bind
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
318 4 1 5 4.0 CCCCc1nc2ccccc2c2nc(-c3ccc(O)cc3)nn12
CHEMBL1800784 aa3r_human Human No 8.0 IC50 = 10.5 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
355 5 1 6 1.8 C=CCN1C(=O)N2C[C@H](CC)N=C2c2[nH]c(-c3cc(OC)nn3C)nc21
CHEMBL341259 aa3r_human Human No 6.0 IC50 = 1000 nM Bind
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
336 4 0 4 4.9 CCCCc1nc2cccc(Cl)c2c2nc(-c3ccccc3)nn12
CHEMBL20888 aa3r_human Human No 7.0 IC50 = 103 nM Funct
Antagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECA
298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C
CHEMBL544678 aa3r_human Human No 7.0 IC50 = 103 nM Funct
Antagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECA
298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C
CHEMBL2322929 aa3r_human Human No 7.0 IC50 = 103 nM Funct
Inhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECAInhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECA
329 3 1 5 3.4 CC(=O)Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL2042298 aa3r_human Human Yes 7.0 IC50 = 104 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
427 7 5 10 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O
CHEMBL2070884 aa3r_human Human No 7.0 IC50 = 105 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
419 4 2 9 1.5 C#CCN1CCC(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)CC1
CHEMBL1480 aa3r_human Human Yes 6.0 IC50 = 1057 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
383 4 1 5 4.0 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1cccc(Cl)c1Cl
CHEMBL520122 aa3r_human Human No 7.0 IC50 = 107 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assay
365 3 1 5 4.2 O=C(Nc1nc2ccccc2c2cn(-c3ccccc3)nc12)c1ccccn1
CHEMBL4439336 aa3r_human Human No 6.0 IC50 = 1072 nM Bind
Displacement of [3H]PSB11 from human A3 adenosine receptor Y265F (7.36) mutant transiently expressed in CHOK1 cell membranes measured after 2 hrs by scintillation spectrometric methodDisplacement of [3H]PSB11 from human A3 adenosine receptor Y265F (7.36) mutant transiently expressed in CHOK1 cell membranes measured after 2 hrs by scintillation spectrometric method
517 9 1 10 1.7 CCCn1c(=O)c2c(nc3cc(OC)ccn32)n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O
CHEMBL1203324 aa3r_human Human Yes 5.0 IC50 = 10750 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2
CHEMBL141343 aa3r_human Human Yes 5.0 IC50 = 10750 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
520 5 1 8 4.2 Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2
CHEMBL464859 aa3r_human Human Yes 7.0 IC50 = 109.7 nM Funct
Agonist activity at wild type human A3 receptor M177'5.38A 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 M177'5.38A 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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL284969 aa3r_human Human Yes 8.0 IC50 = 11.2 nM Funct
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
369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1
CHEMBL235717 aa3r_human Human No 7.9 IC50 = 11.6 nM Funct
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
459 4 1 7 4.2 COc1ccc(C(=O)Nc2nc3ccc(Cl)cc3n3c(=O)c(-c4ccc(C)cc4)nn23)cc1
CHEMBL123694 aa3r_human Human No 7.0 IC50 = 110 nM Bind
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
316 4 0 4 4.6 CCCCc1nc2cc(C)ccc2c2nc(-c3ccccc3)nn12
CHEMBL1479 aa3r_human Human Yes 5.0 IC50 = 11160 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C
CHEMBL2042310 aa3r_human Human No 7.0 IC50 = 113 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
810 18 6 13 6.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL2322909 aa3r_human Human No 6.9 IC50 = 115 nM Funct
Inhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECAInhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECA
433 4 0 6 4.6 Cc1nc(N(C(=O)c2ccccc2)C(=O)c2ccccc2)c2nn(-c3ccccc3)cc2n1
CHEMBL2071039 aa3r_human Human No 6.9 IC50 = 116 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
452 4 3 9 1.6 CCNC(=O)N1CCC(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)CC1
CHEMBL726 aa3r_human Human Yes 4.9 IC50 = 11935 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F
CHEMBL391483 aa3r_human Human No 7.9 IC50 = 12 nM Funct
Antagonist activity at human adenosine A3 receptor after 15 to 30 minsAntagonist activity at human adenosine A3 receptor after 15 to 30 mins
521 5 4 9 0.4 CNC(=O)[C@]12CN[C@H]([C@@H]1O)[C@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)O2
CHEMBL2071048 aa3r_human Human No 7.9 IC50 = 12 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
528 5 3 9 3.1 Cc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1
CHEMBL193141 aa3r_human Human No 7.9 IC50 = 12 nM Funct
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
312 1 1 5 2.0 O=c1[nH]c2ccccc2n2c(=O)c(-c3ccc(Cl)cc3)nn12
CHEMBL124724 aa3r_human Human No 7.9 IC50 = 12 nM Bind
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
320 5 1 5 3.6 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(CC)cc3)nn12
CHEMBL1800782 aa3r_human Human No 7.9 IC50 = 12.2 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
355 5 1 6 1.8 C=CCN1C(=O)N2CC(CC)N=C2c2[nH]c(-c3cc(OC)nn3C)nc21
CHEMBL422820 aa3r_human Human No 7.9 IC50 = 12.4 nM Funct
Inhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human A3 receptorInhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human A3 receptor
494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3nn(CCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL2042305 aa3r_human Human No 6.9 IC50 = 120 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
607 12 5 10 3.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O
CHEMBL2071051 aa3r_human Human No 6.9 IC50 = 120 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1
CHEMBL2079181 aa3r_human Human No 6.9 IC50 = 120 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1
CHEMBL122230 aa3r_human Human No 6.9 IC50 = 120 nM Bind
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
292 4 0 5 3.9 CCCCc1nc2ccccc2c2nc(-c3ccco3)nn12
CHEMBL250699 aa3r_human Human Yes 4.9 IC50 = 12000 nM Bind
Displacement of [125I]AB-MECA from adenosine A3 receptorDisplacement of [125I]AB-MECA from adenosine A3 receptor
357 5 1 4 4.9 COc1cc(NC(=O)c2ccc(-c3ccc(Cl)cc3)o2)cc(OC)c1
CHEMBL2042303 aa3r_human Human No 6.9 IC50 = 121 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
630 13 6 13 2.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL2070886 aa3r_human Human No 6.9 IC50 = 121 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
471 5 2 9 3.1 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL1016 aa3r_human Human Yes 5.9 IC50 = 1219.9 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
440 7 2 7 4.0 CCOc1nc2c(n1Cc1ccc(cc1)c1ccccc1c1n[nH]nn1)c(ccc2)C(=O)O
CHEMBL437309 aa3r_human Human No 4.9 IC50 = 12260 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
571 5 1 7 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)cc2n(C)c1=O
CHEMBL236373 aa3r_human Human Yes 6.9 IC50 = 125 nM Funct
Activity at human adenosine A3 receptor expressed in CHO cells assessed as antagonism of Cl-IB-MECA-inhibited cAMP productionActivity at human adenosine A3 receptor expressed in CHO cells assessed as antagonism of Cl-IB-MECA-inhibited cAMP production
295 3 2 4 2.2 COc1ccc(NC(=O)c2nc(=O)[nH]c3ccccc23)cc1
CHEMBL62350 aa3r_human Human Yes 5.9 IC50 = 1250 nM Bind
Inhibitory activity against cyclic AMP production in human adenosine A3 receptor assayInhibitory activity against cyclic AMP production in human adenosine A3 receptor assay
256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O
CHEMBL2322903 aa3r_human Human No 6.9 IC50 = 128 nM Funct
Inhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECAInhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECA
359 4 1 6 3.4 COc1ccc(-n2cc3nc(C)nc(NC(=O)c4ccccc4)c3n2)cc1
CHEMBL3754500 aa3r_human Human No 7.9 IC50 = 13 nM Funct
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
397 4 1 6 4.8 O=C(Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12)c1cccs1
CHEMBL422820 aa3r_human Human No 7.9 IC50 = 13.9 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptorInhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor
494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3nn(CCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL332577 aa3r_human Human No 6.9 IC50 = 130 nM Bind
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
360 4 1 5 4.0 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12
CHEMBL332577 aa3r_human Human No 6.9 IC50 = 130 nM Bind
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
360 4 1 5 4.0 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12
CHEMBL1081160 aa3r_human Human No 6.9 IC50 = 130.3 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL1258170 aa3r_human Human No 4.9 IC50 = 13000 nM Funct
Antagonist activity at adenosine A3 receptor by cAMP assayAntagonist activity at adenosine A3 receptor by cAMP assay
465 6 2 7 5.6 COc1ccc(Nc2c(-c3ccc4nccnc4c3)c(C)nn2-c2ccccc2C)c(C(=O)O)c1
CHEMBL208705 aa3r_human Human No 5.9 IC50 = 1315 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
411 4 2 7 1.4 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)Nc4ccccn4)cc3)cc2n(C)c1=O
CHEMBL603 aa3r_human Human Yes 5.9 IC50 = 1363 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C
CHEMBL330394 aa3r_human Human Yes 6.9 IC50 = 138 nM Funct
Activity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation countingActivity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation counting
251 1 1 5 2.8 Oc1nc2ccccc2c2cc(-c3ccco3)nn12
CHEMBL2042308 aa3r_human Human No 5.9 IC50 = 1390 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
838 14 6 11 7.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL1800781 aa3r_human Human No 7.8 IC50 = 14.5 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
341 4 1 6 1.4 C=CCN1C(=O)N2CC(C)N=C2c2[nH]c(-c3cc(OC)nn3C)nc21
CHEMBL1800862 aa3r_human Human No 7.8 IC50 = 14.6 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
342 5 1 6 2.0 C=CCN1C(=O)N2CC(CC)N=C2c2[nH]c(-c3cc(OC)no3)nc21
CHEMBL141154 aa3r_human Human No 7.8 IC50 = 14.8 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 10.8-21.5Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 10.8-21.5
422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL239193 aa3r_human Human No 6.9 IC50 = 140 nM Funct
Activity at human adenosine A3 receptor expressed in CHO cells assessed as antagonism of Cl-IB-MECA-inhibited cAMP productionActivity at human adenosine A3 receptor expressed in CHO cells assessed as antagonism of Cl-IB-MECA-inhibited cAMP production
306 3 2 4 2.8 CC(=O)Nc1nc(C(=O)Nc2ccccc2)c2ccccc2n1
CHEMBL122163 aa3r_human Human No 6.9 IC50 = 140 nM Bind
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
378 5 0 4 6.0 CCCCc1nc2ccccc2c2nc(-c3ccc(-c4ccccc4)cc3)nn12
CHEMBL3769755 aa3r_human Human Yes 5.9 IC50 = 1400 nM Bind
Inhibition of adenosine A3 receptor (unknown origin)Inhibition of adenosine A3 receptor (unknown origin)
414 3 0 7 4.4 COC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2c(sc(C)c2C)-n2c(C)nnc21
CHEMBL2042309 aa3r_human Human No 5.9 IC50 = 1407 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
854 14 7 12 7.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL2042299 aa3r_human Human No 6.9 IC50 = 141 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
442 7 6 11 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL434063 aa3r_human Human Yes 4.8 IC50 = 14318 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
495 12 2 6 4.9 CN(CCOc1ccc(C[C@H](Nc2ccccc2C(=O)c2ccccc2)C(=O)O)cc1)c1ccccn1
CHEMBL516851 aa3r_human Human No 6.8 IC50 = 145 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assay
399 3 1 5 4.9 O=C(Nc1nc2ccccc2c2cn(-c3ccc(Cl)cc3)nc12)c1ccncc1
CHEMBL209944 aa3r_human Human No 5.8 IC50 = 1467 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
563 10 2 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O
CHEMBL584 aa3r_human Human Yes 4.8 IC50 = 14796 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C
CHEMBL2181977 aa3r_human Human No 6.8 IC50 = 148 nM Funct
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
471 5 2 6 5.2 Cc1ccc(-c2nc(NC(=O)Nc3ccc(F)cc3)c3nnn(Cc4ccccc4F)c3n2)cc1
CHEMBL211071 aa3r_human Human No 4.8 IC50 = 14860 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
565 7 1 9 2.3 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)cc21
CHEMBL2042307 aa3r_human Human No 6.8 IC50 = 149 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
685 12 5 10 4.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL306043 aa3r_human Human No 5.8 IC50 = 1492 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
None None None None
CHEMBL73237 aa3r_human Human Yes 7.8 IC50 = 15 nM Funct
Antagonist activity at human adenosine A3 receptor after 15 to 30 minsAntagonist activity at human adenosine A3 receptor after 15 to 30 mins
281 3 3 9 -1.3 CO[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(N)ncnc21
CHEMBL2071046 aa3r_human Human No 7.8 IC50 = 15 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
532 5 3 9 2.9 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(F)cc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL125339 aa3r_human Human No 7.8 IC50 = 15 nM Bind
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
384 5 2 6 3.4 O=C(O)CCc1nc2[nH]cnc2c2nc(-c3ccc(-c4ccccc4)cc3)nn12
CHEMBL141154 aa3r_human Human No 7.8 IC50 = 15.1 nM Funct
Inhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human Adenosine A3 receptorInhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human Adenosine A3 receptor
422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL464859 aa3r_human Human Yes 7.8 IC50 = 15.5 nM Funct
Agonist activity at wild type human A3 receptor L90'3.32A 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 L90'3.32A 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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL1800786 aa3r_human Human No 7.8 IC50 = 15.9 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
391 4 1 6 2.4 COc1cc(-c2nc3c([nH]2)C2=N[C@H](C)CN2C(=O)N3Cc2ccccc2)n(C)n1
CHEMBL235317 aa3r_human Human No 6.8 IC50 = 150 nM Funct
Antagonist activity at human adenosine A3 receptor after 15 to 30 minsAntagonist activity at human adenosine A3 receptor after 15 to 30 mins
495 5 3 9 1.1 OC[C@]12CO[C@H]([C@@H]1O)[C@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)O2
CHEMBL331837 aa3r_human Human No 6.8 IC50 = 150 nM Bind
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
348 4 1 5 4.3 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(C(C)(C)C)cc3)nn12
CHEMBL326538 aa3r_human Human No 5.8 IC50 = 1510 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
457 5 1 5 4.5 O=C(OCc1cccc(Oc2ccccc2)c1)N1CCC2(CC1)C(=O)NCN2c1ccccc1
CHEMBL4285494 aa3r_human Human No 6.8 IC50 = 152.9 nM Funct
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as reduction in Cl-IB-MECA-induced inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 10 mins followed by Cl-IB-MECA addition measured after 30 mins by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as reduction in Cl-IB-MECA-induced inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 10 mins followed by Cl-IB-MECA addition measured after 30 mins by liquid scintillation counting method
331 7 1 5 3.9 CC[C@H](C)Oc1cc(NC(C)=O)nc(SCc2ccccc2)n1
CHEMBL210456 aa3r_human Human No 5.8 IC50 = 1525 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
441 5 2 8 1.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)cn1
CHEMBL3311508 aa3r_human Human No 5.8 IC50 = 1560 nM Funct
Agonist activity at human recombinant A3AR expressed in CHO cells assessed as inhibition of forskolin-induced stimulation of cAMP productionAgonist activity at human recombinant A3AR expressed in CHO cells assessed as inhibition of forskolin-induced stimulation of cAMP production
421 6 4 10 0.7 COc1ccc(Cl)cc1CNc1ncnc2c1ncn2[C@@H]1OC[C@@](O)(CO)[C@H]1O
CHEMBL341041 aa3r_human Human No 6.8 IC50 = 160 nM Bind
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
332 5 0 5 4.3 CCCCc1nc2ccccc2c2nc(-c3ccc(OC)cc3)nn12
CHEMBL341041 aa3r_human Human No 6.8 IC50 = 160 nM Bind
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
332 5 0 5 4.3 CCCCc1nc2ccccc2c2nc(-c3ccc(OC)cc3)nn12
CHEMBL2070894 aa3r_human Human No 6.8 IC50 = 166 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
472 5 2 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL1366 aa3r_human Human No 5.8 IC50 = 1688 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
None None None None
CHEMBL1766354 aa3r_human Human No 7.8 IC50 = 17 nM Funct
Antagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 minsAntagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 mins
386 4 2 5 4.0 COc1ccccc1NC(=O)Nc1nn(-c2ccccc2)c(=O)c2ccccc12
CHEMBL1800787 aa3r_human Human No 7.8 IC50 = 17.5 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
391 4 1 6 2.4 COc1cc(-c2nc3c([nH]2)C2=N[C@@H](C)CN2C(=O)N3Cc2ccccc2)n(C)n1
CHEMBL391279 aa3r_human Human No 6.8 IC50 = 170 nM Funct
Antagonist activity at human adenosine A3 receptor after 15 to 30 minsAntagonist activity at human adenosine A3 receptor after 15 to 30 mins
305 2 4 9 -2.2 CNC(=O)[C@]12CN[C@H]([C@@H]1O)[C@H](n1cnc3c(N)ncnc31)O2
CHEMBL2042312 aa3r_human Human No 5.8 IC50 = 1721 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
840 13 7 12 6.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL633 aa3r_human Human Yes 4.8 IC50 = 17547 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2
CHEMBL115444 aa3r_human Human No 5.8 IC50 = 1780 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1
CHEMBL371404 aa3r_human Human No 7.8 IC50 = 18 nM Funct
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
350 5 0 6 2.6 CCCn1c(=O)c2c(nc3n2CC(CC)=C3)n(Cc2ccccc2)c1=O
CHEMBL1766353 aa3r_human Human No 7.8 IC50 = 18 nM Funct
Antagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 minsAntagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 mins
386 4 2 5 4.0 COc1cccc(NC(=O)Nc2nn(-c3ccccc3)c(=O)c3ccccc23)c1
CHEMBL2070893 aa3r_human Human No 6.8 IC50 = 180 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
472 5 2 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4cccnc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL4565447 aa3r_human Human No 4.7 IC50 = 18400 nM Funct
Antagonist activity at human adenosine receptor A3 expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assayAntagonist activity at human adenosine receptor A3 expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assay
280 3 0 3 4.2 CCOc1cccc2cc(-c3ccc(C)cc3)c(=O)oc12
CHEMBL114535 aa3r_human Human Yes 6.7 IC50 = 186 nM Funct
Inhibition of [35S]GTP-gamma-S, binding stimulated by 20 uM 5''-N-ethyluronamidoadenosine (NECA) in membranes of HEK293 cells expressing human Adenosine A3 receptorInhibition of [35S]GTP-gamma-S, binding stimulated by 20 uM 5''-N-ethyluronamidoadenosine (NECA) in membranes of HEK293 cells expressing human Adenosine A3 receptor
416 6 1 6 3.6 CCOC(=O)c1c(NC(=O)Cc2ccccc2)sc2c1CCN(C(=O)OCC)C2
CHEMBL281129 aa3r_human Human No 6.7 IC50 = 188 nM Funct
Antagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECA
301 2 1 9 1.6 CSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C
CHEMBL378527 aa3r_human Human No 4.7 IC50 = 18950 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
467 8 2 7 2.1 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(CC)c1=O
CHEMBL126150 aa3r_human Human No 7.7 IC50 = 19 nM Bind
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
370 4 1 5 3.8 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(Br)cc3)nn12
CHEMBL2322923 aa3r_human Human No 7.7 IC50 = 19.7 nM Funct
Inhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECAInhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECA
329 3 1 5 3.4 Cc1nc(NC(=O)c2ccccc2)c2nn(-c3ccccc3)cc2n1
CHEMBL139182 aa3r_human Human No 7.7 IC50 = 19.8 nM Funct
Inhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human A3 receptorInhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human A3 receptor
508 8 2 9 5.0 COc1ccc(NC(=O)Nc2nc3nn(CCCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL324512 aa3r_human Human No 6.7 IC50 = 190 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 130-279Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 130-279
454 4 3 10 2.2 Cn1cc2c(nc(NC(=O)Nc3ccc(S(=O)(=O)O)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL4088238 aa3r_human Human No 5.7 IC50 = 1910 nM Funct
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase in presence of [alpha-31P]ATPAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase in presence of [alpha-31P]ATP
447 5 3 10 2.0 Cc1cc(C)n(C[C@H]2O[C@@H](n3cnc4c(NC5CCCC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL153062 aa3r_human Human Yes 5.7 IC50 = 1915 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
220 8 1 1 4.7 CCCCCCCCCc1ccc(O)cc1
CHEMBL4079314 aa3r_human Human No 5.7 IC50 = 1940 nM Funct
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase in presence of [alpha-31P]ATPAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase in presence of [alpha-31P]ATP
517 6 3 10 3.6 Cc1cc(C)cc(-c2nc(NC3CCCC3)c3ncn([C@@H]4O[C@H](Cn5nc(C)cc5C)[C@@H](O)[C@H]4O)c3n2)c1
CHEMBL324735 aa3r_human Human No 8.7 IC50 = 2 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptorInhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptor
374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1
CHEMBL144979 aa3r_human Human No 8.7 IC50 = 2 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 1.1-3.8Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 1.1-3.8
434 4 2 7 4.8 COc1ccc(NC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL340657 aa3r_human Human No 8.7 IC50 = 2.1 nM Bind
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
292 4 1 5 3.0 CCCCc1nc2[nH]ncc2c2nc(-c3ccccc3)nn12
CHEMBL340657 aa3r_human Human No 8.7 IC50 = 2.1 nM Bind
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
292 4 1 5 3.0 CCCCc1nc2[nH]ncc2c2nc(-c3ccccc3)nn12
CHEMBL324735 aa3r_human Human No 8.7 IC50 = 2.1 nM Bind
Inhibitory activity against Human Adenosine A3 receptor expressed in CHO cellsInhibitory activity against Human Adenosine A3 receptor expressed in CHO cells
374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1
CHEMBL119709 aa3r_human Human Yes 8.7 IC50 = 2.1 nM Funct
Agonist activity at wild type human A3 receptor L90'3.32A 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 L90'3.32A 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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL431733 aa3r_human Human Yes 8.7 IC50 = 2.2 nM Funct
Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptorInhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor
544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I
CHEMBL3770310 aa3r_human Human No 8.6 IC50 = 2.3 nM Funct
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
392 5 5 10 -1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4O)ncnc32)[C@H](O)[C@@H]1O
CHEMBL1098108 aa3r_human Human No 8.6 IC50 = 2.4 nM Funct
Antagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
359 4 1 6 3.3 COc1ccc(C(=O)Nc2nc(-c3ccccc3)nc3nn(C)cc23)cc1
CHEMBL167753 aa3r_human Human No 8.6 IC50 = 2.4 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptor; range 1.2-4.9Inhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptor; range 1.2-4.9
408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL141550 aa3r_human Human No 8.6 IC50 = 2.4 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptorInhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor
438 3 2 6 5.5 O=C(Nc1cccc(Cl)c1)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12
CHEMBL583747 aa3r_human Human No 8.6 IC50 = 2.5 nM Funct
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
792 15 8 12 1.2 CNC(=O)[C@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(Cl)c4)nc(C#CCCC(=O)NCCNC(=O)CCCC[C@H]4SC[C@H]5NC(=O)N[C@H]54)nc31)[C@H](O)[C@@H]2O
CHEMBL119709 aa3r_human Human Yes 8.6 IC50 = 2.5 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL402848 aa3r_human Human No 8.6 IC50 = 2.7 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced cAMP accumulation
347 8 1 6 3.5 CCCSc1nc(NC(C)=O)cc(OCc2ccc(OC)cc2)n1
CHEMBL329791 aa3r_human Human No 8.6 IC50 = 2.7 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 1.7-4.2Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 1.7-4.2
404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL1800788 aa3r_human Human No 7.7 IC50 = 20.4 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
405 5 1 6 2.8 CCC1CN2C(=O)N(Cc3ccccc3)c3nc(-c4cc(OC)nn4C)[nH]c3C2=N1
CHEMBL1800863 aa3r_human Human No 7.7 IC50 = 20.4 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
378 4 1 6 2.7 COc1cc(-c2nc3c([nH]2)C2=NC(C)CN2C(=O)N3Cc2ccccc2)on1
CHEMBL211762 aa3r_human Human No 5.7 IC50 = 2085 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
439 6 2 7 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O
CHEMBL517867 aa3r_human Human No 7.7 IC50 = 21 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assay
354 3 1 5 4.4 O=C(Nc1nc2ccccc2c2cn(-c3ccccc3)nc12)c1ccco1
CHEMBL2070883 aa3r_human Human No 6.7 IC50 = 212 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
421 5 2 9 2.0 C=CCN1CCC(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)CC1
CHEMBL445067 aa3r_human Human No 6.7 IC50 = 215 nM Funct
Antagonist activity against Cl-IB-MECA inhibited cAMP level in CHO cells transfected with human A3 receptorAntagonist activity against Cl-IB-MECA inhibited cAMP level in CHO cells transfected with human A3 receptor
501 6 1 7 4.8 COc1ccc(-n2nc3c(NC(=O)C(c4ccccc4)c4ccccc4)nc4ccccc4n3c2=O)cc1
CHEMBL727 aa3r_human Human Yes 4.7 IC50 = 21687 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
167 0 3 4 0.6 Nc1nc2[nH]cnc2c(=S)[nH]1
CHEMBL282575 aa3r_human Human Yes 4.7 IC50 = 21780 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
376 2 1 3 5.1 C[C@]12CC[C@@H]3c4ccc(OC(=O)c5ccccc5)cc4CC[C@H]3[C@@H]1CC[C@@H]2O
CHEMBL210931 aa3r_human Human No 4.7 IC50 = 21880 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
539 7 1 7 2.8 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(CC)c1=O
CHEMBL124659 aa3r_human Human No 7.7 IC50 = 22 nM Bind
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
414 4 0 4 5.7 CCCCc1nc2ccc(Cl)cc2c2nc(-c3ccc(Br)cc3)nn12
CHEMBL1077943 aa3r_human Human No 7.6 IC50 = 22.9 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL119709 aa3r_human Human Yes 7.6 IC50 = 22.9 nM Funct
Agonist activity at wild type human A3 receptor M177'5.38A 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 M177'5.38A 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
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL411 aa3r_human Human Yes 5.7 IC50 = 2208 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1
CHEMBL3415022 aa3r_human Human Yes 6.7 IC50 = 221 nM Funct
Antagonist activity against human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-induced inhibition of forskolin-induced cAMP production by scintillation counting methodAntagonist activity against human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-induced inhibition of forskolin-induced cAMP production by scintillation counting method
243 1 1 4 2.4 Cc1nc2sc(-c3ccccc3)nc2c(=O)[nH]1
CHEMBL1289 aa3r_human Human Yes 6.7 IC50 = 223 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl
CHEMBL2042297 aa3r_human Human No 7.6 IC50 = 23 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
326 3 4 9 -1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(F)nc32)[C@H](O)[C@@H]1O
CHEMBL2069325 aa3r_human Human No 7.6 IC50 = 23 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
528 6 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL1800783 aa3r_human Human No 7.6 IC50 = 23.4 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
355 5 1 6 1.8 C=CCN1C(=O)N2C[C@@H](CC)N=C2c2[nH]c(-c3cc(OC)nn3C)nc21
CHEMBL1080241 aa3r_human Human No 6.6 IC50 = 233.1 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL279403 aa3r_human Human Yes 6.6 IC50 = 238 nM Funct
Activity at human adenosine A3 receptor expressed in CHO cells assessed as antagonism of Cl-IB-MECA-inhibited cAMP productionActivity at human adenosine A3 receptor expressed in CHO cells assessed as antagonism of Cl-IB-MECA-inhibited cAMP production
265 2 2 3 2.2 O=C(Nc1ccccc1)c1nc(=O)[nH]c2ccccc12
CHEMBL1800861 aa3r_human Human No 7.6 IC50 = 24.2 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
328 4 1 6 1.7 C=CCN1C(=O)N2CC(C)N=C2c2[nH]c(-c3cc(OC)no3)nc21
CHEMBL113956 aa3r_human Human No 5.6 IC50 = 2460 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1
CHEMBL118 aa3r_human Human Yes 4.6 IC50 = 24622 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1
CHEMBL1800864 aa3r_human Human No 7.6 IC50 = 25.3 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
392 5 1 6 3.1 CCC1CN2C(=O)N(Cc3ccccc3)c3nc(-c4cc(OC)no4)[nH]c3C2=N1
CHEMBL1935765 aa3r_human Human No 6.6 IC50 = 250 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by competition protein binding assay
432 6 2 9 3.8 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2n1
CHEMBL1417172 aa3r_human Human Yes 4.6 IC50 = 25300 nM Funct
Antagonist activity at human adenosine receptor A3 expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assayAntagonist activity at human adenosine receptor A3 expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assay
282 3 0 4 3.5 COc1ccc(-c2cc3cccc(OC)c3oc2=O)cc1
CHEMBL114643 aa3r_human Human Yes 6.6 IC50 = 255 nM Funct
Inhibition of [35S]GTP-gamma-S, binding stimulated by 20 uM 5''-N-ethyluronamidoadenosine (NECA) in membranes of HEK293 cells expressing human Adenosine A3 receptorInhibition of [35S]GTP-gamma-S, binding stimulated by 20 uM 5''-N-ethyluronamidoadenosine (NECA) in membranes of HEK293 cells expressing human Adenosine A3 receptor
398 6 1 8 4.1 COc1ccc(-c2csc(NC3OC(=O)c4c3ccc(OC)c4OC)n2)cc1
CHEMBL828 aa3r_human Human Yes 4.6 IC50 = 25640 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
199 0 1 2 3.9 c1ccc2c(c1)Nc1ccccc1S2
CHEMBL2042300 aa3r_human Human No 6.6 IC50 = 259 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
505 7 5 10 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL3751909 aa3r_human Human No 7.6 IC50 = 26 nM Funct
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
421 5 1 6 4.7 COc1ccc(-c2nc(NC(=O)c3ccccc3)c3nn(-c4ccccc4)cc3n2)cc1
CHEMBL2071043 aa3r_human Human No 7.6 IC50 = 26 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
520 4 3 9 3.3 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NC4CCCCCC4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL465946 aa3r_human Human No 7.6 IC50 = 26 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assay
378 3 1 4 5.1 Cc1cccc(C(=O)Nc2nc3ccccc3c3cn(-c4ccccc4)nc23)c1
CHEMBL339529 aa3r_human Human No 7.6 IC50 = 26 nM Bind
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
336 4 0 4 4.9 CCCCc1nc2ccccc2c2nc(-c3ccc(Cl)cc3)nn12
CHEMBL349019 aa3r_human Human No 7.6 IC50 = 26 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 15-44Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 15-44
442 3 2 8 4.2 Cn1cc2c(nc(NC(=O)Nc3ccc(Cl)c(Cl)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL340580 aa3r_human Human No 6.6 IC50 = 260 nM Bind
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
302 4 0 4 4.3 CCCCc1nc2ccccc2c2nc(-c3ccccc3)nn12
CHEMBL340580 aa3r_human Human No 6.6 IC50 = 260 nM Bind
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
302 4 0 4 4.3 CCCCc1nc2ccccc2c2nc(-c3ccccc3)nn12
CHEMBL2070880 aa3r_human Human No 6.6 IC50 = 262 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
381 3 3 9 1.1 Cn1cc2c(nc(NC(=O)NC3CCNCC3)n3nc(-c4ccco4)nc23)n1
CHEMBL1200348 aa3r_human Human Yes 5.6 IC50 = 2628 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL1221 aa3r_human Human Yes 5.6 IC50 = 2628 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL101818 aa3r_human Human Yes 6.6 IC50 = 263 nM Funct
Activity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation countingActivity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation counting
267 1 1 5 3.3 Oc1nc2ccccc2c2cc(-c3cccs3)nn12
CHEMBL3770679 aa3r_human Human No 6.6 IC50 = 269.2 nM Funct
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
482 8 4 10 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL4439336 aa3r_human Human No 7.6 IC50 = 27 nM Bind
Displacement of [3H]PSB11 from human A3 adenosine receptor transiently expressed in CHOK1 cell membranes measured after 2 hrs by scintillation spectrometric methodDisplacement of [3H]PSB11 from human A3 adenosine receptor transiently expressed in CHOK1 cell membranes measured after 2 hrs by scintillation spectrometric method
517 9 1 10 1.7 CCCn1c(=O)c2c(nc3cc(OC)ccn32)n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O
CHEMBL116903 aa3r_human Human Yes 7.6 IC50 = 27.5 nM Funct
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
351 4 5 10 -1.2 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4O)ncnc32)[C@H](O)[C@@H]1O
CHEMBL1800785 aa3r_human Human No 7.6 IC50 = 27.6 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
391 4 1 6 2.4 COc1cc(-c2nc3c([nH]2)C2=NC(C)CN2C(=O)N3Cc2ccccc2)n(C)n1
CHEMBL2181965 aa3r_human Human No 6.6 IC50 = 270 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells by [S35]GTPgammaS binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells by [S35]GTPgammaS binding assay
373 3 1 3 3.3 CCCn1c2nc([nH]c2c2=NCCn2c1=O)c1ccc(cc1)Br
CHEMBL3962269 aa3r_human Human No 7.6 IC50 = 28 nM Bind
Adenosine A3 Receptor Radioligand Binding Assay: .(R)- and (S)-(4-Fluorophenyl)(4-((5-methyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)methanol was tested in a radioligand binding assay, according to the procedure described in Olah et al., Mol. Pharmacol. 1994, 45, 978-982 and Salvatore et al., Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 10365-10369, in human recombinant CHO-K1 cells expressing the human adenosine A3 receptor. Incubations of a range of concentration of each compound were carried out in duplicates for 1 h at 25° C. in 25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA, in the presence of 0.5 nM [125I] AB-MECA. Non-specific binding was determined in the presence of 1 uM IB-MECA.Adenosine A3 Receptor Radioligand Binding Assay: .(R)- and (S)-(4-Fluorophenyl)(4-((5-methyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)methanol was tested in a radioligand binding assay, according to the procedure described in Olah et al., Mol. Pharmacol. 1994, 45, 978-982 and Salvatore et al., Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 10365-10369, in human recombinant CHO-K1 cells expressing the human adenosine A3 receptor. Incubations of a range of concentration of each compound were carried out in duplicates for 1 h at 25° C. in 25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA, in the presence of 0.5 nM [125I] AB-MECA. Non-specific binding was determined in the presence of 1 uM IB-MECA.
349 4 3 5 3.6 Cc1cc(Nc2nc([C@H](O)c3ccc(F)cc3)nc3ccccc23)n[nH]1
CHEMBL1766352 aa3r_human Human No 7.6 IC50 = 28 nM Funct
Antagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 minsAntagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 mins
386 4 2 5 4.0 COc1ccc(NC(=O)Nc2nn(-c3ccccc3)c(=O)c3ccccc23)cc1
CHEMBL339019 aa3r_human Human No 7.6 IC50 = 28 nM Bind
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
370 4 0 4 5.6 CCCCc1nc2ccc(Cl)cc2c2nc(-c3ccc(Cl)cc3)nn12
CHEMBL434639 aa3r_human Human No 7.6 IC50 = 28 nM Bind
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
320 4 0 4 4.4 CCCCc1nc2ccccc2c2nc(-c3ccc(F)cc3)nn12
CHEMBL211449 aa3r_human Human No 7.6 IC50 = 28.3 nM Funct
Antagonist activity against Cl-IB-MECA inhibited cAMP level in CHO cells transfected with human A3 receptorAntagonist activity against Cl-IB-MECA inhibited cAMP level in CHO cells transfected with human A3 receptor
485 4 0 7 4.5 O=C(c1ccccc1)N(C(=O)c1ccccc1)c1nc2ccccc2n2c(=O)n(-c3ccccc3)nc12
CHEMBL1559 aa3r_human Human Yes 5.6 IC50 = 2811 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1
CHEMBL91 aa3r_human Human Yes 5.6 IC50 = 2811 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1
CHEMBL2071044 aa3r_human Human No 7.5 IC50 = 29 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
514 5 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL490605 aa3r_human Human No 7.5 IC50 = 29.8 nM Funct
Antagonist activity at NECA-stimulated human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at NECA-stimulated human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
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
CHEMBL296419 aa3r_human Human Yes 4.5 IC50 = 29120 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2
CHEMBL1777844 aa3r_human Human No 4.5 IC50 = 29500 nM Funct
Antagonist activity at human adenosine receptor A3 expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assayAntagonist activity at human adenosine receptor A3 expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assay
296 4 0 4 3.9 CCOc1cccc2cc(-c3ccc(OC)cc3)c(=O)oc12
CHEMBL572765 aa3r_human Human No 8.5 IC50 = 3 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 2.0-4.3Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 2.0-4.3
392 3 2 8 3.1 Cn1cc2c(nc(NC(=O)Nc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL235513 aa3r_human Human No 8.5 IC50 = 3.1 nM Funct
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
445 4 1 7 3.9 COc1ccc(C(=O)Nc2nc3ccc(Cl)cc3n3c(=O)c(-c4ccccc4)nn23)cc1
CHEMBL165224 aa3r_human Human No 8.5 IC50 = 3.2 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 1.8-5.6Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 1.8-5.6
418 3 2 10 2.6 Cn1cc2c(nc(NC(=O)Nc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)n1
CHEMBL122987 aa3r_human Human No 8.5 IC50 = 3.3 nM Bind
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
338 5 1 6 3.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(SC)cc3)nn12
CHEMBL464859 aa3r_human Human Yes 8.4 IC50 = 3.8 nM Funct
Agonist activity at wild type human A3 receptor M174'5.35A 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 M174'5.35A 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
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL2071041 aa3r_human Human No 7.5 IC50 = 30 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
492 4 3 9 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NC4CCCC4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL2070885 aa3r_human Human Yes 7.5 IC50 = 30 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
477 5 2 9 3.4 Cn1cc2c(nc(NC(=O)NC3CCN(CC4CCCCC4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL2078778 aa3r_human Human Yes 7.5 IC50 = 30 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
477 5 2 9 3.4 Cn1cc2c(nc(NC(=O)NC3CCN(CC4CCCCC4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL1800736 aa3r_human Human No 7.5 IC50 = 30.3 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
339 4 1 5 2.1 C=CCN1C(=O)N2CC(CC)N=C2c2[nH]c(-c3cc(C)nn3C)nc21
CHEMBL2070882 aa3r_human Human No 6.5 IC50 = 301 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
423 5 2 9 2.3 CCCN1CCC(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)CC1
CHEMBL7002 aa3r_human Human Yes 5.5 IC50 = 3047 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1
CHEMBL3922797 aa3r_human Human No 6.5 IC50 = 308.3 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
458 8 2 9 5.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(NCc3cccnc3)sc12
CHEMBL212458 aa3r_human Human No 7.5 IC50 = 31.8 nM Funct
Antagonist activity against Cl-IB-MECA inhibited cAMP level in CHO cells transfected with human A3 receptorAntagonist activity against Cl-IB-MECA inhibited cAMP level in CHO cells transfected with human A3 receptor
515 5 0 8 4.5 COc1ccc(-n2nc3c(N(C(=O)c4ccccc4)C(=O)c4ccccc4)nc4ccccc4n3c2=O)cc1
CHEMBL4526845 aa3r_human Human No 5.5 IC50 = 3100 nM Funct
Antagonist activity at human adenosine receptor A3 expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assayAntagonist activity at human adenosine receptor A3 expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assay
316 1 1 3 3.9 O=c1oc2c(O)cccc2cc1-c1ccc(Br)cc1
CHEMBL209019 aa3r_human Human No 5.5 IC50 = 3169 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
493 5 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O
CHEMBL305660 aa3r_human Human Yes 5.5 IC50 = 3195.3 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1
CHEMBL338837 aa3r_human Human No 6.5 IC50 = 320 nM Bind
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
370 4 0 4 5.6 CCCCc1nc2cc(Cl)ccc2c2nc(-c3ccc(Cl)cc3)nn12
CHEMBL1219 aa3r_human Human Yes 5.5 IC50 = 3219 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
359 8 1 5 3.0 COCCCOc1ccnc(C[S+]([O-])c2nc3ccccc3[nH]2)c1C
CHEMBL2312719 aa3r_human Human Yes 6.5 IC50 = 324 nM Funct
Activity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation countingActivity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation counting
291 2 1 4 2.9 COc1ccc(-c2cc3c4ccccc4[nH]c(=O)n3n2)cc1
CHEMBL1201049 aa3r_human Human Yes 5.5 IC50 = 3249 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL808 aa3r_human Human Yes 5.5 IC50 = 3249 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL691 aa3r_human Human Yes 4.5 IC50 = 32925 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C
CHEMBL2042306 aa3r_human Human No 7.5 IC50 = 33 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
622 12 6 11 3.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL124897 aa3r_human Human No 7.5 IC50 = 33 nM Bind
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
366 5 0 5 4.9 CCCCc1nc2ccc(Cl)cc2c2nc(-c3ccc(OC)cc3)nn12
CHEMBL3358920 aa3r_human Human Yes 5.5 IC50 = 3300 nM Bind
Binding affinity to human adenosine A3 receptorBinding affinity to human adenosine A3 receptor
457 6 2 2 6.9 OC(=O)C[C@H]1CCc2c1[nH]c1c2cc(cc1)OCc1ccc(c(c1)C(F)(F)F)C1CCCC1
CHEMBL333843 aa3r_human Human No 5.5 IC50 = 3330 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
403 6 2 7 3.4 O=C(NCCCn1c(O)nc2ccccc21)OCc1cc2c(cc1Cl)OCO2
CHEMBL508338 aa3r_human Human No 5.5 IC50 = 3386 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
None None None None
CHEMBL188035 aa3r_human Human No 7.5 IC50 = 34 nM Funct
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
275 1 1 4 3.6 Cc1ccc(-n2cc3c(O)nc4ccccc4c3n2)cc1
CHEMBL2071040 aa3r_human Human No 7.5 IC50 = 34 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
466 4 3 9 2.0 CC(C)NC(=O)N1CCC(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)CC1
CHEMBL2071049 aa3r_human Human No 7.5 IC50 = 34 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
544 6 3 10 2.8 COc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1
CHEMBL121890 aa3r_human Human No 7.5 IC50 = 34 nM Bind
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
316 4 0 4 4.6 CCCCc1nc2ccccc2c2nc(-c3ccc(C)cc3)nn12
CHEMBL123669 aa3r_human Human No 7.5 IC50 = 34 nM Bind
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
366 5 0 5 4.9 CCCCc1nc2cc(Cl)ccc2c2nc(-c3ccc(OC)cc3)nn12
CHEMBL1800733 aa3r_human Human No 7.5 IC50 = 34.2 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
325 3 1 5 1.7 C=CCN1C(=O)N2CC(C)N=C2c2[nH]c(-c3cc(C)nn3C)nc21
CHEMBL508112 aa3r_human Human Yes 6.5 IC50 = 347 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1
CHEMBL326263 aa3r_human Human No 5.5 IC50 = 3480 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1
CHEMBL124138 aa3r_human Human No 7.5 IC50 = 35 nM Bind
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
346 6 0 5 4.7 CCCCc1nc2ccccc2c2nc(-c3ccc(OCC)cc3)nn12
CHEMBL1800734 aa3r_human Human No 7.5 IC50 = 35.9 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
325 3 1 5 1.7 C=CCN1C(=O)N2C[C@@H](C)N=C2c2[nH]c(-c3cc(C)nn3C)nc21
CHEMBL964 aa3r_human Human Yes 6.5 IC50 = 356 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC
CHEMBL3952824 aa3r_human Human No 6.4 IC50 = 360.8 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
380 6 1 7 4.6 CCc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL3407784 aa3r_mouse Mouse No 4.4 IC50 = 36000 nM Bind
Binding affinity to mouse adenosine A3 receptor expressed in HEK293 cell membranesBinding affinity to mouse adenosine A3 receptor expressed in HEK293 cell membranes
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
CHEMBL3753507 aa3r_human Human No 7.4 IC50 = 37 nM Funct
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
398 4 1 7 4.2 O=C(Nc1nc(-c2cccs2)nc2cn(-c3ccccc3)nc12)c1ccncc1
CHEMBL1080421 aa3r_human Human No 7.4 IC50 = 37.3 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL3601563 aa3r_human Human No 6.4 IC50 = 370 nM Bind
Inhibition of adenosine A3 receptor (unknown origin)Inhibition of adenosine A3 receptor (unknown origin)
339 3 0 3 5.0 COc1ccc2c([C@H]3CCc4ccc(Cl)cc43)nccc2c1OC
CHEMBL83 aa3r_human Human Yes 5.4 IC50 = 3701 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1
CHEMBL588119 aa3r_human Human Yes 5.4 IC50 = 3705.8 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1
CHEMBL420499 aa3r_human Human No 5.4 IC50 = 3730 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
497 9 0 5 5.3 COc1ccc(CN2CCN(C(=O)CCn3cc(C)c4ccccc43)CC2)cc1OCc1ccccc1
CHEMBL114613 aa3r_human Human No 5.4 IC50 = 3750 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
496 9 0 5 6.0 COc1ccc(SCCC(=O)N2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)cc1
CHEMBL210457 aa3r_human Human No 4.4 IC50 = 38050 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
455 6 2 8 1.1 COc1ccc(CNS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)nc1
CHEMBL3752438 aa3r_human Human No 7.4 IC50 = 39 nM Funct
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
422 5 1 7 4.1 COc1ccc(-c2nc(NC(=O)c3ccncc3)c3nn(-c4ccccc4)cc3n2)cc1
CHEMBL124725 aa3r_human Human No 8.4 IC50 = 4 nM Bind
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
306 4 1 5 3.3 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(C)cc3)nn12
CHEMBL1562432 aa3r_human Human No 8.4 IC50 = 4 nM Funct
Inverse agonist activity at human recombinant A3 adenosine receptor expressed CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human recombinant A3 adenosine receptor expressed CHO cells by [35S]GTPgammaS binding assay
397 2 1 3 4.4 CC[C@H]1N=c2n(C1)c(=O)n(c1c2[nH]c(n1)c1cc(Cl)cc(c1Cl)Cl)C
CHEMBL124137 aa3r_human Human No 8.4 IC50 = 4.1 nM Bind
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
278 3 1 5 2.6 CCCc1nc2[nH]ncc2c2nc(-c3ccccc3)nn12
CHEMBL330286 aa3r_human Human No 8.4 IC50 = 4.1 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 2.9-6.0Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 2.9-6.0
446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL348925 aa3r_human Human No 8.4 IC50 = 4.2 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 2.7-6.6Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 2.7-6.6
452 3 2 8 3.7 Cn1cc2c(nc(NC(=O)Nc3ccc(Br)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL3753544 aa3r_human Human No 8.4 IC50 = 4.3 nM Funct
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
451 6 1 7 4.8 COc1ccc(C(=O)Nc2nc(-c3ccc(OC)cc3)nc3cn(-c4ccccc4)nc23)cc1
CHEMBL3753976 aa3r_human Human No 8.4 IC50 = 4.4 nM Funct
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
481 5 0 9 5.2 O=C(c1ccco1)N(C(=O)c1ccco1)c1nc(-c2cccs2)nc2cn(-c3ccccc3)nc12
CHEMBL423934 aa3r_human Human No 8.4 IC50 = 4.5 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 3.0-6.9Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 3.0-6.9
450 6 2 8 4.8 CCCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL302765 aa3r_human Human Yes 8.4 IC50 = 4.5 nM Funct
Inhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human Adenosine A3 receptorInhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human Adenosine A3 receptor
432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC
CHEMBL351285 aa3r_human Human No 8.3 IC50 = 4.6 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 2.7-7.8Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 2.7-7.8
388 3 2 8 3.2 Cc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL65271 aa3r_human Human Yes 8.3 IC50 = 4.8 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 2.5-9.3Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 2.5-9.3
418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL344501 aa3r_human Human No 8.3 IC50 = 4.8 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 2.8-8.1Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 2.8-8.1
408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL122037 aa3r_human Human No 8.3 IC50 = 4.9 nM Bind
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
326 4 1 5 3.7 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(Cl)cc3)nn12
CHEMBL2070891 aa3r_human Human No 7.4 IC50 = 40 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
496 5 2 10 2.9 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccc(C#N)cc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL344706 aa3r_human Human No 7.4 IC50 = 40.2 nM Funct
Inhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human Adenosine A3 receptorInhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human Adenosine A3 receptor
283 3 1 8 1.7 CCCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1
CHEMBL1800735 aa3r_human Human No 7.4 IC50 = 40.9 nM Funct
Antagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counterAntagonist activity human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-mediated inhibition of forskolin-stimulated [3H]cAMP accumulation after 150 mins by scintillation counter
325 3 1 5 1.7 C=CCN1C(=O)N2C[C@H](C)N=C2c2[nH]c(-c3cc(C)nn3C)nc21
CHEMBL460291 aa3r_human Human Yes 5.4 IC50 = 4036 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
455 7 1 7 4.4 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OCC)C1c1ccccc1/C=C/C(=O)OC(C)(C)C
CHEMBL16687 aa3r_human Human Yes 6.4 IC50 = 406 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptorInhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor
285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1
CHEMBL326389 aa3r_human Human Yes 6.4 IC50 = 407 nM Funct
Inhibition of [35S]GTP-gamma-S, binding stimulated by 5 uM 5''-N-ethyluronamidoadenosine (NECA) in membranes of HEK293 cells expressing human Adenosine A3 receptorInhibition of [35S]GTP-gamma-S, binding stimulated by 5 uM 5''-N-ethyluronamidoadenosine (NECA) in membranes of HEK293 cells expressing human Adenosine A3 receptor
466 8 2 4 4.9 CCOC(=O)CNC(c1ccccc1)c1cc(Br)ccc1NC(=O)c1ccccc1
CHEMBL2071038 aa3r_human Human No 7.4 IC50 = 41 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
467 6 2 11 1.4 CCOC(=O)CN1CCC(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)CC1
CHEMBL454780 aa3r_human Human No 7.4 IC50 = 41 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assay
365 3 1 5 4.2 O=C(Nc1nc2ccccc2c2cn(-c3ccccc3)nc12)c1ccncc1
CHEMBL4098408 aa3r_human Human No 5.4 IC50 = 4140 nM Funct
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase in presence of [alpha-31P]ATPAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase in presence of [alpha-31P]ATP
413 4 3 8 2.2 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(Nc4ccc(Cl)cc4F)ncnc32)[C@@H]1O
CHEMBL459265 aa3r_human Human Yes 5.4 IC50 = 4166 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1
CHEMBL64894 aa3r_human Human Yes 5.4 IC50 = 4166 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1
CHEMBL547 aa3r_human Human Yes 5.4 IC50 = 4169 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C\C(=O)O)C(C)(C)CCC1
CHEMBL115249 aa3r_human Human No 5.4 IC50 = 4180 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
396 9 0 4 4.0 CCOc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1
CHEMBL3415025 aa3r_human Human No 7.4 IC50 = 42 nM Funct
Antagonist activity against human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-induced inhibition of forskolin-induced cAMP production by scintillation counting methodAntagonist activity against human adenosine A3 receptor expressed in CHO cells assessed as blockade of Cl-IB-MECA-induced inhibition of forskolin-induced cAMP production by scintillation counting method
277 1 1 4 3.0 Cc1nc2sc(-c3ccc(Cl)cc3)nc2c(=O)[nH]1
CHEMBL2070892 aa3r_human Human No 7.4 IC50 = 42 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
516 6 2 11 3.0 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccc([N+](=O)[O-])cc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL125062 aa3r_human Human No 7.4 IC50 = 42 nM Bind
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
334 6 1 5 4.0 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(CCC)cc3)nn12
CHEMBL611095 aa3r_human Human No 7.4 IC50 = 42 nM Funct
Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptorInhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor
560 9 5 11 0.0 C=CCN(C)S(=O)(=O)c1ccc(NC(=O)Nc2ncnc3c2ncn3C2O[C@H](C(=O)NCC)[C@@H](O)[C@H]2O)cc1
CHEMBL325516 aa3r_human Human No 5.4 IC50 = 4210 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL11359 aa3r_human Human No 5.4 IC50 = 4243 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
None None None None
CHEMBL2068237 aa3r_human Human No 5.4 IC50 = 4243 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
None None None None
CHEMBL4289256 aa3r_human Human No 6.4 IC50 = 428.2 nM Funct
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as reduction in Cl-IB-MECA-induced inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 10 mins followed by Cl-IB-MECA addition measured after 30 mins by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as reduction in Cl-IB-MECA-induced inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 10 mins followed by Cl-IB-MECA addition measured after 30 mins by liquid scintillation counting method
331 7 1 5 4.1 CCCOc1cc(NC(C)=O)nc(S[C@@H](C)c2ccccc2)n1
CHEMBL4102409 aa3r_human Human No 6.4 IC50 = 430 nM Bind
Displacement of [3H]HEMADO from human adenosine A3 receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]HEMADO from human adenosine A3 receptor expressed in HEK293 cell membranes after 90 mins
368 6 1 6 4.0 CCCn1c(Oc2cccc(OC)c2)nc2nc(C3CCCC3)[nH]c2c1=O
CHEMBL210969 aa3r_human Human No 5.4 IC50 = 4314 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
553 8 2 7 3.3 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(CC)c1=O
CHEMBL787 aa3r_human Human Yes 6.4 IC50 = 434 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1
CHEMBL2071042 aa3r_human Human No 7.4 IC50 = 44 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
506 4 3 9 2.9 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NC4CCCCC4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL20555 aa3r_human Human No 7.4 IC50 = 45 nM Funct
Antagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECA
447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C
CHEMBL554955 aa3r_human Human No 7.4 IC50 = 45 nM Funct
Antagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECA
447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C
CHEMBL2070890 aa3r_human Human No 7.4 IC50 = 45 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
501 6 2 10 3.1 COc1ccc(CN2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1
CHEMBL339556 aa3r_human Human No 7.4 IC50 = 45 nM Bind
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
336 4 0 4 4.9 CCCCc1nc2ccc(Cl)cc2c2nc(-c3ccccc3)nn12
CHEMBL340182 aa3r_human Human No 6.4 IC50 = 450 nM Bind
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
368 5 1 5 4.7 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(-c4ccccc4)cc3)nn12
CHEMBL2071045 aa3r_human Human No 7.3 IC50 = 46 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
542 7 3 9 3.2 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL21572 aa3r_human Human No 6.3 IC50 = 466 nM Funct
Antagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECA
463 5 1 11 2.9 CSc1c2c(nc(NC(=O)Cc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)nn1C
CHEMBL1062 aa3r_human Human Yes 5.3 IC50 = 4730 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
330 1 1 3 3.8 CC(=O)[C@@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C
CHEMBL104 aa3r_human Human Yes 5.3 IC50 = 4752 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1
CHEMBL305906 aa3r_human Human Yes 5.3 IC50 = 4758 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1
CHEMBL334255 aa3r_human Human Yes 5.3 IC50 = 4758 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1
CHEMBL340093 aa3r_human Human No 7.3 IC50 = 48 nM Bind
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
336 4 0 4 4.9 CCCCc1nc2cc(Cl)ccc2c2nc(-c3ccccc3)nn12
CHEMBL217899 aa3r_human Human Yes 5.3 IC50 = 4800 nM Bind
Inhibition of adenosine A3 receptorInhibition of adenosine A3 receptor
339 3 0 6 4.1 CCc1nn(C2CCCC2)c2c1CCn1c(-c3cccs3)nnc1-2
CHEMBL516966 aa3r_human Human No 7.3 IC50 = 49 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assay
368 3 1 5 4.7 Cc1ccc(C(=O)Nc2nc3ccccc3c3cn(-c4ccccc4)nc23)o1
CHEMBL125288 aa3r_human Human No 6.3 IC50 = 490 nM Bind
Binding affinity for human adenosine A3 receptor expressed in HEK293 cellsBinding affinity for human adenosine A3 receptor expressed in HEK293 cells
370 4 0 4 5.3 CCCCc1nc2ccccc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12
CHEMBL125288 aa3r_human Human No 6.3 IC50 = 490 nM Bind
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
370 4 0 4 5.3 CCCCc1nc2ccccc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12
CHEMBL186113 aa3r_human Human Yes 8.3 IC50 = 5 nM Funct
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
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
CHEMBL434534 aa3r_human Human No 8.3 IC50 = 5 nM Funct
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
337 4 1 6 1.9 CCCn1c(=O)c2c(nc3[nH]c(C)cn32)n(Cc2ccccc2)c1=O
CHEMBL123346 aa3r_human Human No 8.3 IC50 = 5 nM Bind
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
368 5 1 5 4.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(-c4ccccc4)cc3)nn12
CHEMBL123346 aa3r_human Human No 8.3 IC50 = 5 nM Bind
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
368 5 1 5 4.7 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(-c4ccccc4)cc3)nn12
CHEMBL304726 aa3r_human Human No 8.3 IC50 = 5.1 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 3.5-7.6Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 3.5-7.6
430 6 2 9 3.6 C=CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL302765 aa3r_human Human Yes 8.3 IC50 = 5.2 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 4.4-6.5Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 4.4-6.5
432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC
CHEMBL142562 aa3r_human Human No 8.3 IC50 = 5.3 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human A3 adenosine receptorInhibition of cAMP accumulation in CHO cells expressing human A3 adenosine receptor
394 3 3 7 3.6 O=C(Nc1cccc(Cl)c1)Nc1nc2n[nH]cc2c2nc(-c3ccco3)nn12
CHEMBL138332 aa3r_human Human No 8.3 IC50 = 5.3 nM Funct
Inhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human A3 receptorInhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human A3 receptor
436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL3752840 aa3r_human Human No 8.3 IC50 = 5.3 nM Funct
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
397 4 1 6 4.8 O=C(Nc1nc(-c2cccs2)nc2cn(-c3ccccc3)nc12)c1ccccc1
CHEMBL125340 aa3r_human Human No 8.3 IC50 = 5.4 nM Bind
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
356 5 2 6 2.7 O=C(O)CCCc1nc2[nH]cnc2c2nc(-c3ccc(Cl)cc3)nn12
CHEMBL3751978 aa3r_human Human No 8.3 IC50 = 5.5 nM Funct
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
387 4 1 7 4.4 O=C(Nc1nc(-c2cccs2)nc2cn(-c3ccccc3)nc12)c1ccco1
CHEMBL354161 aa3r_human Human No 8.3 IC50 = 5.5 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptorInhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptor
419 4 2 10 2.8 Cn1cc2c(nc(NC(=O)Nc3ccc([N+](=O)[O-])cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL138332 aa3r_human Human No 8.3 IC50 = 5.5 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 4.0-7.5Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 4.0-7.5
436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1
CHEMBL3752862 aa3r_human Human No 8.3 IC50 = 5.6 nM Funct
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
403 4 1 7 4.9 O=C(Nc1nc(-c2cccs2)nc2cn(-c3ccccc3)nc12)c1cccs1
CHEMBL351211 aa3r_human Human No 8.3 IC50 = 5.6 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 3.0-10.8Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 3.0-10.8
404 4 2 9 2.9 COc1ccccc1NC(=O)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12
CHEMBL1094132 aa3r_human Human No 8.2 IC50 = 5.7 nM Funct
Antagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
420 5 2 5 5.2 O=C(Nc1ccccc1)Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12
CHEMBL125647 aa3r_human Human No 8.2 IC50 = 5.9 nM Bind
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
282 4 1 6 2.6 CCCCc1nc2[nH]cnc2c2nc(-c3ccco3)nn12
CHEMBL2070889 aa3r_human Human No 7.3 IC50 = 50 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
485 5 2 9 3.4 Cc1ccc(CN2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1
CHEMBL1935748 aa3r_human Human No 7.3 IC50 = 50 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by competition protein binding assay
431 6 2 8 4.4 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2c1
CHEMBL611091 aa3r_human Human No 7.3 IC50 = 50 nM Funct
Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptorInhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor
562 9 5 11 0.3 CCNC(=O)[C@H]1OC(n2cnc3c(NC(=O)Nc4ccc(S(=O)(=O)N(CC)CC)cc4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL1935753 aa3r_human Human No 6.3 IC50 = 500 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by competition protein binding assay
283 3 1 8 1.7 CCCn1ncc2nc(N)n3nc(-c4ccco4)nc3c21
CHEMBL116735 aa3r_human Human No 5.3 IC50 = 5080 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1
CHEMBL1200633 aa3r_human Human Yes 6.3 IC50 = 512.1 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O
CHEMBL30008 aa3r_human Human Yes 5.3 IC50 = 5198 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1
CHEMBL539027 aa3r_human Human Yes 5.3 IC50 = 5198 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1
CHEMBL552659 aa3r_human Human Yes 5.3 IC50 = 5198 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1
CHEMBL408 aa3r_human Human Yes 5.3 IC50 = 5208 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2
CHEMBL388590 aa3r_human Human Yes 5.3 IC50 = 5222 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1
CHEMBL211813 aa3r_human Human No 5.3 IC50 = 5249 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
533 5 1 8 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)s5)CC4)cc3)cc2n(C)c1=O
CHEMBL38 aa3r_human Human Yes 5.3 IC50 = 5275 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1
CHEMBL1094143 aa3r_human Human No 7.3 IC50 = 53 nM Funct
Antagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
405 5 1 5 4.8 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1ccccc1
CHEMBL954 aa3r_human Human Yes 5.3 IC50 = 5350 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1
CHEMBL518258 aa3r_human Human No 7.3 IC50 = 54 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assay
378 3 1 4 5.1 Cc1ccc(C(=O)Nc2nc3ccccc3c3cn(-c4ccccc4)nc23)cc1
CHEMBL115076 aa3r_human Human No 5.3 IC50 = 5470 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
443 3 1 6 3.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC2(CC1)C(=O)NCN2c1ccccc1
CHEMBL608755 aa3r_human Human No 7.3 IC50 = 55 nM Funct
Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptorInhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor
562 8 5 11 0.3 CCNC(=O)[C@H]1OC(n2cnc3c(NC(=O)Nc4ccc(S(=O)(=O)N(C)C(C)C)cc4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL40583 aa3r_human Human Yes 5.3 IC50 = 5544 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
268 0 0 0 5.6 Cc1ccc2cc3c(ccc4ccccc43)c3c2c1CC3
CHEMBL672 aa3r_human Human Yes 5.2 IC50 = 5701 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
360 6 0 4 4.7 CC(C)OC(=O)C(C)(C)Oc1ccc(C(=O)c2ccc(Cl)cc2)cc1
CHEMBL469664 aa3r_human Human Yes 5.2 IC50 = 5760 nM Bind
Inhibition of adenosine A3 receptorInhibition of adenosine A3 receptor
508 5 2 3 5.3 O=C(Nc1ccc(Br)cc1)c1cccc(S(=O)(=O)Nc2ccc(Br)cc2)c1
CHEMBL116463 aa3r_human Human No 5.2 IC50 = 5980 nM Bind
Inhibition of human adenosine A3 receptorInhibition of human adenosine A3 receptor
517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1
CHEMBL340221 aa3r_human Human No 8.2 IC50 = 6.2 nM Bind
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
264 2 1 5 2.2 CCc1nc2[nH]ncc2c2nc(-c3ccccc3)nn12
CHEMBL341376 aa3r_human Human No 8.2 IC50 = 6.4 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptorInhibition of IB-MECA agonist-mediated cAMP production in membranes of CHO cells expressing human Adenosine A3 receptor
373 4 1 8 2.5 Cn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1
CHEMBL65271 aa3r_human Human Yes 8.2 IC50 = 6.5 nM Funct
Inhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human A3 receptorInhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human A3 receptor
418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL164686 aa3r_human Human No 8.2 IC50 = 6.6 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 3.7-117Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 3.7-117
442 3 2 8 3.9 Cn1cc2c(nc(NC(=O)Nc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL357663 aa3r_human Human No 8.2 IC50 = 6.8 nM Funct
Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 5.1-8.9Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor; range 5.1-8.9
446 4 2 9 4.1 COc1ccc(NC(=O)Nc2nc3nn(C(C)(C)C)cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL2042301 aa3r_human Human No 4.2 IC50 = 60097 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
658 9 6 11 3.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL195437 aa3r_human Human Yes 5.2 IC50 = 6014 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1
CHEMBL2322898 aa3r_human Human No 7.2 IC50 = 61 nM Funct
Inhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECAInhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECA
405 5 1 5 4.7 O=C(Cc1ccccc1)Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12
CHEMBL123310 aa3r_human Human Yes 6.2 IC50 = 610 nM Bind
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
230 3 1 5 1.7 CCCCc1nc2[nH]cnc2c2nc(C)nn12
CHEMBL1381098 aa3r_human Human Yes 5.2 IC50 = 6100 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
185 1 0 2 3.6 S=C=Nc1cccc2ccccc12
CHEMBL2322907 aa3r_human Human No 7.2 IC50 = 63 nM Funct
Inhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECAInhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECA
421 5 1 6 4.7 COc1ccc(-n2cc3nc(-c4ccccc4)nc(NC(=O)c4ccccc4)c3n2)cc1
CHEMBL1262 aa3r_human Human Yes 6.2 IC50 = 634.5 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1
CHEMBL496 aa3r_human Human Yes 6.2 IC50 = 638.9 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl
CHEMBL209208 aa3r_human Human No 5.2 IC50 = 6438 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
455 7 2 8 1.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCOc4ccccn4)cc3)cc2n(C)c1=O
CHEMBL611104 aa3r_human Human No 7.2 IC50 = 65 nM Funct
Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptorInhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor
586 11 5 11 0.6 C=CCN(CC=C)S(=O)(=O)c1ccc(NC(=O)Nc2ncnc3c2ncn3C2O[C@H](C(=O)NCC)[C@@H](O)[C@H]2O)cc1
CHEMBL2322930 aa3r_human Human No 7.2 IC50 = 65 nM Funct
Inhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECAInhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECA
391 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12)c1ccccc1
CHEMBL464859 aa3r_human Human Yes 4.2 IC50 = 65600 nM Funct
Inhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptorInhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptor
308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N
CHEMBL72613 aa3r_human Human No 5.2 IC50 = 6700 nM Funct
Inhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptorInhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptor
593 10 3 14 2.3 CO/C(=C\c1ccc(O)cc1)C(=O)O[C@@H]1[C@H](OC(=O)/C=C/c2c[nH]cn2)[C@@H](CSC)O[C@H]1n1cnc2c(N)ncnc21
CHEMBL122928 aa3r_human Human No 6.2 IC50 = 680 nM Bind
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
306 5 1 5 2.9 CCCCc1nc2[nH]cnc2c2nc(Cc3ccccc3)nn12
CHEMBL2042311 aa3r_human Human No 8.2 IC50 = 7.0 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
492 7 4 9 1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O
CHEMBL88147 aa3r_human Human Yes 8.1 IC50 = 7.2 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells by [S35]GTPgammaS binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells by [S35]GTPgammaS binding assay
403 4 1 6 4.4 O=C(Nc1nc2ccc(cc2c2n1nc(n2)c1ccco1)Cl)Cc1ccccc1
CHEMBL1094131 aa3r_human Human No 8.1 IC50 = 7.6 nM Funct
Antagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
439 5 1 5 5.4 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1cccc(Cl)c1
CHEMBL164992 aa3r_human Human No 8.1 IC50 = 7.8 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 5.5-10.9Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 5.5-10.9
404 4 2 9 2.9 COc1cccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)c1
CHEMBL305975 aa3r_human Human Yes 8.1 IC50 = 7.9 nM Funct
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
371 4 2 5 4.3 COc1ccccc1NC(=O)Nc1nc(-c2ccccn2)nc2ccccc12
CHEMBL4282074 aa3r_human Human No 8.1 IC50 = 7.9 nM Funct
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as reduction in Cl-IB-MECA-induced inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 10 mins followed by Cl-IB-MECA addition measured after 30 mins by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cells assessed as reduction in Cl-IB-MECA-induced inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 10 mins followed by Cl-IB-MECA addition measured after 30 mins by liquid scintillation counting method
331 7 1 5 4.1 CCCSc1nc(NC(C)=O)cc(O[C@@H](C)c2ccccc2)n1
CHEMBL4078360 aa3r_human Human No 6.2 IC50 = 701 nM Funct
Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase in presence of [alpha-31P]ATPAntagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase in presence of [alpha-31P]ATP
507 5 3 10 3.1 Cc1cc(C)n(C[C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1
CHEMBL277041 aa3r_human Human Yes 4.2 IC50 = 71000 nM Funct
Inhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptorInhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptor
297 3 3 9 -0.6 CSC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O
CHEMBL1726 aa3r_human Human Yes 5.2 IC50 = 7120 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
388 6 1 7 3.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1c1ccccc1[N+](=O)[O-]
CHEMBL193 aa3r_human Human Yes 5.1 IC50 = 7214 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-]
CHEMBL18797 aa3r_human Human Yes 5.1 IC50 = 7231 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
340 4 1 2 5.4 CSc1ccc(/C=C2/C(C)=C(CC(=O)O)c3cc(F)ccc32)cc1
CHEMBL1670 aa3r_human Human Yes 5.1 IC50 = 7445 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1
CHEMBL3973260 aa3r_human Human No 6.1 IC50 = 746.7 nM Funct
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
378 6 1 7 4.6 C=Cc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1
CHEMBL1935747 aa3r_human Human No 7.1 IC50 = 75 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of Cl-IB-MECA-induced cAMP production by competition protein binding assay
403 4 2 8 3.5 COc1ccc(NC(=O)Nc2nc3cn(C)cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL2042302 aa3r_human Human No 6.1 IC50 = 756 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
674 9 7 12 3.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O
CHEMBL519614 aa3r_human Human No 7.1 IC50 = 76 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assay
365 3 1 5 4.2 O=C(Nc1nc2ccccc2c2cn(-c3ccccc3)nc12)c1cccnc1
CHEMBL212528 aa3r_human Human No 5.1 IC50 = 7600 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
483 8 2 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccc(OC)cn4)cc3)cc2n(C)c1=O
CHEMBL3769641 aa3r_human Human No 7.1 IC50 = 79.4 nM Funct
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
458 5 5 10 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC45CC6CC(CC(O)(C6)C4)C5)ncnc32)[C@H](O)[C@@H]1O
CHEMBL2042304 aa3r_human Human No 8.1 IC50 = 8 nM Funct
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
506 8 4 9 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O
CHEMBL235543 aa3r_human Human No 8.1 IC50 = 8.2 nM Funct
Antagonist activity at human adenosine A3 receptor after 15 to 30 minsAntagonist activity at human adenosine A3 receptor after 15 to 30 mins
494 5 4 9 0.6 OC[C@]12CN[C@H]([C@@H]1O)[C@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)O2
CHEMBL1096078 aa3r_human Human No 8.1 IC50 = 8.2 nM Funct
Antagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A3 receptor expressed in CHO cells assessed as blockade of NECA-mediated inhibition of forskolin-stimulated [3H]cAMP production treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
450 6 2 6 5.2 COc1ccc(NC(=O)Nc2nc(-c3ccccc3)nc3nn(Cc4ccccc4)cc23)cc1
CHEMBL339066 aa3r_human Human No 8.1 IC50 = 8.2 nM Bind
Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter
380 4 0 4 5.1 CCCCc1nc2ccccc2c2nc(-c3ccc(Br)cc3)nn12
CHEMBL339066 aa3r_human Human No 8.1 IC50 = 8.2 nM Bind
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
380 4 0 4 5.1 CCCCc1nc2ccccc2c2nc(-c3ccc(Br)cc3)nn12
CHEMBL164281 aa3r_human Human No 8.1 IC50 = 8.2 nM Funct
Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 4.4-15.2Inhibition of IB-MECA agonist-mediated cAMP production in CHO cell membranes expressing human Adenosine A3 receptor; range 4.4-15.2
408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3ccccc3Cl)n3nc(-c4ccco4)nc23)n1
CHEMBL1766358 aa3r_human Human No 8.1 IC50 = 8.3 nM Funct
Antagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 minsAntagonist activity at human cloned adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP accumulation after 15 mins
416 5 2 6 4.0 COc1ccc(OC)c(NC(=O)Nc2nn(-c3ccccc3)c(=O)c3ccccc23)c1
CHEMBL3754475 aa3r_human Human No 8.1 IC50 = 8.5 nM Funct
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
411 5 1 6 4.7 O=C(Cc1ccccc1)Nc1nc(-c2cccs2)nc2cn(-c3ccccc3)nc12
CHEMBL209122 aa3r_human Human No 8.1 IC50 = 8.6 nM Funct
Antagonist activity against Cl-IB-MECA inhibited cAMP level in CHO cells transfected with human A3 receptorAntagonist activity against Cl-IB-MECA inhibited cAMP level in CHO cells transfected with human A3 receptor
426 4 2 8 2.9 COc1ccc(-n2nc3c(NC(=O)c4ccccc4)nc4c(N)cccc4n3c2=O)cc1
CHEMBL332800 aa3r_human Human No 8.1 IC50 = 8.7 nM Bind
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
398 6 2 6 3.7 O=C(O)CCCc1nc2[nH]cnc2c2nc(-c3ccc(-c4ccccc4)cc3)nn12
CHEMBL2322908 aa3r_human Human No 7.1 IC50 = 80 nM Funct
Inhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECAInhibition of human A3 adenosine receptor transfected in CHO cells assessed as inhibition of forskolin-induced cyclic AMP production after 10 mins by competitive protein binding assay in presence of CI-IB-MECA
435 6 1 6 4.7 COc1ccc(-n2cc3nc(-c4ccccc4)nc(NC(=O)Cc4ccccc4)c3n2)cc1
CHEMBL265587 aa3r_human Human No 7.1 IC50 = 81 nM Funct
Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptorInhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor
506 6 6 11 -1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC(=O)Nc4ccc(S(N)(=O)=O)cc4)ncnc32)[C@H](O)[C@@H]1O
CHEMBL22113 aa3r_human Human No 6.1 IC50 = 813 nM Funct
Antagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECA
450 5 2 10 3.6 COc1ccc(NC(=O)Nc2nc3nn(C)c(SC)c3c3nc(-c4ccco4)nn23)cc1
CHEMBL330664 aa3r_human Human No 7.1 IC50 = 82 nM Funct
Activity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation countingActivity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation counting
295 1 1 4 3.9 Oc1nc2ccccc2c2cc(-c3ccc(Cl)cc3)nn12
CHEMBL2070887 aa3r_human Human No 7.1 IC50 = 82 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
489 5 2 9 3.2 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccc(F)cc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL2071050 aa3r_human Human No 7.1 IC50 = 82 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL2078766 aa3r_human Human No 7.1 IC50 = 82 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL290106 aa3r_human Human Yes 6.1 IC50 = 829 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O
CHEMBL464040 aa3r_human Human No 7.1 IC50 = 83 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assayAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of CI-IB-MECA-mediated inhibition of cAMP accumulation by competition protein binding assay
388 3 1 5 5.1 O=C(Nc1nc2ccccc2c2cn(-c3ccc(Cl)cc3)nc12)c1ccco1
CHEMBL1082723 aa3r_human Human Yes 5.1 IC50 = 8300 nM Bind
Binding affinity to human recombinant adenosine 3 receptorBinding affinity to human recombinant adenosine 3 receptor
389 0 3 2 4.3 C[C@H]1Cc2c([nH]c3cc(Cl)c(F)cc23)[C@@]2(N1)C(=O)Nc1ccc(Cl)cc12
CHEMBL2079587 aa3r_human Human Yes 5.1 IC50 = 8325 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
328 0 2 2 4.1 C[C@]12Cc3c[nH]nc3C[C@@H]1CC[C@@H]1[C@@H]2CC[C@@]2(C)[C@H]1CC[C@]2(C)O
CHEMBL212464 aa3r_human Human No 6.1 IC50 = 844 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
467 8 2 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O
CHEMBL2203622 aa3r_human Human No 6.1 IC50 = 850 nM Funct
Antagonist activity at adenosine A3 receptorAntagonist activity at adenosine A3 receptor
298 0 0 4 4.0 Cn1c2cnc1OCC/C=C\CCCCOc1ccccc1-2
CHEMBL3407784 aa3r_canlf Dog No 5.1 IC50 = 8500 nM Bind
Binding affinity to canine adenosine A3 receptor expressed in HEK293 cell membranesBinding affinity to canine adenosine A3 receptor expressed in HEK293 cell membranes
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
CHEMBL280888 aa3r_human Human No 6.1 IC50 = 852 nM Funct
Antagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECAAntagonist activity as inhibition of cAMP generation after agonist-modulation of Adenosine A3 receptor with 100 nM CI-IB-MECA
329 4 1 9 2.4 CCCSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C
CHEMBL119385 aa3r_human Human Yes 5.1 IC50 = 8547 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
435 3 0 5 5.5 O=c1ncn2nc(Sc3ccc(F)cc3F)ccc2c1-c1c(Cl)cccc1Cl
CHEMBL3215298 aa3r_human Human Yes 6.1 IC50 = 870 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
None None None CC[C@H](C)[C@H]1O[C@]2(C=C[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(C=C[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O
CHEMBL99193 aa3r_human Human No 7.1 IC50 = 88 nM Funct
Activity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation countingActivity at human adenosine A3 receptor transfected in CHO cells assessed as Cl-IB-MECA-inhibited cAMP accumulation by scintillation counting
275 1 1 4 3.6 Cc1ccc(-c2cc3c4ccccc4nc(O)n3n2)cc1
CHEMBL3908849 aa3r_human Human No 5.1 IC50 = 8800 nM Bind
Antagonist activity at adenosine 3 receptor (unknown origin)Antagonist activity at adenosine 3 receptor (unknown origin)
475 4 3 5 4.1 NC(=O)n1cc(NC(=O)N2CCC[C@H]2C(=O)Nc2cccc(OC(F)(F)F)c2)c2ccccc21
CHEMBL210383 aa3r_human Human No 5.1 IC50 = 8888 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(C)c1=O
CHEMBL124887 aa3r_human Human No 8.0 IC50 = 9.1 nM Bind
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
412 7 2 6 4.1 O=C(O)CCCCc1nc2[nH]cnc2c2nc(-c3ccc(-c4ccccc4)cc3)nn12
CHEMBL270676 aa3r_human Human No 8.0 IC50 = 9.2 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced cAMP accumulationAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced cAMP accumulation
351 7 1 5 4.2 CCCSc1nc(NC(C)=O)cc(OCc2ccc(Cl)cc2)n1
CHEMBL2071047 aa3r_human Human No 7.1 IC50 = 90 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
548 5 3 9 3.4 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(Cl)cc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL2070888 aa3r_human Human No 7.0 IC50 = 91 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
505 5 2 9 3.7 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccc(Cl)cc4)CC3)n3nc(-c4ccco4)nc23)n1
CHEMBL2070881 aa3r_human Human No 6.0 IC50 = 910 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as forskolin/C1-IB-MECA-induced inhibition of cAMP production
395 3 2 9 1.5 CN1CCC(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)CC1
CHEMBL86754 aa3r_human Human Yes 6.0 IC50 = 933 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
397 0 1 2 3.2 Oc1c(I)cc(I)c2cccnc12
CHEMBL212416 aa3r_human Human No 6.0 IC50 = 950 nM Bind
Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cellsDisplacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells
546 7 1 8 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C#N)cc5)CC4)cc3)cc2n(C)c1=O
CHEMBL12131 aa3r_human Human Yes 7.0 IC50 = 96 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
662 4 2 3 7.1 Cc1cc(C(C#N)c2ccc(Cl)cc2)c(Cl)cc1NC(=O)c1cc(I)cc(I)c1O
CHEMBL1386 aa3r_human Human No 6.0 IC50 = 989.1 nM Bind
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
None None None None
CHEMBL2181968 aa3r_human Human No 9.8 Kd = 0.2 nM Funct
Antagonist activity at human recombinant adenosine A3 receptor expressed in HEK293 cellsAntagonist activity at human recombinant adenosine A3 receptor expressed in HEK293 cells
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
CHEMBL2023738 aa3r_human Human No 9.5 Kd = 0.3 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrsAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrs
533 14 3 9 3.2 COc1ccc(-n2nc3c(NC(=O)CCC(=O)NCCCCCCCCN)nc4ccccc4n3c2=O)cc1
CHEMBL2024149 aa3r_human Human No 9.4 Kd = 0.4 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrsAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrs
None None None COc1ccc(-n2nc3c(NC(=O)CCC(=O)NCCOCCOCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)nc4ccccc4n3c2=O)cc1
CHEMBL304726 aa3r_human Human No 9.1 Kd = 0.8 nM Bind
Binding affinity against human Adenosine A3 receptor in CHO cellsBinding affinity against human Adenosine A3 receptor in CHO cells
430 6 2 9 3.6 C=CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL4062581 aa3r_human Human No 8.9 Kd = 1.3 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]GTPgammaS binding measured after 30 minsAntagonist activity at human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]GTPgammaS binding measured after 30 mins
406 6 0 8 2.3 COc1cccc(Cn2c(=O)n(CC3CC3)c(=O)c3c2nc2cc(OC)ccn23)c1
CHEMBL3939800 aa3r_human Human Yes 8.9 Kd = 1.4 nM Bind
Adenosine A3 Receptor Radioligand Binding Assay: .(R)- and (S)-(4-Fluorophenyl)(4-((5-methyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)methanol was tested in a radioligand binding assay, according to the procedure described in Olah et al., Mol. Pharmacol. 1994, 45, 978-982 and Salvatore et al., Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 10365-10369, in human recombinant CHO-K1 cells expressing the human adenosine A3 receptor. Incubations of a range of concentration of each compound were carried out in duplicates for 1 h at 25° C. in 25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA, in the presence of 0.5 nM [125I] AB-MECA. Non-specific binding was determined in the presence of 1 uM IB-MECA.Adenosine A3 Receptor Radioligand Binding Assay: .(R)- and (S)-(4-Fluorophenyl)(4-((5-methyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)methanol was tested in a radioligand binding assay, according to the procedure described in Olah et al., Mol. Pharmacol. 1994, 45, 978-982 and Salvatore et al., Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 10365-10369, in human recombinant CHO-K1 cells expressing the human adenosine A3 receptor. Incubations of a range of concentration of each compound were carried out in duplicates for 1 h at 25° C. in 25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA, in the presence of 0.5 nM [125I] AB-MECA. Non-specific binding was determined in the presence of 1 uM IB-MECA.
349 4 3 5 3.6 Cc1cc(Nc2nc([C@@H](O)c3ccc(F)cc3)nc3ccccc23)n[nH]1
CHEMBL2023739 aa3r_human Human No 8.8 Kd = 1.4 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrsAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrs
364 4 2 8 0.9 COc1ccc(-n2nc3c(NC(=O)CN)nc4ccccc4n3c2=O)cc1
CHEMBL4462442 aa3r_human Human No 5.9 Kd = 1258.9 nM Funct
Competitive surmountable antagonist activity at human A3 adenosine receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]-GTPgammaS binding preincubated for 60 mins followed by 2-Cl-IB-MECA and [35S]-GTPgammaS addition and measured after 30 minsCompetitive surmountable antagonist activity at human A3 adenosine receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]-GTPgammaS binding preincubated for 60 mins followed by 2-Cl-IB-MECA and [35S]-GTPgammaS addition and measured after 30 mins
513 9 1 10 1.5 CCCn1c(=O)c2c(nc3cc(OC)ccn32)n(CCCNC(=O)c2ccc(S(C)(=O)=O)cc2)c1=O
CHEMBL2024151 aa3r_human Human No 6.8 Kd = 147.9 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrsAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrs
1175 27 4 17 6.6 CCN1/C(=C/C=C/C=C/C2=[N+](CCCCCC(=O)NCCOCCOCCNC(=O)CCC(=O)Nc3nc4ccccc4n4c(=O)n(-c5ccc(OC)cc5)nc34)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(C)c2cc(S(=O)(=O)O)ccc21
CHEMBL322968 aa3r_human Human No 6.8 Kd = 158.5 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]GTPgammaS binding preincubated with or without for 60 mins followed by addition of 2-Cl-IB-MECA and [35S]GTPgammaS measured after 30 minsAntagonist activity at human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]GTPgammaS binding preincubated with or without for 60 mins followed by addition of 2-Cl-IB-MECA and [35S]GTPgammaS measured after 30 mins
322 3 1 6 1.4 COc1ccn2c(c1)nc1c2c(=O)[nH]c(=O)n1Cc1ccccc1
CHEMBL447664 aa3r_human Human Yes 5.8 Kd = 1584.9 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A3 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay
321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N
CHEMBL2024148 aa3r_human Human No 7.8 Kd = 16.6 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrsAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrs
None None None COc1ccc(-n2nc3c(NC(=O)CCC(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)nc4ccccc4n3c2=O)cc1
CHEMBL2023737 aa3r_human Human No 7.7 Kd = 20.9 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrsAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrs
537 14 3 11 0.9 COc1ccc(-n2nc3c(NC(=O)CCC(=O)NCCOCCOCCN)nc4ccccc4n3c2=O)cc1
CHEMBL3962269 aa3r_human Human No 7.5 Kd = 28.5 nM Bind
Adenosine A3 Receptor Radioligand Binding Assay: .(R)- and (S)-(4-Fluorophenyl)(4-((5-methyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)methanol was tested in a radioligand binding assay, according to the procedure described in Olah et al., Mol. Pharmacol. 1994, 45, 978-982 and Salvatore et al., Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 10365-10369, in human recombinant CHO-K1 cells expressing the human adenosine A3 receptor. Incubations of a range of concentration of each compound were carried out in duplicates for 1 h at 25° C. in 25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA, in the presence of 0.5 nM [125I] AB-MECA. Non-specific binding was determined in the presence of 1 uM IB-MECA.Adenosine A3 Receptor Radioligand Binding Assay: .(R)- and (S)-(4-Fluorophenyl)(4-((5-methyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)methanol was tested in a radioligand binding assay, according to the procedure described in Olah et al., Mol. Pharmacol. 1994, 45, 978-982 and Salvatore et al., Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 10365-10369, in human recombinant CHO-K1 cells expressing the human adenosine A3 receptor. Incubations of a range of concentration of each compound were carried out in duplicates for 1 h at 25° C. in 25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA, in the presence of 0.5 nM [125I] AB-MECA. Non-specific binding was determined in the presence of 1 uM IB-MECA.
349 4 3 5 3.6 Cc1cc(Nc2nc([C@H](O)c3ccc(F)cc3)nc3ccccc23)n[nH]1
CHEMBL2024150 aa3r_human Human No 8.5 Kd = 3.4 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrsAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrs
None None None COc1ccc(-n2nc3c(NC(=O)CCC(=O)NCCOCCOCCNC(=O)CCCCCNC(=O)COc4ccc(C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)nc4ccccc4n3c2=O)cc1
CHEMBL2024147 aa3r_human Human No 7.4 Kd = 38.0 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrsAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrs
426 4 2 8 2.9 COc1ccc(-n2nc3c(NC(=O)c4ccc(N)cc4)nc4ccccc4n3c2=O)cc1
CHEMBL4439336 aa3r_human Human No 7.4 Kd = 39.8 nM Funct
Competitive insurmountable antagonist activity at human A3 adenosine receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]-GTPgammaS binding measured after 30 minsCompetitive insurmountable antagonist activity at human A3 adenosine receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]-GTPgammaS binding measured after 30 mins
517 9 1 10 1.7 CCCn1c(=O)c2c(nc3cc(OC)ccn32)n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O
CHEMBL1625681 aa3r_human Human No 8.3 Kd = 4.9 nM Bind
Binding affinity to human recombinant A3 adenosine receptor expressed in CHO cellsBinding affinity to human recombinant A3 adenosine receptor expressed in CHO cells
295 2 1 3 2.5 CC[C@@H]1Cn2c(=N1)c1[nH]c(nc1n(c2=O)C)c1ccccc1
CHEMBL186113 aa3r_human Human Yes 8.3 Kd = 5.0 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of Cl-IB-MECA-mediated cyclic AMP productionAntagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of Cl-IB-MECA-mediated cyclic AMP production
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
CHEMBL2413248 aa3r_human Human No 8.3 Kd = 5.2 nM Bind
Binding affinity to human adenosine A3 receptor expressed in CHO cells by flow cytometric analysisBinding affinity to human adenosine A3 receptor expressed in CHO cells by flow cytometric analysis
None None None N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCCC(=O)Nc5nc6ccc(Cl)cc6c6nc(-c7ccco7)nn56)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O
CHEMBL2024152 aa3r_human Human No 8.3 Kd = 5.6 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrsAntagonist activity at human adenosine A3 receptor expressed in forskolin-stimulated CHO cells assessed as inhibition of NECA-induced CRE-SPAP gene transcription by measuring intracellular cAMP level after 5 hrs
1549 58 4 28 3.0 COc1ccc(-n2nc3c(NC(=O)CCC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)c4ccc(-c5c6ccc(=[N+](C)C)cc-6oc6cc(N(C)C)ccc56)c(C(=O)[O-])c4)nc4ccccc4n3c2=O)cc1
CHEMBL2413248 aa3r_human Human No 8.2 Kd = 6.7 nM Bind
Binding affinity to human adenosine A3 receptor expressed in CHO cells after 90 minsBinding affinity to human adenosine A3 receptor expressed in CHO cells after 90 mins
None None None N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCCC(=O)Nc5nc6ccc(Cl)cc6c6nc(-c7ccco7)nn56)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O
CHEMBL322968 aa3r_human Human No 7.2 Kd = 63.1 nM Funct
Antagonist activity at human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]GTPgammaS binding measured after 30 minsAntagonist activity at human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]GTPgammaS binding measured after 30 mins
322 3 1 6 1.4 COc1ccn2c(c1)nc1c2c(=O)[nH]c(=O)n1Cc1ccccc1
CHEMBL4462442 aa3r_human Human No 6.2 Kd = 631.0 nM Funct
Competitive surmountable antagonist activity at human A3 adenosine receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]-GTPgammaS binding measured after 30 minsCompetitive surmountable antagonist activity at human A3 adenosine receptor expressed in CHO cell membranes assessed as inhibition of 2-Cl-IB-MECA-induced [35S]-GTPgammaS binding measured after 30 mins
513 9 1 10 1.5 CCCn1c(=O)c2c(nc3cc(OC)ccn32)n(CCCNC(=O)c2ccc(S(C)(=O)=O)cc2)c1=O
CHEMBL1771603 aa3r_human Human No 11.0 Ki = 0.0 nM Funct
Antagonist activity at human adenosine A3 receptorAntagonist activity at human adenosine A3 receptor
376 3 2 8 1.3 Cn1cc2c(nc(NC(=O)N[n+]3ccccc3)n3nc(-c4ccco4)nc23)n1
CHEMBL118923 aa3r_human Human No 11.0 Ki = 0.0 nM Bind
Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 11.0 Ki = 0.0 nM Bind
Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counterDisplacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL118923 aa3r_human Human No 11.0 Ki = 0.0 nM Bind
Displacement of [3H]-MRE 3008-F20 from Human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [3H]-MRE 3008-F20 from Human Adenosine A3 receptor expressed in HEK293 cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 11.0 Ki = 0.0 nM Bind
Displacement of [3H]-MRE 3008-F20 from Human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [3H]-MRE 3008-F20 from Human Adenosine A3 receptor expressed in HEK293 cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL118923 aa3r_human Human No 11.0 Ki = 0.0 nM Bind
Displacement of [3H]MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by scintillation counterDisplacement of [3H]MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by scintillation counter
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 11.0 Ki = 0.0 nM Bind
Displacement of [3H]MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by scintillation counterDisplacement of [3H]MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by scintillation counter
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL118923 aa3r_human Human No 10.9 Ki = 0.0 nM Bind
Displacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in HEK293 cellsDisplacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in HEK293 cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 10.9 Ki = 0.0 nM Bind
Displacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in HEK293 cellsDisplacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in HEK293 cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL3754229 aa3r_human Human No 10.6 Ki = 0.0 nM Bind
Displacement of [125I]AB-MECA at human A3A receptor expressed in CHO cell membrane after 60 mins by scintillation counting methodDisplacement of [125I]AB-MECA at human A3A receptor expressed in CHO cell membrane after 60 mins by scintillation counting method
427 5 1 7 4.8 COc1ccc(C(=O)Nc2nc(-c3cccs3)nc3cn(-c4ccccc4)nc23)cc1
CHEMBL89852 aa3r_human Human No 10.5 Ki = 0.0 nM Bind
Binding affinity at cloned human adenosine A3 receptor expressed in HEK293 cells was determined using [125I]AB-MECA as radioligandBinding affinity at cloned human adenosine A3 receptor expressed in HEK293 cells was determined using [125I]AB-MECA as radioligand
477 6 1 5 6.1 CCO/C(O)=C1\C(C)=NC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1C#Cc1ccccc1
CHEMBL118923 aa3r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of [3H]-MRE 3008-F20 from Human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [3H]-MRE 3008-F20 from Human Adenosine A3 receptor expressed in HEK293 cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of [3H]-MRE 3008-F20 from Human Adenosine A3 receptor expressed in HEK293 cellsDisplacement of [3H]-MRE 3008-F20 from Human Adenosine A3 receptor expressed in HEK293 cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL118923 aa3r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by liquid scintillation countingDisplacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by liquid scintillation counting
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by liquid scintillation countingDisplacement of [3H]-MRE-3008-F20 from human adenosine A3 receptor expressed in CHO cells after 120 mins by liquid scintillation counting
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL118923 aa3r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cellsDisplacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 10.4 Ki = 0.0 nM Bind
Displacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cellsDisplacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL118923 aa3r_human Human No 10.3 Ki = 0.0 nM Bind
Displacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in HEK293 cellsDisplacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in HEK293 cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL332091 aa3r_human Human No 10.3 Ki = 0.0 nM Bind
Displacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in HEK293 cellsDisplacement of [3H]MRE3008-F20 from human adenosine A3 receptor expressed in HEK293 cells
375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1
CHEMBL119709 aa3r_human Human Yes 10.1 Ki = 0.1 nM Bind
Binding affinity to human adenosine A3 receptor by radioligand displacement assayBinding affinity to human adenosine A3 receptor by radioligand displacement assay
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL119709 aa3r_mouse Mouse Yes 10.1 Ki = 0.1 nM Bind
Displacement of [125I]N6-(-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from mouse recombinant adenosine A3 receptor expressed in HEK293 cellsDisplacement of [125I]N6-(-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from mouse recombinant adenosine A3 receptor expressed in HEK293 cells
510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I
CHEMBL1091268 aa3r_human Human No 10.0 Ki = 0.1 nM Bind
Displacement of [3H]NECA from human cloned adenosine A3 receptor expressed in CHO cellsDisplacement of [3H]NECA from human cloned adenosine A3 receptor expressed in CHO cells
383 4 1 7 2.9 Cn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccccc4)nc23)n1
CHEMBL340868 aa3r_human Human No 10.0 Ki = 0.1 nM Bind
In vitro binding affinity at human Adenosine A3 receptor from HEK293 cells by [125I]AB-MECA displacement.In vitro binding affinity at human Adenosine A3 receptor from HEK293 cells by [125I]AB-MECA displacement.
467 7 1 5 6.4 CCOC(=O)C1=C(c2ccccc2)Nc2cc(C)c(C(=O)OCC)cc2C1/C=C/c1ccccc1
CHEMBL144979 aa3r_human Human No 9.9 Ki = 0.1 nM Bind
Binding affinity for human adenosine A3 receptorBinding affinity for human adenosine A3 receptor
434 4 2 7 4.8 COc1ccc(NC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL145767 aa3r_human Human No 9.9 Ki = 0.1 nM Bind
Binding affinity for human adenosine A3 receptorBinding affinity for human adenosine A3 receptor
390 4 3 8 2.9 COc1ccc(NC(=O)Nc2nc3n[nH]cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL348975 aa3r_human Human No 9.9 Ki = 0.1 nM Bind
Binding affinity for human adenosine A3 receptorBinding affinity for human adenosine A3 receptor
402 4 2 8 3.7 CCn1cc2c(nc(NC(=O)Nc3ccc(C)cc3)n3nc(-c4ccco4)nc23)n1
CHEMBL145767 aa3r_human Human No 9.9 Ki = 0.1 nM Bind
Binding affinity to human adenosine A3 receptorBinding affinity to human adenosine A3 receptor
390 4 3 8 2.9 COc1ccc(NC(=O)Nc2nc3n[nH]cc3c3nc(-c4ccco4)nn23)cc1
CHEMBL209992 aa3r_human Human No 9.9 Ki = 0.1 nM Bind
Displacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cellsDisplacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cells
404 3 3 8 2.9 CCn1cc2c(n1)N=C(NC(=O)Nc1ccc(C)cc1)N1NC(c3ccco3)=NC21
CHEMBL144979 aa3r_human Human No 9.9 Ki = 0.1 nM Bind
Displacement of [3H]MRE3008-F20 from human Adenosine A3 receptor expressed in HEK cells; range 0.08-0.24Displacement of [3H]MRE3008-F20 from human Adenosine A3 receptor expressed in HE